Showing papers in "International Journal of Pharmacy and Pharmaceutical Sciences in 2017"
TL;DR: In this paper, the authors extracted gelatin from the scales of a freshwater fish, Labeo rohita, and performed proximate analysis and physico-chemical analysis of the fish scale gelatin.
Abstract: Objective: Gelatin is widely used biopolymer in various industries due to its excellent biocompatibility, biodegradability properties. In the present study, gelatin was extracted from fish wastes, as an alternative source. Methods: This biopolymer was extracted from the scales of freshwater fish, Labeo rohita . After extraction, the proximate analysis and physico-chemical analysis of the fish scale gelatin were carried out. This functional polymer was also characterized using different analytical methods, such as UV-vis spectroscopy, scanning electron microscopy (SEM), and X-ray diffraction (XRD) for the evaluation of crystalline and surface morphology, and fourier transform infrared spectroscopy (FTIR) for structural determination. Results: The scales of L. rohita yield 24% (dry weight basis) of gelatin, indicating this fish species as potential source of gelatin. The proximate analysis determined was low moisture content (4.2%), ash (1.4%) and high protein (90%) content. The result of the study confirms the effectiveness of extraction method used. Conclusion: The fish scales of L. rohita are found to be a sustainable and renewable source of gelatin with desirable functionalities and it is the best alternative for mammalian gelatin in food and other industries.
81 citations
TL;DR: In this paper, the green synthesis of silver nanoparticles using marine the red alga Spyridia fusiformis and antibacterial activity was carried out. Methods: the seaweed extract was used for the synthesis of AgNPs at room temperature.
Abstract: Objective: In the present system, the green synthesis of silver nanoparticles using marine the red alga Spyridia fusiformis and antibacterial activity was carried out . Methods: The seaweed extract was used for the synthesis of AgNPs at room temperature. The silver nanoparticles were characterized by using UV–Visible spectroscopy, Fourier transform infrared spectroscopy, transmission electron microscope and X-ray diffraction (XRD) techniques. The antibacterial activity of biosynthesized silver nanoparticles was carried out by disc diffusion method against pathogenic bacteria. Results: The UV-visible spectroscopy revealed surface plasmon resonance at 450 nm. The FT-IR measurements showed the possible functional groups responsible for the formation of nanoparticles. The X-ray diffraction analysis showed that the particles were crystalline in nature. TEM micrograph has shown the formation of silver nanoparticles with the size in the range of 5–50 nm. The silver nanoparticles synthesized from the S. fusiformis showed higher activity and proved their efficacy in controlling the pathogenic bacterial strains. The nanoparticles showed highest inhibition activity on K. pneumaniae and S. aureus up to 26 and 24±0.01 mm at 100 μg/ml of nanoparticles. Conclusion: The synthesised AgNPs have shown the best antibacterial activity against human pathogens E. coli, K. pneumoniae, S. aureus and P. aeruginosa . The above eco-friendly AgNPs synthesis procedure could be a viable solution for industrial applications in the future and therapeutic needs.
43 citations
TL;DR: The results clearly indicate a promising potential of the use of cashew bark exudate gum as a gelling material with HPMC K4M to prepare 4 % lidocaine HCl topical gels of good skin permeation capability.
Abstract: Objective: The objective of the current work was to prepare and evaluate ex vivo skin permeation of cashew bark exudate gum based 4 % lidocaine HCl topical gels. Methods: In the current work, 4 % lidocaine HCl topical gels were prepared by using different concentrations of cashew bark exudate gum, HPMC K4M, lidocaine HCl, methyl paraben (as preservative) and glycerin (as plasticizer). The formulated topical gels were evaluated for pH, viscosity, and ex vivo skin permeation through excised porcine ear skin membrane. Results: The pHs of these formulated 4 % lidocaine HCl topical gels were found within the range of 6.04±0.02 to 6.52±0.04; whereas, the viscosities were measured within the range, 4.38±0.02 x 10 6 to 4.74±0.04 x 10 6 cps. Sustained ex vivo permeation of lidocaine was measured over 7 h. Highest ex vivo permeation flux was measured when 0.1 % menthol was incorporated as a permeation enhancer. It was also higher than that of the marketed 4 % lidocaine HCl topical gel. The stability study by freeze thaw cycle method revealed physically stable gels without the occurrence of syneresis. Conclusion: The results clearly indicate a promising potential of the use of cashew bark exudate gum as a gelling material with HPMC K4M to prepare 4 % lidocaine HCl topical gels of good skin permeation capability
37 citations
TL;DR: A promising potential is indicated of the use of cashew gum as matrix forming a material with HPMC K4M to prepare matrix tablets for gastro retentive delivery of hydralazine HCl through the combined approach of floatation and bioadhesion to reduce the dosing rate with better patient compliances.
Abstract: Objective: The objective of this paper was to prepare and evaluate floating-bioadhesive cashew gum-hydroxypropyl methylcellulose (HPMC K4M) matrix tablets for the gastro-retentive release of hydralazine HCl. Methods: The cashew gum-HPMC K4M matrix tablets of hydralazine HCl were prepared by direct compression method with the incorporation of sodium bicarbonate and citric acid as effervescent agents. Drug contents, weight variations, hardness, friability, in vitro swelling, in vitro floatation, ex vivo mucoadhesion and in vitro drug release of these matrix tablets were evaluated. Results: Drug contents, weight variations, hardness and friability of these matrix tablets were within the compendia limits. These tablets were floated well in vitro over 12 h in simulated gastric fluid (SGF, pH 1.2) with minimum lag time. The ex vivo adhesion of these matrix tablets with goat intestinal mucosa exhibited good bioadhesion in a wash off test. All these cashew gum-HPMC K4M floating-bioadhesive matrix tablets of hydralazine HCl showed in vitro sustained releases of hydralazine HCl over 12 h in SGF, pH 1.2. The in vitro hydralazine HCl followed Korsmeyer-Peppas kinetic model and anomalous (non-Fickian) diffusion mechanism. The drug-polymer compatibility analysis by FTIR spectroscopy indicated the absence of any drug-polymer interaction within this cashew gum-HPMC K4M floating-bioadhesive matrix tablets of hydralazine HCl. Conclusion: The results clearly indicate a promising potential of the use of cashew gum as matrix forming a material with HPMC K4M to prepare matrix tablets for gastro retentive delivery of hydralazine HCl through the combined approach of floatation and bioadhesion to reduce the dosing rate with better patient compliances.
37 citations
TL;DR: The present review summarizes up to date information of various biological activities of isoxazole analogs, reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, antiinflammatory activity, antioxidant activity, anticancer activity, CNS activity, antitubercular activity and miscellaneous activities.
Abstract: Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group & found in many β-lactamase resistant antibiotics, such as cloxacillin, dicloxacillin and flucloxacillin. The synthetic androgenic steroid danazol also has an isoxazole ring. The substituted isoxazoles are well developed in literature to posses significant biological activities. The disubstituted and trisubstituted isoxazoles have been reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, antiinflammatory activity, antioxidant activity, anticancer activity, CNS activity, antitubercular activity and miscellaneous activities like GABA agonistic activity, inhibitory activity, antihypertensive activity, and glutamate transporter activity. The present review summarizes up to date information of various biological activities of isoxazole analogs.
35 citations
TL;DR: In this article, a cross-linked keratin hydrogel was prepared by integrating keratin from chicken feather into an aloe-vera, Chitosan and honey based dressing formulation separately.
Abstract: Objective : A novel cross-linked keratin hydrogel was prepared by integrating keratin from chicken feather into an aloe-vera, Chitosan and honey based dressing formulation separately. Methods : Keratin fibres extracted from chicken feathers are eco-friendly, non-abrasive, biodegradable, insoluble in organic solvents and having good mechanical properties, hydrophobic behaviour, low density and finally cheap. Keratin based hydrogels were prepared with five types of ingredients and studied for their wound healing properties. The analysis of keratin-based hydrogel was done by Fourier Transform Infra-red Spectroscopy (FTIR) and X-ray diffraction (XRD) analysis. Results : Keratinocytes containing keratin travel from the wound border to initiate the process of healing. The characteristics of keratin-based hydrogel derived from chicken feather made it an effective wound care therapeutic product. X-ray diffraction (XRD) analysis showed the crystallinity index in between 30-50% of the hydrogen. Conclusion : The test for swelling and solubility were carried out on the hydrogen to determine the solid content and water absorbance capacity. Overall, this product is safe to use as an effective wound healing product with appropriate properties.
33 citations
TL;DR: Tolerant trees species can serve as a sink, and sensitive tree species can act as an indicator for air pollution mitigation, provides useful insights for selecting tolerant species for future planning and Greenbelt development in urban areas.
Abstract: Objective: Air pollution is one of the major global tribulations in many developing cities around the world. Addressing this sort of pollution is more intricate than other ecological challenges. As pollution is an upcoming issue, we aimed at assessing the air pollution tolerant plants from roadside exposed to vehicular air pollution from two different locations in Thane city. Methods: In the present study, commonly available ten roadside tree species selected from polluted and control area, and their air pollution tolerance index (APTI) determined in Thane city. The biochemical parameters viz. pH, ascorbic acid, total chlorophyll, relative water content (RWC) were considered to calculate APTI by using standard method. Results: The study shows that the control site has more APTI than the polluted site. The APTI observed minimum in Tectona grandis 5.2±0.3247 and maximum in Azadirachta indica 13.5±0.4404. Reduction in APTI at polluted site shows that Alstonia scholaris (6.6%), Tamarindus indica (8.8%) and Azadirachta indica (10.3%) were the most tolerant tree species, while Tectona grandis (47.5%) , Acacia nilotica (27.4%) and Cassia fistula (20.7%) were more sensitive tree species. The results showed the order of tolerance (% difference in APTI) as Alstonia scholaris (6.6%)>Tamarindus indica (8.8%)>Azadirachta indica (10.3%)>Moringa pterygosperma (11.9%)>Mangifera indica (13.9%)>Bahunia variegate (14.3%)>Annona squamosa (18.7%)>Cassia fistula (20.7%)>Acacia nilotica (27.4%)>Tectona grandis (47.5%). Conclusion: Tolerant trees species can serve as a sink, and sensitive tree species can act as an indicator for air pollution mitigation. Thus, this study provides useful insights for selecting tolerant species for future planning and Greenbelt development in urban areas.
28 citations
TL;DR: In this paper, the in vitro total phenolics, flavonoids contents, antioxidant and antimicrobial activities of various solvent extracts from the medicinal plant Physalis minima Linn were estimated using Folin-Ciocalteu and aluminium chloride colorimetric methods respectively.
Abstract: Objective: To estimate the in vitro total phenolics, flavonoids contents, antioxidant and antimicrobial activities of various solvent extracts from the medicinal plant Physalis minima Linn . Methods: The crude bioactive were extracted from the dried powder of Physalis minima using methanol, ethyl acetate, chloroform and hexane solvents. Total phenolic content (TPC) and total flavonoid content (TFC) were estimated using Folin-Ciocalteu and aluminium chloride colorimetric methods respectively. 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2 ’ -azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and ferric reducing antioxidant power (FRAP) assays were used to determine the in vitro antioxidant capacity. The antimicrobial assay was done through agar well diffusion; minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined using broth microdilution methods against the Gram-negative bacteria ( Klebsiella pneumoniae , Escherichia coli , Pseudomonas aeruginosa , Proteus vulgaris ) and Gram-positive bacteria ( Staphylococcus aureus ). Results: TPC expressed as gallic acid equivalents (GAE) ranged from 60.27±1.73-151.25±2.50 mg GAE/g dry weight, and TFC expressed as quercetin equivalents (QE) ranged from 56.66±0.80-158.84±2.30 mg QE/g dry weight. Methanol extract showed the highest antioxidant activity followed by ethyl acetate, chloroform, hexane extract and the IC 50 values of methanol extract for scavenging DPPH and ABTS free radicals were 280.23±5.75-173.40±0.38µg/ml, respectively. All the extracts have shown potent antimicrobial activity for the zone of inhibition ranged from 9-35 mm; MICs and MBCs values ranged from 0.125-4.0 and 0.25-8.0 mg/ml, respectively towards tested pathogenic species. Conclusion: The comprehensive analysis of the present results demonstrated that Physalis minima possess high potential antioxidant properties which could be used as a viable source of natural antioxidants in treating infections caused by above-mentioned pathogens.
25 citations
TL;DR: In this paper, a Bougainvillea x buttiana (var. Rose) Holttum and Standl extract (BxbREE) was prepared and its chemical composition, antioxidant and anti-inflammatory activity were evaluated.
Abstract: Objective: A Bougainvillea x buttiana (var. Rose) Holttum and Standl extract (BxbREE) was prepared and its chemical composition, antioxidant and anti-inflammatory activity were evaluated. Methods: For the analyses of the phytochemical compounds present in BxbREE extract, gas chromatography-mass spectrometry (GC/MS) was used. To explore the anti-oxidant, anti-inflammatory activities, total phenolic contents, carbohydrates, lipids and carrageenan-induce paw edema models, respectively, were used. For in vivo experiments, the extract was orally, intraperitoneally and/or subcutaneously administered at doses of 0.04, 0.4, 4 and 40 mg/kg. Results: GC/MS analyses showed the presence of 7 compounds, including 2-Propenoic acid, 3-(2-hydroxyphenyl)-, (E)-(1.19%); 2-Methoxy-4-vinylphenol (0.22%); 3-O-Methyl-d-glucose (92.14%); n -Hexadecanoic acid (0.76%); Hexadecanoic acid, ethyl ester (1.17%); 9,12-octadecadienoic acid, ethyl ester (1.93%); and 9,12,15-Octadecatrienoic acid, ethyl ester (Z,Z,Z) (2.59%). Phytochemical qualitative analysis showed the presence of total phenolic contents at 320 mg of Gallic acid Equivalent/gram of dried extract (GA-Eq/g extract); carbohydrates 5.18 mg/ml and lipids 13.88 mg/ml. In accordance the structures the major compound was 3-O-Methyl-d-glucose. Our results also clearly indicate that BxbREE decreases inflammation in BALB/c mice as a subplantar injection of carrageenan-induced paw edema. The extract presented a potent dose-dependent inhibitory effect. The edema inhibition percentage was significantly lower in groups of animals treated with BxbREE by via intraperitoneal or subcutaneous when compared with those results obtained for groups treated by orally administration (p<0.001). Conclusion: In conclusion, this study established the anti-oxidant and anti-inflammatory activities of Bougainvillea x buttiana (var. Rose); also, this extract could be considered to be a natural anti-oxidant agent that represents an anti-inflammatory remedy.
24 citations
TL;DR: A simple, accurate, precise, linear, rugged and rapid RP-HPLC method was developed for quantitative estimation of sofosbuvir in human plasma and should be suitable for conducting pharmacokinetics studies and therapeutic drug monitoring.
Abstract: Objective: This study points to build up and validate a simple methodology to quantify the most used drug sofosbuvir for the treatment of hepatitis C virus (HCV) infection, in human plasma by using atazanavir as an Internal Standard (IS) for preclinical studies and validate as per USFDA guidelines. Methods: Sofosbuvir was isolated from plasma samples by liquid-liquid extraction method using acetonitrile; good chromatographic separation was achieved on Kromasil Column (250 mm ×4.6 mm, 5 µm). The mobile phase consisted of 0.1 % orthophosphoric acid (OPA) buffer pH 2 and acetonitrile in the ratio of (68:32, v/v), respectively. The analysis time was 7 min at a flow rate 1 ml/min. The photodiode array detector (PDA) detection was carried out at 228 nm. The suggested method was validated by performing linearity, system suitability, specificity and sensitivity, accuracy and precision, recovery, ruggedness, stability studies. The method was validated as per USFDA guidelines. Results: The developed method resulted in retention times of sofosbuvir and IS were found out to be 4.7 and 4.2 min respectively. The calibration curves are linear (r2 = 0.999) over the concentration range of 0.050-2.0 µg/ml of plasma analytes concentration. LOQ value was found to be 0.050 µg/ml with precision and accuracy. Within-batch % mean accuracy of the method ranged between 96.00% and 109.09%, and within-batch and total precision, expressed as the coefficient of variation, was 1.40–10.33%. Overall percentage mean recovery of sofosbuvir from spiked plasma was 84.14%. All the validated parameters were found to be within the limit. Conclusion: A simple, accurate, precise, linear, rugged and rapid RP-HPLC method was developed for quantitative estimation of sofosbuvir in human plasma and should be suitable for conducting pharmacokinetics studies and therapeutic drug monitoring.
21 citations
Journal Article•
TL;DR: Given that various species of Cinnamomum are being widely used in traditional medicine and culinary purposes, their main therapeutic aspects, toxicity, and adverse effects warrant further investigation in the future.
Abstract: The objective of this review is to systematically appraise the literature available to date on biological activities ( in vitro and in vivo ) of extracts and constituents from Cinnamomum . An extensive review of the literature available in various recognised databases including PubMed, Google Scholar and Scopus on the biological activities of various species of the Cinnamomum were undertaken. The literature provided information on biological activities of the species of the genus Cinnamomum . Crude extracts and constituents from about 30 species of Cinnamomum displayed significant antibacterial, antifungal, antiseptic, antiviral, anti-inflammatory, antipyretic, antioxidant, chemopreventive, cytotoxic, antidiabetic, hypolipidemic, antispasmodic, antiulcer, antiplatelet, anodyne, choleretic, immunostimulant, anaesthetic and sedative activities. Essential oil, aqueous/alcoholic extracts, cinnamaldehyde and proanthocyanidins were reported to be mainly responsible for biological activities displayed by most of the plants. Plants of Cinnamomum genus possess a wide spread of biological activities validating their use in traditional medicine. However, most of the available references lack information on active constituents, doses, duration of the treatment, storage conditions and positive controls for examining biological activities. The molecular mechanisms involved in eliciting biological activities were not comprehensively elucidated. Investigations to prove the safe use of these plants in traditional medicine are very limited. Thus, more studies on identification of bioactive constituents and their molecular mechanisms are needed. In addition, given that various species of Cinnamomum are being widely used in traditional medicine and culinary purposes, their main therapeutic aspects, toxicity, and adverse effects warrant further investigation in the future.
TL;DR: Results reflected significant relations and inter-relationships between oxidative stress and inflammation markers in type 2 diabetes in its early stage and indicated that metformin may need to be combined with another drug.
Abstract: Objective: Great interest is directed to inflammation and oxidative stress involvement in type 2 diabetes pathogenesis. Many researchers suggest they play roles but exactly how is still not clear enough. This encouraged us to investigate relations and potential inter-relationships between them and insulin resistance in type 2 diabetes in its early stage. Whether metformin drug alone, as frequently prescribed, is enough for type 2 diabetes management in this early stage was an objective. Methods: Blood sugar indices, adiponectin (ADIPOQ), tumor necrosis factor-α (TNF-α), malondialdehyde (MDA), nitric oxide (NO), C-reactive protein (CRP), liver and kidney function tests and lipid profile were monitored in non-diabetic volunteers, pre-diabetic and newly diagnosed type 2 diabetic patients before and after metformin drug utilization for 5 mo. Results: MDA, inflammation markers and alanine aminotransferase (ALT) were elevated, and blood sugar indices and lipid profile showed pathological alterations in diabetics compared to non-diabetics; changes were worse in type 2 cases. They were improved to different degrees by metformin treatment except for pancreatic β-cells function and ADIPOQ level showed no significant improvements and it couldn’t normalize ALT. Conclusion: Results reflected significant relations and inter-relationships between oxidative stress and inflammation markers in type 2 diabetes in its early stage and indicated that metformin may need to be combined with another drug.
TL;DR: In this article, a series of benzothiazole derivatives 7(a-l) were synthesized and synthesised compounds were characterised for different physical and chemical properties like molecular formula, molecular weight, melting point, percentage yield, Rf value, IR, 1 HNMR, 13 CNMR and mass spectroscopy.
Abstract: Objective: The objective of the present research investigation involves synthesis and biological evaluation of antidiabetic activity of benzothiazole derivatives. Methods: A novel series of benzothiazole derivatives 7(a-l) were synthesised and synthesised compounds were characterised for different physical and chemical properties like molecular formula, molecular weight, melting point, percentage yield, Rf value, IR, 1 HNMR, 13 CNMR and mass spectroscopy. The newly synthesised benzothiazole derivatives were subsequently assayed in vivo to investigate their hypoglycemic activity by the alloxan-induced diabetic model in rats. Results: All the synthesised derivatives showed significant biological efficacy. The compound 7d at 350 mg/kg exerted maximum glucose lowering effects whereas 7c showed minimum glucose lowering effects. All the compounds were effective, and experimental results were statistically significant at p<0.01 and p<0.05 level. Conclusion: From the results, it is clear that compound 7d demonstrated potent anti-diabetic activity and would be of better use in drug development to combat the metabolic disorder in future.
TL;DR: The role of herbal plants and their phytoconstituents against neurodegenerative diseases and other related disorders are highlighted, focusing on their mechanism of action and therapeutic potential.
Abstract: Neurodegeneration refers to a condition of neuronal death occurring as a result of progressive disease of long termand is becoming a major health problem in the 21st century. Neurons degenerated are not replaced resulting in cognitive loss ,many neurodegenerative disorders, such as schizophrenia, depression, Alzheimer's Disease (AD) dementia, cerebrovascular impairment, seizure disorders, head injury, Parkinsonism. Neuroprotection refers to the strategies and possible mechanisms that are able to protect the central nervous system (CNS) against neuronal injury and neurodegenerative disorders. The past decade has witnessed an intense interest in herbal plants having long-term health promoting or medicinal qualities. Comprehensive research and discovery has demonstrated that natural products, medicinal herbs, plant extracts, and their metabolites, have great potential as neuroprotective agent. Although the precise mechanisms of action of herbal drugs have yet to be determined, some of them have been shown to exert anti-inflammatory and/or antioxidant effects. Thus the herbal plants can be a valuable source of drug against neurodegenerative disorders which will require high-throughput screening. This review will highlight the role of herbal plants and their phytoconstituents against neurodegenerative diseases and other related disorders, focusing on their mechanism of action and therapeutic potential. Keywords:
TL;DR: The utility of eosin dye in quality control laboratories as an ion pairing agent for drug analysis was discussed in this paper, where the utility of spectrofluorimetry over spectrophotometry was discussed.
Abstract: Globally, dyes are widely used in the pharmaceutical, food, textile, cosmetics, plastics, leather, paint, ink and paper industries. Eosin is an acidic orange-pink dye and has very strong staining properties. Haematoxylin and eosin Y (H&E) combination is the most common staining and primary diagnostic technique in histo-pathological laboratories. This review mainly discussed the utility of eosin dye in quality control laboratories as an ion pairing agent for drug analysis. Eosin Y is one the most common ion pairing agent and its mono and di anionic forms of eosin Y are capable of interacting with many drug molecules to form colored/fluorescent binary or ternary complexes that can be analyzed with or without extraction by spectrofluorimetry and/or spectrophotometry. Quenching fluorescence and advantages of spectrofluorimetry over spectrophotometry were also discussed. Fluorescence detection greatly enhances the sensitivity and providing a sensitive and relatively inexpensive instrumental method of analysis using eosin Y for various important drugs in pure, commercial dosage forms and biological fluids
TL;DR: It is proposed that gold nanoparticles synthesized and conjugated with doxorubicin from G. lucidum might be a significant resource of drug delivery for anti-cancer preparation that may advantage breast cancer treatment.
Abstract: Objective: The present investigations are to mycosynthesis and characterization of gold nanoparticles conjugated with doxorubicin and evaluated anticancer activity. Methods: The characterization of the gold nanoparticles using ultraviolet–visible spectroscopy. FTIR investigations were carried out to find and read the functional group responsible designed at the bioconversion of gold ions and crystalline arrangement of gold nanoparticles was detected in the XRD study. The gold nanoparticles conjugated with doxorubicin were treated against MCF-7-dox resisted breast cancer cells and observed the in vitro cytotoxicity by MTT assay, SCGE (Comet), Apoptosis and Mito-potential assay. Further more we determinate the mRNA expression of ABCB1 gene and cDNA was synthesized from the mRNA for amplification of the ABCB1 gene corresponding to the specific primer. Results: Surface Plasmon resonance showed the development of gold nanoparticles in UV–Visible spectra at 537 nm. The synthesized gold nanoparticles were polydisperse spherical and it was determined by EDAX and stabilized in the solution to the spherical shapes further confirmed by High-resolution transmission electron microscope analysis designate in the reading of 2–100 nm. The anticancer assays were given significant results and the mRNA expression of ABCB1 gene and cDNA was amplified as directly proportional to the expression of ABCB1 gene. Conclusion: We propose that gold nanoparticles synthesized and conjugated with doxorubicin from G. lucidum might be a significant resource of drug delivery for anti-cancer preparation that may advantage breast cancer treatment.
TL;DR: The ability of these newly developed hydrogel beads containing nimesulide for its sustained release could possibly be advantageous to patient compliance with reduced dosing interval is demonstrated.
Abstract: Objective: The objective of this study was to formulate and evaluate the drug release studies using locust bean gum (LBG) and sodium alginate (NaAlg) and cross-linked with glutaraldehyde for the controlled release (CR) of nimesulide, an anti-inflammatory drug. Methods: Locust bean gum (LBG) and sodium alginate (NaAlg) blend hydrogel beads were prepared by an extrusion method using glutaraldehyde as a crosslinker. Nimesulide an anti-inflammatory drug was encapsulation within LBG/NaAlg blend hydrogel beads. Morphology, size, encapsulation efficiency and drug release from these hydrogel beads were evaluated by different characterization techniques such as fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), x-ray diffraction (X-RD) studies. Results: Drug-loaded hydrogel beads were analyzed by FTIR, which indicates the interaction between drug and polymers. DSC thermograms on drug-loaded microbeads confirmed the polymorphism of nimesulide and indicated a molecular level dispersion of the drug in the hydrogel beads. SEM confirmed the spherical nature and rough surface of the hydrogel beads produced. X-RD study was performed to understand the crystalline nature of drug after encapsulated into the hydrogel beads and confirmed the complete dispersion of the drug in the polymer matrix. In vitro release studies conducted in pH-7.4 which indicated a dependence of release rate on the amount of drug loading and the amount of LBG/NaAlg, but slow release rates were extended up to 48 h. The cumulative release data were fitted to an empirical equation to compute diffusion exponent (n) which indicated the non-fickian trend for drug release. Conclusion: These results clearly demonstrated that the ability of these newly developed hydrogel beads containing nimesulide for its sustained release could possibly be advantageous to patient compliance with reduced dosing interval.
TL;DR: It was clear from the study that seaweeds incorporated in small amounts in the dishes consumed in the daily diet can bring a control on postprandial blood glucose level.
Abstract: Objective: The present work was to investigate the alpha amylase and alpha-glucosidase inhibitory activity of the selected edible seaweeds. Methods: The seaweeds namely Acanthophora spicifera, Gracilaria corticata, Gracilaria edulis, Ulva lactuca and Ulva reticulata were selected for this study. Six and eight hours of ethanol and aqueous extract were used for the estimation of alpha amylase using DNS method and alpha-glucosidase inhibition activity. Results: The study reported that the solvent from ethanol and aqueous in eight hours of extraction showed a higher inhibitory activity than six hours of extraction. Maximum of 89.1±0.96 and 79.55±3.08 percent of alpha-amylase and alpha-glucosidase inhibition activity were detected in the eight hours of aqueous extract (0.5 ml) of Ulva reticulata and Gracilaria edulis respectively. All the selected edible seaweeds had significant differences (p<0.05) in alpha amylase and alpha glucosidase inhibition activity between the selected seaweeds with different extracts. Conclusion: It was concluded that all the selected edible seaweeds have the potential to act as a potent inhibitor of the carbohydrate hydrolyzing enzyme. Thus, it was clear from the study that seaweeds incorporated in small amounts in the dishes consumed in the daily diet can bring a control on postprandial blood glucose level.
TL;DR: Extemporaneous compounding practice are an essential part of pharmacist’ competency and these unique skills need to be preserved and regulations that cover rationalisedCompounding practice is necessary.
Abstract: Objective: To identify the frequency and scope of extemporaneous compounding practice reported in community and hospital pharmacies. Method s : A systematic literature review was undertaken to identify the prevalence of extemporaneous compounding practice in community and hospital pharmacies, including the reasons of providing compounding services. Results: Nine studies were identified and evaluated in which extemporaneous products prepared by pharmacist could be identified. Most of the studies record that prevalence of extemporaneous compounding practice is very low (less than 5%). Prescribing of compounded medicines occurs more frequently in paediatrics and for special patients’ need. The major types of extemporaneous compounding products were dermatological dosage forms and followed by oral solutions and oral suspensions. Reasons for providing compounding practice were to make a customised products that not available commercially and to provide full pharmaceutical care to patients. Issues about the stability of compounded products, accuracy in dose strength and lack of standardised protocol in extemporaneous compounding need to be addressed. Conclusion: Extemporaneous compounding practice are an essential part of pharmacist’ competency. These unique skills need to be preserved and regulations that cover rationalised compounding practice is necessary.
TL;DR: BD-T was found to be more effective, safe and tolerable for the treatment of psoriasis compared with the marketed product.
Abstract: Objective: The main aim of this study was to design and characterise betamethasone di-propionate loaded transfersomes (BD-T); as a topical formulation for the treatment of localized plaque psoriasis. Methods: A full factorial design (2 3 ) was applied to study the effects of three independent variables: drug content, type of surfactants and surfactant contents on particle size (PS), entrapment efficiency (EE %), zeta potential (ZP), polydispersity index (PI) and drug release profiles. The optimized BD-T was formulated as a hydrogel using 5% sodium carboxymethyl cellulose. The gel was characterized for viscosity, drug content, in vitro drug release and stability. A comparative clinical study was performed on 20 patients with psoriasis to investigate the effect of BD-T gel and the marketed betamethasone dipropionate (BD) cream. Results: The optimized BD-T formulation containing 50 mg betamethasone dipropionate (BD) and 5 mg tween 80 showed spherical unilamellar vesicles with an average particle size of 242.80, % EE of 90.19%, ZP of-15.00 mV, PI of 0.407 and K 0 of 4.290 mg/hr. The formulation showed good stability at 4 °C and 25 °C for 6 mo. The results revealed significant clinical improvement and a significant increase in safety and tolerability with BD-T gel compared with BD cream. Conclusion : As a conclusion, BD-T was found to be more effective, safe and tolerable for the treatment of psoriasis compared with the marketed product.
TL;DR: In this paper, drug loaded matrix type transdermal films of imipramine hydrochloride were prepared by the solvent evaporation method with the help of polymers along with polyethene glycol (PEG) 400 was used as plasticizer and dimethyl sulfoxide (DMSO) is used as penetration enhancer.
Abstract: Objective: The aim of the present investigation was to form matrix type transdermal patches containing imipramine hydrochloride were prepared using two polymers by solvent evaporation technique to minimise the dose of the drug for lesser side effect and increase the bioavailability of a drug. Methods: In the present study, drug loaded matrix type transdermal films of imipramine hydrochloride were prepared by the solvent evaporation method with the help of polymers along with polyethene glycol (PEG) 400 was used as plasticizer and dimethyl sulfoxide (DMSO) was used as penetration enhancer. Drug-polymer interactions determine by FTIR and a standard calibration curve of imipramine hydrochloride was determined by using UV estimation. Results: The formulated transdermal patch by using PVP K-30, HPMC K100M showed good physical properties. All prepared formulations indicated good physical stability. The formulation F-1 gave the most suitable transdermal film with all desirable physicochemical properties. The thickness of the patches was varied from 0.263±0.67 mm to 0.301±0.61 mm, uniformity of patches showed that patches prepared by solvent evaporation while low standard deviation values ensued by thickness measurements of the film, and weights ranged between 50.5±0.75 mg and 52.15±2.15 mg, which indicates that different batches patch weights, were comparatively similar. Folding endurance was found to be>200 that is satisfactory for the patches, drug content was found to be 5.33±0.14 mg to 5.57±0.095 mg. In vitro, drug permeation studies of formulations were performed by using K-C diffusion cells using abdomen skin of the albino rat. The results were best in in -vitro skin permeation through rat skin as compared to all other formulations prepared with a hydrophilic polymer containing permeation enhancer. The formulation, F1 is considered as the best formulation, since it shows maximum in vitro drug release as 84.71±3.07 % at 24 h. The drug release kinetics studies showed that the majority of formulations were governed by Higuchi model and mechanism of release was non-Fickian mediated. Conclusion: In conclusion, controlled release transdermal drug delivery system (TDDS) patches of imipramine hydrochloride can be prepared using the polymer combinations, with plasticizer and enhancer. The release rate of drug through patched increased simultaneously as the concentration of hydrophilic polymer was increased. However, the mechanism of drug release of all formulations was non-Fickian. The properties of a film did not change during the period of study.
TL;DR: All the synthesized compounds have exhibited promising anti-TB, antimicrobial and antioxidant activities and some of the compounds have shown promising antioxidant properties.
Abstract: Objective: The aim of this study was to the synthesis of indole, coumarinyl and pyridinyl derivatives of isoniazid as potent anti-TB and antimicrobial agents and their molecular docking studies. Methods: The structures of the newly synthesized compounds were confirmed by FT-IR, 1 HNMR, and Mass spectroscopic methods and to evaluate the biological studies like anti-TB, antimicrobial and antioxidant activities. The mode of action of these active compounds was carried out by molecular docking studies. Results: Among all the synthesized compounds tested 5d was found to be the most active with M. tuberculosis H 37 Rv strain at 12.5µg/ml, 5b at 25µg/ml, 4d was found to be the most active with S. typhi, S. aureus and A. Nizer , 5a with A. Oryzae , 5c with A. terrous and A. Flavous and 5d with Shegella at 100µg/ml and some of the compounds like 4d, 5a, 5b and 5d have shown promising antioxidant properties. Conclusion: All the synthesized compounds have exhibited promising anti-TB, antimicrobial and antioxidant activities.
TL;DR: In this paper, the effects of solvent polarity on solvation free energy, dipole moment, polarizability, first order hyperpolarizability and different molecular properties like chemical hardness and softness, chemical potential, electronegativity, electrophilicity index of aspirin which may lead to better understand the reactivity and stability of aspirin in different solvent systems.
Abstract: Objective: The aim of the study is to explore the effects of solvent polarity on solvation free energy, dipole moment, polarizability, first order hyperpolarizability and different molecular properties like chemical hardness and softness, chemical potential, electronegativity, electrophilicity index of aspirin which may lead to better understand the reactivity and stability of aspirin in different solvent systems. Methods: Becke, 3-parameter, Lee-Yang-Parr (B3LYP) level of theory with 6-31G(d,p) basis set was employed to conduct all type of calculations for both in the gas phase and in solution. The solvation free energy, dipole moment and molecular properties were calculated by applying the Solvation Model on Density (SMD) in four solvent systems namely water, methanol, ethanol and n -octanol. Results: The solvation energies steadily increased as the dielectric constant was decreased i.e. free energy increases with decreasing polarity of the solvent. The dipole moment of aspirin was found to be increased when going from non-polar to polar solvents. The dipole moment of aspirin was higher in different solvents than that of the gas phase. The polarizability and first order hyperpolarizability were also increased with the increasing dielectric constant of the solvent. Moreover, ongoing from non-polar to polar solvent the chemical potential, electronegativity and electrophilicity index were increased except in n -octanol. The chemical potential, electronegativity and electrophilicity index of aspirin in n -octanol was higher than that of ethanol. On the other hand, chemical hardness was increased with decreasing polarity of the solvent and the inverse relation was found in the case of softness. Conclusion: The calculated solvation free energy, dipole moment, polarizability, first order hyperpolarizability and molecular properties found in this study may lead to the understanding of stability and reactivity of aspirin in different solvent systems.
TL;DR: It can be concluded that floating drug delivery system of quinapril HCl can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability.
Abstract: Objective: The present study was undertaken with an objective to design, develop and evaluate gastro retentive floating tablets of an antihypertensive drug, quinapril HCl, which release the drug in a sustained manner over a period of 12 h. Methods: In this research work, we used hydrophilic polymer hydroxypropyl methylcellulose (HPMC K4M), the gas generating agent sodium bicarbonate and citric acid at different ratios for the preparation of tablets. A 3 2 factorial design was applied systematically; the amount of HPMC K4M (X 1 ) and the amount of citric acid (X 2 ) were selected as independent variables. The dependent variables chosen were percentage drug release at 6 h (Q 6 ), percentage drug release at 12 h (Q 12 ) and floating lag time. The high concentration of HPMC K4M and citric acid gives a sustained release for quinapril HCl floating tablets. The tablets were prepared by direct compression technique and evaluated for tablet thickness, hardness, weight variation, friability, floating lag time and In vitro drug release. Results: The In vitro drug release indicated the floating dosage forms showed slower release when the concentration of HPMC K4M increases. Formulation F4 having ratio 25:8 (HPMC K4M: citric acid) was considered as an optimised formulation which shows satisfactory sustained drug release and remained buoyant on the surface of the medium for more than 12 h. It can also conclude that floating drug delivery system of quinapril HCl can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability. Conclusion: The developed effervescent based floating tablets are a promising floating drug delivery system for oral sustained administration of quinapril HCl.
TL;DR: To isolate and characterize novel actinomycetes and to evaluate their antibacterial activity against drug-resistant pathogenic bacteria, 19 soil samples were collected from different localities of Ad-Dawadmi, Saudi Arabia.
Abstract: Objective: To isolate and characterize novel actinomycetes and to evaluate their antibacterial activity against drug-resistant pathogenic bacteria Methods: In the present study, 19 soil samples were collected from different localities of Ad-Dawadmi, Saudi Arabia. Actinomycetes were isolated from these samples using serial dilution and plating method on Actinomycetes isolation agar supplemented with nalidixic acid and actidione to inhibit bacteria and fungi. Crude extracts of potential actinomycetes were produced by submerged fermentation. The antimicrobial activity of crude extracts of actinomycetes was tested against different bacteria using the agar well diffusion method. Characterization of the isolates was done by morphological, physiological and biochemical methods. Results: A total of 9 (47%) isolates of actinomycetes were isolated from 19 different soil samples tested. Among them, 4 (44%) isolates confirmed as Streptomyces sp. showed potential antimicrobial activity against one or more test organisms. Crude extracts were made from these 4 actinomycetes isolates(DOM1, DOM3, DP3, DP4)and tested for their antibacterial activities against 4 different clinical bacterial strains ( Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcu s) . Crude extract from DP3 isolate showed highest antibacterial activity against all the four test organisms (28 mm, 21 mm, 20 mm and 18 mm) respectively and DP4 showed lowest antibacterial activity against all the four test organisms (14 mm, 12 mm, 0 mm, 6 mm) respectively. The highest zone of inhibition was shown by DP3 against Staphylococcus aureus (28 mm) and Escherichia coli was resistant for DP4. Most of the Inhibition zones produced by crude extracts showed significant differences when compared with control, tested against test organisms (P<0.05). Inhibition zones produced by DP3 and DOM1 against Staphylococcus aureus were 28 mm and 23 mm, respectively which were strong active when compared with control Ciprofloxacin (18 mm). Conclusion: Further studies for purification of bioactive metabolites and molecular characterization analysis of isolated Streptomyces sp. are in progress which would be helpful in discovering novel compounds of commercial value.
TL;DR: The most common instability problem of gelatin capsules arises from negative impact of extremes of temperature and especially atmospheric relative humidity on the mechanical integrity of the capsule shells with adverse effect extended even to the fill material as mentioned in this paper.
Abstract: The most common instability problem of gelatin capsules arises from negative impact of extremes of temperature and especially atmospheric relative humidity on the mechanical integrity of the capsule shells with adverse effect extended even to the fill material. Moreover, choice of fill materials is highly restricted either due to their specific chemical structure, physical state or hygroscopicity. Additional reports of unpredictable disintegration and dissolution of filled hard gelatin capsules in experimental studies have prompted the search for a better alternative capsule shell material. The present review aims to provide an overview on the physicochemical, pharmaceutical and biopharmaceutical properties of hydroxypropyl methylcellulose (HPMC) as capsule shell material and perform comparative evaluation of HPMC and gelatin in terms of in vitro / in vivo performance and storage stability. HPMC capsule provides a highly flexible and widely acceptable platform capable of solving numerous challenges currently facing the pharmaceutical and nutraceutical industries and expands the possibilities for selection of different types of fill materials. The current topic introduces a new section on influence of various factors on in vitro dissolution of HPMC capsules. Delayed in vitro disintegration/dissolution of HPMC capsules in aqueous medium does not produce any negative effect in vivo . However, advancements in the processes of production and filling of HPMC capsule shells and detailed studies on effects of various parameters on their in vitro / in vivo dissolution would establish their supremacy over hard gelatin capsules in future.
TL;DR: The hydrogen atom at the position C4 was proved to have acidic and nucleophilic functionalities making the sydnone ring reactive towards electrophilic reagents, enabling sydnones to interact with biomolecules resulting in important therapeutic effects.
Abstract: Various literature sources have documented sydnones as important molecules with exclusive chemical properties and a wide spectrum of bioactivities. Sydnone can be defined as a five-membered pseudo-aromatic heterocyclic molecule. Classically, 1,2,3-oxadiazole forms the main skeleton of sydnone. The molecule has delocalized balanced positive and negative charges. The five annular atoms share the positive charge and the enolate-like exocyclic oxygen atom bears the negative charge. The hydrogen atom at the position C4 was proved to have acidic and nucleophilic functionalities making the sydnone ring reactive towards electrophilic reagents. These unique chemical features enable sydnones to interact with biomolecules resulting in important therapeutic effects like anticancer, antidiabetic, antimicrobial, antioxidant and anti-inflammatory. Consequently, we aim from the current article to review the available chemical and pharmacological information on sydnone and its derivatives.
TL;DR: In silico studies showed that xanthone derivatives could be effective as potential inhibitors against COX-2, although they are not selective.
Abstract: Objective: To demonstrate the potential ofdifferent xanthone derivatives as cyclooxygenase-2 (COX-2) inhibitor agents and their selectivity against cycloooxygenase-1 (COX-1) and COX-2 using molecular simulation. Methods: Nine novel xanthone derivatives (compounds A-I) were employed to dock against protein COX-2 (Protein Data Bank/PDB ID: 1CX2) and COX-1 (PDB ID: 3N8Z). Celecoxib, a selective COX-2 inhibitor, was chosen as a control compound. The free binding energy produced by the docking was scored using Protein-Ligand Ant System (PLANTS) and the hydrogen bonds (H-bonds) between ligands and enzymes were visualised using Pymol. Results: Molecular docking studies revealed that celecoxib docked to the active site of COX-2 enzyme, but not to COX-1; whereasxanthone derivatives docked to the active site of both COX-2 and COX-1. Free binding energy of xanthone derivatives ranged between-73,57 to-79,18 and between-73,06 to-79,25 against COX-2 and COX-1, respectively, and-78,13 against celecoxib. H-bonds in the molecule of xanthone derivatives and COX-2 protein were found in amino acid residues Arg 120 , Tyr 355 , Tyr 385 ,and Ser 353 . There was an insignificant difference between the free binding energyof xanthone derivatives against COX-2 and against COX-1, suggesting that their inhibition was non-selective. Conclusion: In conclusion, in silico studies showed that xanthone derivatives could be effective as potential inhibitors against COX-2, although they are not selective.
TL;DR: In this paper, a study was designed to screen the phytochemicals present in various solvents extracts of Ruta graveolens (Rue) and furthermore to investigate their antimicrobial activity.
Abstract: Objective: This study was designed to screen the phytochemicals present in various solvents extracts of Ruta graveolens (Rue) and furthermore to investigate their antimicrobial activity. Methods: The leaves, stems and seeds of Rue were extracted using four different solvents viz. ethanolic, methanolic, chloroform, and aqueous of varying polarity. The phytochemical screening was carried out qualitatively and Gas Chromatography-Mass Spectroscopy (GC-MS) analysis was performed to identify major phytoconstituents present in the methanolic leaf extract. The antimicrobial effect of extracts was evaluated against six microbial strains namely Bacillus subtillis, Escherichia coli, Proteus vulgaris, Candida albicans, Candida tropicalis and Micrococcus luteus with disc diffusion method. Results: Phytochemical analysis revealed the presence of various secondary metabolites such as flavonoids, alkaloids, terpenoids, saponins and carotenoid. The methanolic leaf extract showed the presence of both tannin and phenolic contents in the higher amount, whereas aqueous extract displayed in the least amount. GC-MS analysis of methanolic leaf extract revealed the presence of approximately 26 phytochemical constituents. The antimicrobial assay revealed that B. subtilis showed a high zone of inhibition (20 mm) at 200 mg/ml of methanolic extract. However, E. coli and C. tropicalis did not show any zone of inhibition against each solvent extract. Conclusion: In conclusion, secondary metabolites present in the extracts have biological activities which warrant further to evaluate in vivo pharmacological studies.
TL;DR: This review was compiled to provide consolidated information covering different aspects of the plant, to provide a basis on which to plan future studies and to promote sustainable use of Z. officinale.
Abstract: The rhizomes of Zingiber officinale Roscoe (Zingiberaceae), commonly known as ginger, is one of the most widely used spice and condiment. It is also an integral part of many traditional medicines and has been extensively used in Chinese, Ayurvedic, Tibb-Unani, Srilankan, Arabic, and African traditional medicines, since antiquity, for many unrelated human ailments including common colds, fever, sore throats, vomiting, motion sickness, gastrointestinal complications, indigestion, constipation, gastritis, epigastric discomfort, gastric ulcerations, indigestion, nausea vomiting etc. and scientific studies have validated the ethnomedicinal uses. The chemistry, phytochemical, pharmacological and molecular studies of Z. officinale is reviewed. This review was compiled to provide consolidated information covering different aspects of the plant, to provide a basis on which to plan future studies and to promote sustainable use of Z. officinale.