Showing papers in "Indian Journal of Pharmaceutical Sciences in 2018"
TL;DR: Nano-emulsions are colloidal dispersion systems that are thermodynamically stable, composed of two immiscible liquids mixed along with emulsifying agents (surfactants and co-sulfactants) to form a single phase nano-emulsion have extensively been investigated as drug delivery systems as mentioned in this paper.
Abstract: Nanoemulsions are colloidal dispersion systems that are thermodynamically stable, composed of two immiscible liquids mixed along with emulsifying agents (surfactants and co-surfactants) to form a single phase Nanoemulsions have extensively been investigated as drug delivery systems This review aims to provide consolidated information regarding various formulation and characterization techniques developed for nanoemulsions Nanoemulsions are formulated using two different methods, the persuasion method and the Brute force method Various characterization techniques for nanoemulsions include determination of entrapment efficiency, particle size, polydispersity index, zeta potential as well as characterization through differential scanning calorimetry, Fourier-transform infrared spectroscopy and transmission electron microscopy Nanoemulsions are further evaluated by studying in vitro drug release, in vitro permeation, stability and thermodynamic stability, shelf life, dispersibility, viscosity, surface tension, friccohesity, refractive index, percent transmittance, pH and osmolarity
171 citations
TL;DR: In this article, the authors synthesize and characterize citric acid crosslinked hydrogel films of carboxymethyl cellulose-tamarind gum for topical drug delivery.
Abstract: The objective of this study was to synthesize and characterize citric acid crosslinked hydrogel films of carboxymethyl cellulose-tamarind gum for topical drug delivery. The hydrogel films were characterized by attenuated total reflectance-Fourier-transform infrared spectroscopy, solid state 13C-nuclear magnetic resonance spectroscopy and differential scanning calorimeter. The prepared hydrogel films were evaluated for the carboxyl content and equilibrium swelling ratio. Moxifloxacin hydrochloride was loaded into these hydrogel films and drug release was monitored in the phosphate buffer pH 7.4. Hemolysis assay was used to study biocompatibility of hydrogel films. Results of the attenuated total reflectance-Fourier-transform infrared spectroscopy, solid state 13C-nuclear magnetic resonance and differential scanning calorimeter confirmed the formation of citric acid-crosslinked hydrogel films. Total carboxyl content of hydrogel film was found to be increased when polymer ratio and amount of citric acid was increased. In contrast, swelling of hydrogel film was found to be decreased with increase in polymer ratio and amount of citric acid. Batch B1 showed highest drug loading with non-Fickian release mechanism. All remaining batches showed non-Fickian release behavior with diffusion coefficient greater than 0.5. Results of hemolysis assay indicated that the citric acid crosslinked carboxymethyl cellulose-tamarind gum hydrogels were safe to be used in drug delivery. These results indicated that the citric acid crosslinked carboxymethyl cellulose-tamarind gum composite hydrogel films has the potential to be used in topical novel drug delivery systems.
68 citations
TL;DR: In this paper, the surface area of nanoparticles was enhanced by calcination in different atmospheric conditions and the antibacterial activity of synthesized nanoparticles were evaluated against different Gram-negative and Gram-positive bacterial strains.
Abstract: Silver is commonly used antibacterial material, and showed improved results when doped to less expensive ZnO nanoparticles. Chemical reduction method with zinc acetate as host and silver nitrate as dopant precursor was used. The surface area of particles was enhanced by calcination in different atmospheric conditions. Antibacterial activity of synthesized nanoparticles was evaluated against different Gram-negative and Gram-positive bacterial strains. Minimum inhibitory (6 to 21 mM) and minimum bactericidal concentrations (23 to 47 mM) indicated that antibacterial activity of nanoparticles was increased by silver doping and calcination in oxygen atmosphere. The X-ray diffraction, scanning electron microscopy and energy dispersive X-ray spectroscopic data further confirmed the hypothesis. Present study confirmed that oxygen treated silver doped zinc oxide nanoparticles could have pharmacological applications as alternative for antibiotics and disinfectants.
46 citations
TL;DR: The present review aims to recapitulate various emerging efforts in the biogenic synthesis of nanoparticles, most significantly their unique mechanisms of action with different approaches as well as the factors that may add up to their antimicrobial activity.
Abstract: Innovations in the nanotechnological arena have paved a path leading to nano-revolution, which has most recently unfurled the role of plants in the biogenic synthesis of nanoparticles. Though synthesis of nanoparticles can be accomplished through physical and chemical techniques, biological course of synthesis has proficiently proved competent over other techniques. The problem of evolving multidrug resistant bacteria, due to irrational use of antibiotics, makes the biogenically synthesized nanoparticles attractive, due to their promising efficacy with negligible side effects. Consequently, the nanoparticles becoming better substitutes for conventional treatment besides overcoming all the limitations. Nanoparticles have great stability and potent antibacterial activity. The uniqueness lies in their size (10 and 500 nm) and dimension offers these particles to dynamically communicate with biomolecules on the cell surfaces and within the cells, so proficiently to decode and designate various biochemical and physiochemical properties of the cells. The present review aims to recapitulate various emerging efforts in the biogenic synthesis of nanoparticles, most significantly their unique mechanisms of action with different approaches as well as the factors that may add up to their antimicrobial activity.
39 citations
TL;DR: The role of tau as an important partner of amyloid-β and tau toxicities, both of which could be used as biomarkers for diagnosis and risk assessment with other molecular chaperones which are associated with Alzheimer’s disease, are reviewed.
Abstract: The pathological emblems of Alzheimer’s disease are the accumulation of amyloid-β plaques and neurofibrillary tangles. The alluvium of toxic amyloid-β-protein in the form of aggregates is central to the pathogenesis of Alzheimer’s disease. The aggregate formation is due to the structural refitting of α-helical sheet of normal, soluble amyloid-β-protein to the β-sheets, which lead to oligomeric, fibrillar, insoluble and disease causing amyloid-β 42. Mounting data suggests that another factor, the tau protein ripens into highly phosphorylated form by several kinases after Aβ-stimulation leads to tangle formation resulting in neuronal bereavement in hippocampus and entorhinal regions as the disease progresses further. An overview has been presented in this review of the role of tau as an important partner of amyloid-β in the pathogenesis of Alzheimer’s disease, both of which could be used as biomarkers for diagnosis and risk assessment with other molecular chaperones which are associated with Alzheimer’s disease. As a part of common pathophysiological mechanism the understanding of amyloid-β and tau toxicities might be helpful for finding molecular targets for the prevention or even cure of Alzheimer’s disease.
29 citations
TL;DR: Results indicate that, gallic acid could be used as an adjuvant with immunosuppressive drugs to reduce their adverse effects on immune system.
Abstract: Gallic acid is a triphenolic acid, widely distributed in fruits, vegetables and plants and is reported to produce antioxidant, antiinflammatory, antifungal, antiviral and antitumor effects. In the present study, immunomoduatory effect of gallic acid was tested against cyclophosphamide and cisplatin; two widely used anticancer agents induced immunosuppression in Swiss albino mice. Cyclophosphamide and cisplatin are known immunosuppressive agents, which elicit variety of immune responses. In recent years much attention is given for the identification of plants or their bioactive compounds as immunomodulators. Three different doses of gallic acid i.e., 100, 200 and 400 mg/kg weight were administered orally for 7 consecutive days. Cyclophosphamide (50 mg/kg) and cisplatin (10 mg/kg) were administered intraperitoneally as single dose. Levamisole 50 mg/kg was used as standard immunomodulatory drug. 0.5 % carboxymethyl cellulose was used as solvent control. Evaluation of immunomodulatory property of gallic acid was done by using haemagglutination antibody titre response and haematological parameters such as white blood cells, red blood cells, platelet counts and haemoglobin levels. Relative weight of thymus an important lymphoid organ was also determined. Augmentation of antibody titre values and haematological end points clearly indicated immunomodulatory effect of gallic acid against cyclophosphamide and cisplatin-induced myelosuppression in Swiss albino mice. Results indicate that, gallic acid could be used as an adjuvant with immunosuppressive drugs to reduce their adverse effects on immune system.
22 citations
TL;DR: The current available non-drug therapies ranging from preclinical to clinical for controlling seizures in epileptic patients with drug resistance have been highlighted and initial results are quite promising, but considerable development is required before these treatments earn a place in the standard clinical care.
Abstract: Epilepsy is one of the most common neurological disorders, characterized by recurrent spontaneous seizures and a major health problem that affects around 1-2 % of the population worldwide. The treatment generally includes antiepileptic drug therapies. However, despite the development of various antiepileptic drugs, about a third of patients are resistant to current pharmacotherapies. Non-drug therapies are also expanding in an exciting and unprecedented way since in patients with drug resistance, non-drug therapies like surgeries; implantable devices and diet are playing a key role in improving the quality of patient’s life. In this review, the current available non-drug therapies ranging from preclinical to clinical for controlling seizures in epileptic patients with drug resistance have been highlighted. Initial results from these therapies are quite promising, but considerable development is required before these treatments earn a place in the standard clinical care.
22 citations
TL;DR: The aim of this review is to evaluate the potential application of surfactant coated nanoparticles as drug carrier system for various central nervous system diseases.
Abstract: Targeting of drugs to brain is one of the most challenging issues for pharmaceutical research as blood-brain barrier acts as an insurmountable obstacle for the passage of systemically delivered therapeutics and the brain extracellular matrix attributes to poor distribution of locally delivered drugs. Amongst various invasive or non-invasive methods to warrant blood-brain barrier, nanoparticle is one of promising ways to administer central nervous system drugs. The concept of nanoparticle-based drug targeting make a tremendous progress and gigantic era to overcome the above limitations with improved drug efficacy and reduced drug toxicity. In recent years, new strategies of surfactant coating of biodegradable polymeric nanoparticles, which differ from conventional methodologies of brain targeting, have emerged at the forefront of medical science. The non-ionic surfactant, polysorbate 80 as a coating material promises an unparalleled opportunity for enhancement of brain targeting of colloidal particles. The aim of this review is to evaluate the potential application of surfactant coated nanoparticles as drug carrier system for various central nervous system diseases.
22 citations
TL;DR: A New series of 1,2,4-triazole derivatives were synthesized using appropriate synthetic route and structures were confirmed by infrared spectroscopy, proton nuclear magnetic resonance, carbon-13 nuclear Magnetic resonance, mass spectroscopic and elemental analysis, which showed significant antitubercular potential against Mycobacterium tuberculosis and clinical isolates.
Abstract: A New series of 1,2,4-triazole derivatives were synthesized using appropriate synthetic route and structures were confirmed by infrared spectroscopy, proton nuclear magnetic resonance, carbon-13 nuclear magnetic resonance, mass spectroscopy and elemental analysis. Antimycobacterial activity of the synthesized compounds (1-12) was carried out and percent reduction in relative light units was calculated using luciferase reporter phage assay. Percent reduction in relative light units for isoniazid was also calculated. The test compounds showed significant antitubercular potential against Mycobacterium tuberculosis H37Rv and clinical isolates, S, H, R and E resistant M. tuberculosis, when tested in vitro. Compound 8 and 12 showed better antitubercular activity compared to reference isoniazid against M. tuberculosis H37Rv strain while compounds 5, 8 and 12 found superior to isoniazid against clinical isolates: S, H, R and E resistant M. tuberculosis. Synthesized compounds were also tested in vitro against representative bacterial and fungal strains. Tested compounds showed better antibacterial activities (minimum inhibitory concentration) against Gram-positive bacteria compared to Gram-negative. Compound 5 showed better antibacterial activity than ampicillin against B. subtilis. Compound 12 in the series displayed most potent antifungal activity, which was comparable to reference fluconazole against both the fungal strains.
21 citations
TL;DR: The antibacterial activity of Suaeda maritima against a wide spectrum of Gram-negative and Gram-positive isolates and multiple antibiotic resistant strains suggested that it may be a potential antibacterial agent to control antibiotic resistant infections.
Abstract: In this study, antimicrobial property of Suaeda maritima, a mangrove associate species collected from lower Gangetic delta complex was evaluated. The antibacterial activity of the extract against a wide spectrum of Gram-negative and Gram-positive isolates and multiple antibiotic resistant strains suggested that it may be a potential antibacterial agent to control antibiotic resistant infections. Among the different solvent fractions examined, n-hexane extract of the shoot of S. maritima L (Dumort) was found to possess highest antibacterial activity against four Gram-positive (Bacillus subtilis, Staphylococcus haemolyticus, Staphylococcus aureus, Enterococcus faecalis) and six Gram-negative (Escherichia coli, Citrobacter sp., Klebsiella pneumoniae, KPC producing K. Pneumonia, Pseudomonas sp. and Stenotrophomonas maltophila) bacteria. Fungicidal activity was noted against Saccharomyces cerevisiae. Minimum inhibitory concentration and minimum bactericidal concentration values were determined in disc diffusion and macrodilution assays. The inhibition zones ranged between 13-20 mm. GC-MS analysis of the n-hexane fraction showed the presence of various fatty acid esters and essential oils. In addition, scytalone known for its antioxidant property, campesterol and ethanone were detected. Antioxidant activity was found having an IC50 value of 52.53 mg/ml.
20 citations
TL;DR: In this paper, different extracts of Acacia nilotica leaves were tested for total phenolic and flavonoid content, antioxidant activities, and positive correlation was observed between the total phenolics content, total flavonoids content and antioxidant activities.
Abstract: In the present study different extracts of Acacia nilotica leaves were tested for total phenolic and flavonoid content, antioxidant activities. Extracts were also subjected to phytochemical analysis using GC-MS analytical techniques. Antioxidant potential was determined using DPPH free radical scavenging assay, hydrogen peroxide scavenging assay, metal chelating assay and β-carotene-linoleic acid assay. Methanol extract exhibited maximum antioxidant activity (94.3 %) followed by the ethyl acetate extract (90.7 %). Total phenolic content was highest in the methanol extract and total flavonoid content in ethyl acetate extract. Positive correlation was observed between the total phenolic content, total flavonoid content and antioxidant activities. Principle component analysis revealed correlation between different parameters. D-pinitol, catechol, N-2,4-dnp-L-arginine, squalene, R-limonene, 9-octadecen-12-ynoic acid, methyl ester, androst-5-en, 2(1-H)-quinolinone, heptacosane, 2-pentadecanone, 6,10,14-trimethyl, linoleic acid, γ-linoleic acid, palmitic acid, stearic acid were the main compounds present in different extracts of Acacia nilotica leaves and could serve as a possible source of natural antioxidants in food and pharmaceutical industry.
TL;DR: The review clearly demonstrates the importance of this plant in ethnomedicine and its immense potential in modern medicine.
Abstract: Myrica esculenta (Myricaceae) commonly known as box berry or kaphal is an important Indian medicinal plant. It is found in foothill tracks of Eastern Himalayas, Meghalaya, Nepal, China and Pakistan. Local tribes mainly use its fruits to prepare pickle and refreshing drinks. Traditionally, the bark has been used for the treatment of cough, asthma, fever, chronic bronchitis, diarrhoea, rheumatism and inflammation; roots have been used in bronchitis, asthma, cholera and flowers claimed to treat earache, diarrhoea, paralysis. Phytochemical studies of the different parts of plant revealed the presence of various bioactive phytoconstituents such as phenolic compounds, alkaloids, glycosides, triterpenoids and volatile oils. The plant is also reported to have innumerable significant pharmacological activities like analgesic, anxiolytic, antiallergic, antidiabetic, antimicrobial, antihypertensive, antiulcer, antioxidant and antiinflammatory evaluated by using various animal models. The objective of the present review article is to compile all the relevant published information regarding traditional uses, phytochemistry and therapeutic potential of M. esculenta. For this purpose various databases and books were examined. The review clearly demonstrates the importance of this plant in ethnomedicine and its immense potential in modern medicine.
TL;DR: A series of metal (II) complexes, [CuL(AcO), H2O (1), [CoL (AcO], 4H2O(2), [MnL( AcO), [NiL(ACO), 4H 2O (3), [ZnL[AcO] and [2H2E(5)] have been synthesized from 2-(2-morpholinoethylimino)methyl)phenol Schiff base ligand in a 1:1 molar ratio as mentioned in this paper.
Abstract: A novel series of metal (II) complexes, [CuL(AcO)].H2O (1), [CoL(AcO)].4H2O (2), [MnL(AcO)].4H2O (3), [NiL(AcO)].4H2O (4) and [ZnL(AcO)].2H2O (5) have been synthesized from 2-(2-morpholinoethylimino)methyl)phenol Schiff base ligand in a 1:1 molar ratio. The resulting compounds were characterized using various physical, chemical and spectral studies. The spectral results indicated square planar geometry around the metal (II) ion and found to possess [ML] stoichiometry. Complexes (1), (2) and (4) exhibited potent antimicrobial, antioxidant and DNA cleavage activities as compared to complexes (3) and (5). In vitro DNA binding properties of complexes (1-5) have been carried out employing the electronic absorption technique. The calculated intrinsic binding constant (Kb) values for the complexes were in the order of 1.3512×105 (1) >2.9843×104 (2) >1.6432×104 (4) >4.2280×103 (5) >2.9100×103 M−1 (3) and the DNA binding affinity values of the complexes obtained by the viscosity titration measurements were in the order of (1)>(2)>(4)>(5)>(3). The observed results suggested that the complexes (1-5) bind to DNA via intercalation.
TL;DR: This review indicated that Nigella sativa and thymoquinone exhibited beneficial cardiovascular effects on cardiotoxicity, hypertension, hyperlipidemia, and atherosclerosis, probably due to the antioxidant and antiinflammatory properties of Nigella sitiva.
Abstract: Various pharmacological effects of Nigella sativa L. have been reported that include, antioxidant, antibacterial, antihistaminic, antihypertensive, hypoglycemic, antifungal, antiinflammatory, anticancer, and immunomodulatory. It has also been reported to produce beneficial effects in cardiovascular, gastrointestinal, reproductive and respiratory disorders. The effects of Nigella sativa had been attributed to constituents such as nigellicine, nigellidine, thymoquinone, dithymoquinone, thymol and carvacrol. In this article the cardiovascular effects of Nigella sativa and its constituents were reviewed. Published data was gathered through search engines and the findings were classified into animal and human studies. The effects of Nigella sativa and its constituents on cardiotoxicity, blood pressure, vascular smooth muscle, endothelial dysfunction, heart rate, cardiac contractility, lipid profile, platelet aggregation and atherosclerosis were reviewed. This review indicated that Nigella sativa and thymoquinone exhibited beneficial cardiovascular effects on cardiotoxicity, hypertension, hyperlipidemia, and atherosclerosis. These effects were probably due to the antioxidant and antiinflammatory properties of Nigella sativa. It seems that Nigella sativa and its constituents could be of therapeutic value in cardiovascular diseases
TL;DR: It’s concluded that synthesized metal complexes showed better antioxidant, antibacterial and antifungal potential as compared to diphenyldithiocarbamate as well as the standard and might turn out to be a valuable treatment of numerous kinds of diseases.
Abstract: Ni(II), Cu(II) and Zn(II) complexes of diphenyldithiocarbamate have been synthesized with the aim of developing antioxidants, potential antibacterial and antifungal agents. Synthesized metal complexes were characterized by magnetic susceptibility, elemental analysis; conductivity measurements, mass spectra, infrared, ultra violet/visible and nuclear magnetic resonance verified the chemical composition of products. Magnetic susceptibility and spectroscopic studies suggested the predicted geometry of the diphenyldithiocarbamate complexes as octahedral geometry of Ni(II) complex distortion square-planer geometry distorted towards tetrahedral for Cu(II) and Zn(II) complexes. Synthesized metal complexes exhibited remarkable antioxidant potential as compared to standard. Zn(II) complex of diphenyldithiocarbamate exhibited IC50 of 31.45±0.31 μM while the standard, butylated hydroxytoluene exhibited IC50 of 44.67±0.45 μM antioxidant activity. Synthesized metal complexes showed very good antibacterial and antifungal potential against Rhodococcuss, Actinomyces viscosus, Bacillus subtilis, Escherichia coli and the fungi, Aspergillus niger, Aspergillus flavus, Candida and Acetomyceta. It’s concluded that synthesized metal complexes showed better antioxidant, antibacterial and antifungal potential as compared to diphenyldithiocarbamate as well as the standard and might turn out to be a valuable treatment of numerous kinds of diseases.
TL;DR: Interactions of acephate, glyphosate, monocrotophos and phorate with bovine serum albumin were explored employing the UV/Vis and Fourier-transform infrared spectroscopy methods and results have shown that out of four pesticides, phorate could show strong interactions with bivine serumalbumin.
Abstract: Binding of pesticides to serum albumin significantly influence their absorption, metabolism, distribution and excretion. In the present study, interactions of acephate, glyphosate, monocrotophos and phorate with bovine serum albumin were explored employing the UV/Vis and Fourier-transform infrared spectroscopy methods. The observed values of binding constant for titled pesticides were. phorate (1.85×107 M-1)>acephate (3.93×104 M-1)>glyphosate (1.31×104 M-1)>monocrotophos (1.12×104 M-1). Results have shown that out of four pesticides, phorate could show strong interactions with bovine serum albumin.
TL;DR: In this paper, pyrazole-containing dihydropyrimidinone motifs (4a-o) and their antimicrobial activity and cytotoxicity were reported.
Abstract: In the present communication synthesis of pyrazole-containing dihydropyrimidinone motifs (4a-o) and their antimicrobial activity and cytotoxicity were reported. The newly synthesized compounds were characterized using infrared, proton nuclear magnetic resonance, carbon-13 nuclear magnetic resonance and mass spectral techniques. Compounds 4b, 4c, 4f, 4g, 4i and 4j were the most active derivatives identified during antimicrobial activity screening. On the basis of antibacterial activities, it was observed that compounds 4b and 4c exhibited activity against methicillin resistant Staphylococcus aureus with minimum inhibitory concentrations of 12.5 and 6.25 µg/ml, respectively. From structure activity relationship studies, it could be concluded that electron withdrawing groups played a crucial role in enhancing antimicrobial and cytotoxic effects of title compounds. In addition, the results of the cytotoxicity studies indicated that compounds 4b, 4c, 4g and 4j possessed lower levels of cytotoxicity.
TL;DR: The pharmacokinetic studies demonstrated that efavirenz-loaded liposomes could significantly upgrade the solubility and oral bioavailability of efvirenz and improve the therapeutic efficacy.
Abstract: To overcome the limited solubility and low bioavailability of efavirenz a liposomal drug delivery system was formulated using thin film hydration technique. Optimal ratios of total lipid blend:drug, soya lecithin:cholesterol and polyethylene glycol 400 concentration were determined using Box Behnken design with vesicle size and entrapment efficiency as responses. The optimized liposomal dispersions were characterized by vesicle size, entrapment efficiency, transmission electron microscopy, in vitro drug release and in vivo pharmacokinetics. The vesicle size was found to be in range of 694.5-1200.0 nm and entrapment efficiency was above 80 %. Statistical studies revealed that vesicle size and entrapment efficiency increased with increase in total lipid blend:drug and polyethylene glycol 400 concentration. Transmission electron microscopy showed that unilamellar and multi-lamellar vesicles were formed. Optimized liposomal dispersion was solidified using nanosponges. Solid liposomes were characterized by micromeritics, differential scanning calorimetry, Fourier-transform infrared spectroscopy and bioavailability. As compared to plain drug a 10-fold increase in percent release was observed in 6 h in liposomal preparation. In vivo pharmacokinetic studies revealed that bioavailability increases 2 folds as compared to plain drug. Lipid-based drug delivery like liposomes are taken up through lymphatic pathway. Since the human immunodeficiency virus settles in lymphoid organs, lymphatic drug delivery can be advantageous in the treatment of acquired immune deficiency syndrome. Thus, the pharmacokinetic studies demonstrated that efavirenz-loaded liposomes could significantly upgrade the solubility and oral bioavailability of efavirenz and improve the therapeutic efficacy.
TL;DR: A series of oxazine substituted 9-anilinoacridines were synthesized, characterized, and evaluated for antitumor activity against Daltons lymphoma ascites cells using in vitro and in vivo methods and indicated that these conjugates exhibited significant antitumour activity.
Abstract: A series of oxazine substituted 9-anilinoacridines were synthesized, characterized, and evaluated for antitumor activity against Daltons lymphoma ascites cells using in vitro and in vivo methods. Results indicated that these conjugates exhibited significant antitumour activity on Daltons lymphoma ascites cells. Among these agents, compounds 4b, 4c, 4e and 4j were the most cytotoxic with CTC50 value of 96.5-190 µg/ml (0.125-0.352 µM). 3D QSAR study was performed using PHASE module of Schrodinger suite.
TL;DR: Improved therapeutic response was obtained as compared to nanoemulsion gel, nanomicellar gel, emulgel and also marketed topical product of Boswellia when examined for in vivo antiinflammatory and analgesic activity in animal models.
Abstract: Boswellia serrata was formulated as topical analgesic and antiinflammatory nanoemmigel, which is a combination of a nanoemulsion and a nanomicellar system in a gel base. Nanoemulsion was formulated by microemulsion-template method by using probe sonication at 5 amp for 5 min. Particle size of nanoemulsion was found to be 141 nm and polydispersity index of 0.333. Nanomicelle was formulated at a ratio 1:1 of drug and surfactant and 1:10 of solvent and antisolvent using solvent evaporation method. The particle size and polydispersity index of the nanomicelle was found to be 31.07 nm and 0.205, respectively. Nanoemmigel was prepared by combining nanoemulsion and nanomicelle in the ratio 1:1 with carbopol 974 as a gelling agent. The nanoemmigel prepared was a buff coloured, opaque gel with smooth texture and good spreadability. Viscosity and drug content of the nanoemmigel was 50720 cps and 103±1.08 %, respectively. In vitro diffusion study of nanoemmigel showed 98.52±1.53 % drug permeation at the end of 5 h. The drug release mechanism of the nanoemmigel formulation can be explained using the Higuchi model. The steady state flux and permeability co-efficient of the nanoemmigel was found to be better than each of nanoemulsion gel and nanomicellar gel due to the utilization of both the pathways available to the drug for permeation through the skin. Improved therapeutic response was obtained as compared to nanoemulsion gel, nanomicellar gel, emulgel and also marketed topical product of Boswellia when examined for in vivo antiinflammatory and analgesic activity in animal models.
TL;DR: It was found that electron-withdrawing group at phenyl ring, attached to the coumarin nucleus was crucial for activity against human immunodeficiency virus.
Abstract: A series of 6-acetyl-coumarin derivatives (2a-n) were synthesized and evaluated for antiretroviral activity in C8166 T-cell line infected with HxBru-Gluc strain of human immunodeficiency virus-1 Michael Addition followed by re-aromatization and subsequent acid-induced elimination of water leads to the formation of coumarin intermediate, which undergoes Claisen-Schmidt condensation with substituted bezaldehydes using silica sulphuric acid as a catalyst to form 6-acetyl-coumarin derivatives, 2a-n In silico absorption, distribution, metabolism, excretion and toxicity parameters of compounds 2a-n were found within their reference limits All synthesized compounds were devoid of cytotoxicity as they have shown cell viability count more than 80 % in cytotoxicity assay Compounds 2a, 2g and 2h showed potent inhibitory activity against human immunodeficiency virus infection with IC50 value of 47, 45 and 035 μM, respectively It was found that electron-withdrawing group at phenyl ring, attached to the coumarin nucleus was crucial for activity against human immunodeficiency virus The present study may be helpful in the development of some potent antiretroviral agents
TL;DR: In this article, the preparation and evaluation of fenofibrate-loaded nanoparticles by precipitation method to enhance solubility and bioavailability was the primary aim of the study.
Abstract: Nanoparticles have applications in the formulation of poorly water soluble drugs to improve their bioavailability. Preparation and evaluation fenofibrate-loaded nanoparticles by precipitation method to enhance solubility and bioavailability was the primary aim of the present investigation. Nano particles of fenofibrate, a BCS class II drug, were prepared by precipitation technique and characterized using Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, zeta potential and drug release studies in vitro. Data from the differential scanning calorimetry, powder X-ray diffractometry and Fourier transform infra-red spectroscopy showed no interaction between drug and the polymers. Scanning electron microscopy images indicated that nanoparticles were spherical in shape. Water solubility of drug-loaded nanoparticles was increased as compared to the pure drug and showed improved dissolution profile, which indicated that nanoprecipitation was simple and precise. This laboratory scale method as well as this approach could be employed for solubility and bioavailability improvement of BCS class II drugs.
TL;DR: In this paper, the authors evaluated some antifertility herbs Bambusa arundinacea (leaf), Bauhinia racemosa Lam and Ficus rancosa (bark) qualitatively and quantitatively in terms of their phytoconstituents.
Abstract: Antifertility herbs are used to prevent conception or fertilization This study is aimed to evaluate some antifertility herbs Bambusa arundinacea (leaf), Bauhinia racemosa Lam and Ficus racemosa (bark) qualitatively and quantitatively in term of their phytoconstituents The total phenolic content was determined by Folin-Ciocalteu reagent using gallic acid as a standard, total flavonoid content by aluminum chloride assay using quercetin as a standard, total tannin content by Folin-Denis' reagent and alkaloid content was determined as equivalents to atropine Saponin content was determined in crude powder of drugs The extracts were screened for presence of various phytoconstituents using preliminary chemical tests and TLC was performed for qualitative analysis Among the four extracts, ethanol extract of B arundinacea leaves showed maximum amount of phenolic content (224±034mg/g) and flavonoid content (465±074 mg/g) as compared to F racemosa and B racemosa bark extracts whereas total tannin content was found maximum in F racemosa bark (896±154 mg/g) Preliminary phytochemical screening revealed the presence of alkaloids, glycosides, flavonoids, carbohydrates, tannins, phenols and saponins Thin layer chromatographic studies of various extracts constituted different colored phytochemical compounds with different Rf values This study gave an insight to the Aerva, the phytoconstituents present in the plant and useful for quantification of the compound in herbal formulation
TL;DR: It could be concluded that the developed polyphenon 60+ciprofloxacin nanoemulsion showed antibacterial activity against Escherichia coli and was transported efficiently to the target organs through vaginal mucosa.
Abstract: The aim of the present study was to develop a nanoemulsion-based delivery system containing green tea catechins called polyphenon 60 and ciprofloxacin for intravaginal delivery to treat urinary tract infection. Polyphenon 60 and ciprofloxacin were encapsulated in a single nanoemulsion system prepared using ultrasonication technique. The nanoemulsion was characterized by determining particle size, zeta potential, morphological structure and estimating in vitro release and antibacterial efficacy. To determine the in vivo pharmacokinetic parameters and intravaginal transportation of nanoemulsion in Sprague Dawley rats, gamma scintigraphy and biodistribution study was conducted with technetium pertechnetate-labelled nanoemulsion. The preliminary antibacterial investigation showed synergy between these compounds with FICindex of 0.42. The developed formulation showed zeta potential of +55.3 mV and globule size of 151.7 nm, with polydispersity index of 0.196. The percent in vitro release for polyphenon 60 at the end of 7 h was 94.8±0.9, whereas for ciprofloxacin it was 75.1±0.15 in simulated vaginal media. Antibacterial activity evaluation against extended spectrum beta lactamase and metallo beta lactamase strains revealed that nanoemulsions containing 4 and 10 mg/ml each of polyphenon 60 and ciprofloxacin effectively inhibited the growth of bacterial strains. In biodistribution study, the percent radiolabelled drug per gram was found to be 3.50±0.26 and 3.81±0.30 in kidney and urinary bladder, respectively at 3 h. From these findings it could be concluded that the developed polyphenon 60+ciprofloxacin nanoemulsion showed antibacterial activity against Escherichia coli and was transported efficiently to the target organs through vaginal mucosa.
TL;DR: It showed that patient education added with a well-designed patient information leaflet has a greater impact on knowledge of the patients towards their disease management, so that the medication adherence is improved.
Abstract: A patient information leaflet is an educational material for educating patients regarding a disease, medications and lifestyle modifications for better care. The present study aimed at preparing, validating and user-testing of diabetes and hypertension information leaflets in different languages among patients. The patient information leaflets on diabetes and hypertension were prepared by referring to the primary, secondary and tertiary resources. The content of the leaflet was validated by an expert committee. The readability of leaflets has been assessed by Flesch Reading Ease and Flesch-Kincaid Grade Level scores using MS Office 2007. The patient information leaflets were translated into Kannada and Malayalam languages with the help of language experts. During the user-testing, baseline knowledge was assessed before providing the patient information leaflet followed by provision of leaflets to the patients. After allowing the patients to read the leaflet for a period of 20 min, patients have again been administered with a set of questions to assess their knowledge. The Flesch Reading Ease and Flesch-Kincaid Grade Level readability scores achieved for diabetes leaflets are 70.4 and Flesch-Kincaid Grade Level score achieved is 6.3 and for hypertension leaflets, the Flesch Reading Ease score is 68.3 and Flesch-Kincaid Grade Level score achieved is 6.9. User testing of the patient information leaflets on diabetes and hypertension in different languages have been carried out on 40 each diabetic and hypertensive patients using knowledge based questionnaire. Knowledge assessment after providing patient information leaflet, the mean scores have significantly risen from 44.80 to 87.99 and 63.19 to 90.13 with p<0.0001, respectively in diabetes and hypertensive patients. It showed that patient education added with a well-designed patient information leaflet has a greater impact on knowledge of the patients towards their disease management, so that the medication adherence is improved.
TL;DR: Saponins from Quillaja saponaria and Camellia oleifera improved the aqueous solubility of danazol and fenofibrate by more than two orders of magnitude.
Abstract: Poor aqueous solubility limits the bioavailability of hydrophobic drugs. Thus, there is an increasing interest in new micelle-forming, drug-solubilizing molecules that can offer improved effectiveness and safety. The effect of 13 saponin extracts on the solubility of fenofibrate and danazol was studied and the relationship between saponin molecular structure and drug solubilisation capacity was assessed. Drug solubility was measured by high-performance liquid chromatography and saponin solubilisation capacity was compared to the conventional surfactant Brij-35. Saponins from Quillaja saponaria and Camellia oleifera improved the aqueous solubility of danazol and fenofibrate by more than two orders of magnitude. For danazol, the solubilisation capacity of the best saponins was 2-3 times higher than Brij-35, whereas for fenofibrate it was slightly lower than the reference surfactant. Both drugs were solubilized very effectively by bidesmosidic oleanane saponins, whereas dammarane, mono- and tri-desmosidic oleanane saponins and steroid (furostanol and spirostanol) saponins had no effect on drug solubility. Exceptions were fenusterol, a furostanol saponin and escin, a monodesmosidic oleanane saponin, which solubilized danazol only.
TL;DR: In this article, the authors developed and evaluated sustained delivery of terbinafine hydrochloride from topical polymeric microsponges using a quasi emulsion solvent diffusion method.
Abstract: The objective of the present study was to develop and evaluate sustained delivery of terbinafine hydrochloride from topical polymeric microsponges. Microsponges of ethyl cellulose containing terbinafine hydrochloride were prepared by quasi emulsion solvent diffusion method. Effect of drug polymer ratio on active drug content, particle size and entrapment efficiency were studied. Drug polymer ratio greatly affects properties (entrapment efficiency, active drug content, particle size) of microsponges. Terbinafine hydrochloride microsponges showed highest actual drug content, entrapment efficiency and smaller particle size, so 1.5:1 ratio of drug and polymer was selected for optimization study. Optimization study was carried out by taking internal phase volume, stirring rate, emulsifier concentration as independent variables and their effects on entrapment efficiency, particle size were studied. It was found that as stirring speed increases, the particle size decreases and entrapment efficiency increases, while as volume of dichloromethane increases, particle size decreases. Morphology of obtained microsponges was revealed by scanning electron microscope and was found to be porous and spherical. Optimized formulation of microsponge was dispersed in Carbopol gel and evaluated for drug content, pH, viscosity and in vitro drug release. Release of drug was found to be sustained through microsponge gel as compared to marketed product and pure drug gel. Ex vivo drug deposition study was carried using rat abdominal skin. Drug deposition was found to be satisfactory. Prepared polymeric microsponges could be a potential topical drug delivery system in antifungal therapy.
TL;DR: It is concluded that essential oil of T. ammi and its fractions have strong antidermatophytic properties with no side effect at low concentrations and thus could produce alternative therapeutics to current antibiotics.
Abstract: Present study was designed to explore the essential oil of Trachyspermum ammi and its fractions against fungi causing dermatophytoses in humans along with toxicological evaluation on mice The chemical composition of T ammi essential oil analyzed by gas chromatography and gas chromatography-mass spectrometry presented 20 compounds Thymol was found to be the major compound (5888 %) followed by p-cymene (2402 %), γ-terpinene (1377 %) and β-pinene (190 %) Antidermatophytic activity was determined by disc diffusion method and minimum inhibitory concentration Maximum zone of inhibition was observed against Chrysosporium tropicum (6383±0166 mm) followed by Trichophyton simii (57±0288 mm), Trichophyton rubrum (5133±0333 mm) and Chrysosporium indicum (45±0577 mm) Minimum inhibitory concentration of T ammi oil ranged from 0025 to 05 μl/ml against test fungi T ammi oil was further subjected for fraction separation through Buchii's glass oven equipment Five fractions were separated at different temperature conditions labeled as TAI-TAV Maximum effects were seen in case of TAIV and TAV fractions Excellent results of TAV was observed against Microsporum gypseum (0015±0002 μl/ml) followed by Microsporum canis (0017±0002 μl/ml), Trichophyton rubrum (002±0000 μl/ml) and Candida albicans (005±0003 μl/ml) No work on T ammi essential oil fractions, their antidermatophytic activity and toxicological behavior on Swiss Albino mice were reported till date Acute dermal irritation assay was applied for toxicological studies on Albino mice Low concentration up to 3 % did not show any irritation on mice skin At 5 % concentration 3 mice showed mild erythema, while on 7 % concentration all five mice exhibited well defined erythema Present study concluded that essential oil of T ammi and its fractions have strong antidermatophytic properties with no side effect at low concentrations and thus could produce alternative therapeutics to current antibiotics
TL;DR: In this paper, the phytochemical components and antioxidant capacity of extracts obtained from Iris taochia plant, which is endemic to Caucasus, were investigated and 15 new compounds were detected and identified using a GC-MS Sytem.
Abstract: In this study, phytochemical components and antioxidant capacity of extracts obtained from Iris taochia plant, which is endemic to Caucasus, were investigated. Fifteen new compounds were detected and identified using a GC-MS Sytem, which were isolated from Iris taochia for the first time. From the calibration curve, the amount of α-amyrin in dry powder of Iris taochia was calculated. The mean amount of α-amyrin found in whole plant powder of Iris taochia was 4.598 μg/10 mg with a percent recovery of 0.045 % for α-amyrin. Antioxidant properties of Iris taochia, in vitro using Fe3+-Fe2+, Cu2+-Cu+ and Fe3+-2,4,6-tripyridyl-s-triazine reducing, 1,1-diphenyl-2-picrylhydrazyl scavenging, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) scavenging, N,N-dimethyl-p-phenylenediamine scavenging and Fe2+ chelating activities were measured. The antioxidative effects of Iris taochia have not been reported earlier. These results shown that crude ethanol and water extracts of Iris taochia had effective reducing effect, radical scavenging activity and metal chelating effects when compared to standard antioxidants. The results indicated that the ethanol and water extracts of Iris taochia could be used as a potential source of natural antioxidants by the pharmaceutical industry or as a conceivable food supplement.
TL;DR: Development of flexible formulations as an alternative to marketed different formulations of the same drug would reduce the cost of the formulation for patients particularly developing countries where accessibility to various types of formulations is less.
Abstract: The oral route of drug administration is mostly preferred by paediatric and geriatric patients. Patient non-compliance due to poor taste and swallowing problems are major issues in paediatric and geriatric drug therapy. Lack of age-appropriate formulations, inadequate labelling instructions, non-compatible and non-palatable medicines are the main reasons for medication errors in paediatric patients. This review mainly highlights major issues of paediatric and geriatric drug therapy and provides the design of oral flexible formulations as an alternative formulation design for age appropriate formulation development. Development of solid oral flexible formulations as an alternative to existing marketed formulations such as conventional tablets, orally disintegrating tablets, chewable and dispersible tablets for paediatric and geriatrics patients is described. Details about drug properties, excipient selection and taste masking approaches were described. The need for bioavailability and bioequivalence studies for flexible formulations also described. Development of flexible formulations as an alternative to marketed different formulations of the same drug would reduce the cost of the formulation for patients particularly developing countries where accessibility to various types of formulations is less. Flexible tablet formulations can be conveniently used by the patients as orally swallowable, orally disintegrating, chewable and as dispersible tablets. Sprinkle formulations such as pellets, granules packed in capsules or sachets can be conveniently used by paediatric and geriatric patients. Properly designed and developed flexible formulations for new chemical entities and off-patent drugs are need of the hour to provide better treatment to varying age groups of paediatrics and geriatrics.