Showing papers in "Tropical Journal of Pharmaceutical Research in 2013"
TL;DR: The ability of employing zeta potential to target drug delivery systems to, and drug release at specific sites of the body are discussed.
Abstract: The zeta potential (ZP) of colloidal systems and nano-medicines, as well as their particle size exert a major effect on the various properties of nano-drug delivery systems. Not only the stability of dosage forms and their release rate are affected but also their circulation in the blood stream and absorption into body membranes are dramatically altered by ZP. In this paper the effect of ZP on the various properties of nano-medicines are reviewed. Furthermore, the ability of employing zeta potential to target drug delivery systems to, and drug release at specific sites of the body are discussed.
1,276 citations
TL;DR: In this paper, a green process for the extracellular production of silver nanoparticles synthesized and stabilized using Penicillium citrinum isolated from soil was evaluated. And the results indicated that the current approach suggests that rapid synthesis of nanoparticles of silver nitrate would be suitable for developing a biological process for mass scale production of formulations.
Abstract: Purpose: To evaluate a green process for the extracellular production of silver (Ag) nanoparticles synthesized and stabilized using Penicillium citrinum isolated from soil. Methods: The pure colonies of Penicillium citrinum were cultured in Czapek dox broth. The supernatant of the broth was examined for the ability to produce silver nanoparticles. The reactions were performed in a dark compartment at 28 oC. After 24 h, the synthesized silver nanoparticles were filtered through a membrane filter (0.45 µ) and characterized by UV-visible spectroscopy, fluorescence spectroscopy, photon correlation spectroscopy (PCS), scanning electron microscopy (SEM) and Fourier transformed infrared spectroscopy (FTIR) for particle size, shape and the presence of different functional groups in the nanoparticles. Results: The silver nanoparticles formed were fairly uniform in size with a spherical shape and a Zaverage diameter of 109 nm. FTIR spectra revealed the presence of amide linkage groups which were also found in the fungal extract itself. Conclusion: The current approach suggests that rapid synthesis of nanoparticles of silver nitrate would be suitable for developing a biological process for mass scale production of formulations.
136 citations
TL;DR: In this article, the antioxidant and antimicrobial activities of polyphenolic extracts of three wild red wild berry fruit species from Southeast Serbia, viz, European cornel (Cornus mas), blackthorn (Prunus spinosa L.) and wild blackberry (Rubus fruticosus).
Abstract: Purpose: To assess the antioxidant and antimicrobial activities of polyphenolic extracts of three wild red wild berry fruit species from Southeast Serbia, viz, European cornel (Cornus mas), blackthorn (Prunus spinosa L.) and wild blackberry (Rubus fruticosus). Methods: Polyphenol content was determined using spectrophotometric and High performance liquid chromatography (HPLC) methods. Antioxidant activity was estimated by 2,2`- diphenyl - 1 - picrylhydrazyl (DPPH) test while reliminary antimicrobial tests were carried out by disc diffusion method in which antibacterial activity was evaluated by measuring the zone of inhibition against test bacterial strains. Broth microdilution method was used to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). Results: The highest amount of total phenols was found in European cornel (8625.89 mg kg -1 FW). Galic acid, caffeic acid, p-coumaric acid, ferulic acid, (+)-catechin, procyanidin B2, (-)-epicatechin, quercetin, rutin and quercetin-3-glucoside were the main polyphenols in the fruit extracts. All extracts showed high scavenging effect on DPPH radical with IC 50 values ranging from 22.19 to 31.18 ml g -1 , as well as high antimicrobial activity on almost all the tested bacterial strains. Conclusion: Extracts of wild berry fruits may be suitable for the preparation of medicinal and nutritional products. Keywords: European cornel, Blackthorn, Wild blackberry, Polyphenols, Antioxidant, Antimicrobial
74 citations
TL;DR: In this paper, the composition of essential oils of two types of mint as well as compare the antimicrobial, antioxidant and anti-inflammatory activities of the two oils were analyzed by steam distillation in a Clevenger-type apparatus.
Abstract: Purpose: To analyze the composition of essential oils of two types of mint as well as compare the antimicrobial, antioxidant and anti-inflammatory activities of the two oils. Methods: Peppermint (M. piperita L.) and chocolate mint (M. piperita L.) oils were obtained by steam distillation in a Clevenger-type apparatus. The chemical composition of the essential oils was determined by gas chromatography-mass spectrometry (GC/MS). The minimal inhibitory concentration (MIC) of the essential oils were determined by broth dilution method. The antioxidant activities of the oils were determined by 2, 2-diphenyl-1-picrylhydrazyl (DPPH)DPPH radical scavenging assay, β-Carotene-linoleic acid assay, andnitric oxide (NO) radical scavenging assay. Results: The two essential oils contain high levels of alcohol (43.47-50.10%) and terpene (18.55-21.07%) with the major compound being menthol (28.19-30.35%). The antimicrobial activity (minimum inhibitory concentration, MIC) of peppermint oil against E. coli, S. aureus and P. aeruginosa (0.15, 0.08, 0.92 %v/v, respectively) was stronger than that of chocolate mint (0.23, 0.09, 1.22 %v/v, respectively). In the anti-oxidant test including DPPH and β-Carotenelinoleic acid assays, peppermint oil showed superior antioxidant properties to chocolate mint oil (4.45 - 19.86 μl/mL). However, with regard to scavenging NO radical activity, chocolate mint oil exhibited higher activity than peppermint (0.31 and 0.42 μl/mL, respectively). Chocolate mint oil also exhibited higher anti-inflammatory activity than peppermint oil (0.03 and 0.08 μl/mL, respectively). Conclusion: The results obtained should help to clarify the functional applications of these folk herbs and their essential oils for aromatherapeutic healing and other folkloric uses.
69 citations
TL;DR: In this paper, the authors investigated the phytochemistry and cytotoxic activity of the leaf, branch and fruit extracts of Vatica diospyroides Symington type LS, an endangered medicinal plant in Thailand.
Abstract: Purpose: To investigate the phytochemistry and cytotoxic activity of the leaf, branch and fruit extracts of Vatica diospyroides Symington type LS, an endangered medicinal plant in the peninsula of Thailand. Methods: Extracts of the mature leaves, branches and fruit (both cotyledon and pericarp) of five-year old tree were obtained using various organic solvents. Thin‐layer chromatography (TLC) and phytochemical screening were employed to identify the chemical constituents. Cytotoxicity was characterized by 50 % inhibition (IC 50 ) of human breast cancer cell lines (MCF-7 and MDA-MB-468) using 3-(4,5-dimethylthaizol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results: The extracts of the plant parts differed in chemical composition. Terpenoids and anthraquinones were present in all extracts, while cardiac glycosides and tannins were isolated from the branches and leaves, respectively. The acetone and methanol extracts of the fruit cotyledons were highly cytotoxic against MDA-MB-468 cell line (IC 50 = 3.1 µg/ml for both extracts), whereas acetone and dichloromethane extracts of the fruit pericarps were highly active against MCF-7 cell line (IC 50 = 18.2 and 21.0 µg/ml, respectively). The other extracts were less active. Conclusion: This work revealed the potentials of V. diospyroides fruit as a cytotoxic agent against human breast cancer cell lines. However, further studies, including identification and purification of the active compounds, will need to be pursued.
59 citations
TL;DR: F. vulgare may be useful in the management of stress and stress-related disorders on account of its multiple actions such as anti-stress, memory-enhancing and antioxidant effects.
Abstract: Purpose : To evaluate the anti-stress and memory-enhancing properties of F. vulgare extract in experimental rats. Methods: F. vulgare plant extract was obtained using Soxhlet extraction technique. The extract, at doses of 50, 100 and 200 mg/kg body weight, was administered orally with an orogastric tube. Urinary levels of vanillylmandelic acid (VMA) and ascorbic acid in rats were used to evaluate anti-stress activity. Conditioned avoidance response was measured in normal and scopolamine-induced amnesic rats to study the memory-enhancing effects. Lipid peroxidation inhibition assay in liver and brain homogenates of rats was used to evaluate antioxidant activity. Results : Daily administration of F. vulgare extract (50, 100 and 200 mg/kg body weight) 1 h prior to induction of stress significantly (p < 0.05) altered the stress-induced urinary biochemical levels of VMA from 395.79 ± 11.23 to 347.12 ± 12.28, 311.21 ± 12.48 and 258.86 ± 10.26 μg/kg, respectively, in 24 h, as well as ascorbic acid excretion levels from 65.74 ± 9.42 to 78.59 ± 8.44, 108.41 ± 15.62 and 125.82 ± 16.94 μg/kg also within the same period, respectively. These changes occurred in a dose-dependent fashion, and the levels in the control groups were unchanged within the same period. The memory deficits induced by scopolamine (1mg/kg, i.p.) in rats was reversed by F. vulgare dose-dependently. The extract also exhibited potent antioxidant effect by inhibition of lipid peroxidation in both rat liver and brain homogenates to a greater extent than the standard antioxidant, ascorbic acid. Conclusion: F. vulgare may be useful in the management of stress and stress-related disorders on account of its multiple actions such as anti-stress, memory-enhancing and antioxidant effects. Keywords: Foeniculum vulgare, Stress, Vanillyl mandelate, Memory, Antioxidant, Ascorbic acid
47 citations
TL;DR: The observed inhibitions of α-amylase and α-glucosidase suggest that the leaf extracts of P. nitida may be useful in the management of diabetes mellitus, which buttresses the traditional use of P-nitrophenylglucopyranoside in some parts of Nigeria.
Abstract: Purpose: To investigate the anti-diabetic potential of Picralima nitida leaf extracts in vitro. Methods: The current study evaluated the anti-diabetic potential of Picralima nitida leaf via in vitro inhibition of α-amylase and α-glucosidase using the acetone, water and ethanol extracts. Preliminary phytochemical analysis was performed on the acetone, aqueous and ethanol extracts of Picralima nitida leaf. The α-amylase inhibitory potentials of the extracts were investigated by reacting different concentrations of the extracts with α-amylase and starch solution while α-glucosidase inhibition was determined by pre-incubating α-glucosidase with different concentrations of the extracts followed by the addition of p-nitrophenylglucopyranoside (pNPG). The mode(s) of inhibition of both enzymes was determined using Lineweaver-Burke plot. Results: The acetone extract of Picralima nitida displayed the most effective inhibition of both αamylase and α-glucosidase activities with half-maximal inhibitory concentration (IC 50 ) of 6.50 and 3.00 mg/ml, respectively. The results also showed that the extracts contain both non-competitive and competitive inhibitors of α-amylase and α-glucosidase respectively. The results of phytochemical analysis of the extract revealed the presence of saponins, flavonoids, tannins, terpenoids and reducing sugars. Conclusion: The observed inhibitions of α-amylase and α-glucosidase suggest that the leaf extracts of P. nitida may be useful in the management of diabetes mellitus. This buttresses the traditional use of P. nitida for the management of sugar-related disorders in some parts of Nigeria.
44 citations
TL;DR: In this paper, the authors summarize the properties of poly(ethylene oxide) and poly(propylene oxide) based copolymers and highlight the works that have been carried out on these materials for transdermal drug delivery.
Abstract: Amphiphilic poly(ethylene oxide)–poly(propylene oxide) (PEO–PPO)-based copolymers are thermoresponsive materials having aggregation properties in aqueous medium. As hydrosolubilizers of poorly water-soluble drugs and improved stability of sensitive agents, these materials have been investigated for improvement in solubility, stability, release and bioavailability of drugs. The goal of the present review is to summarize the properties of PEO–PPO based copolymers and highlight the works that have been carried out on these materials for transdermal drug delivery.
40 citations
TL;DR: There is a high rate of wound infection in Kano, Nigeria and that antibiotic-resistant bacteria are present in the wound sites, and in vitro antibiotic susceptibility tests showed that Pseudomonas aeruginosa was susceptible to ceftazidime, ciprofloxacin and gentamicin.
Abstract: Purpose: To investigate the incidence of different bacteria isolates in 150 wound infections in Aminu Kano Teaching Hospital, Kano, Nigeria and their antibacterial susceptibility patterns. Methods : Wound swab samples were collected from general culture bench of the Microbiology Department, after obtaining consent from the hospital’s Medical Advisory Committee, and cultured for bacterial isolates. The isolates were characterized and identified by standard microbiological methods. Antibiotic susceptibility testing was carried out using Kirby-Bauer-CLSI modified Disc Agar Diffusion technique. Results : Out of the 150 specimens collected, 82 % were infected with bacteria made up predominantl of Staphylococcus aureus (22 %), Pseudomonas aeruginosa (19.9 %), Citrobacter spp (15 %), Escherichia coli (14.7 %) and Proteus mirabilis (14.5 %). In vitro antibiotic susceptibility tests showed that Pseudomonas aeruginosa was susceptible to ceftazidime, ciprofloxacin and gentamicin while the enteric bacteria were generally more resistant to ceftazidime, gentamicin and ciprofloxacin. Conclusion: The findings show that there is a high rate of wound infection in Kano, Nigeria and that antibiotic-resistant bacteria are present in the wound sites. Keywords : Wound infection , Antibiotic, Susceptibility, Bacterial resistance
36 citations
TL;DR: Resistance to tetracyclines is mainly by efflux pumps mediated by tet(K) in S. aureus in northwestern Pakistan, and a majority of the MRSA and all the MSSA were sensitive to doxycycline and minocycline.
Abstract: Purpose: To determine the prevalence and genetic basis of tetracycline resistance in Staphylococcus aureus. Methods: One hundred and thirty (130) clinical isolates of S. aureus were collected from Khyber Teaching Hospital, Peshawar, Pakistan. Susceptibility to antibiotics (doxycycline, tetracycline and minocycline) was determined by Kirby-Bauer disc diffusion method with minimum inhibitory concentration (MIC) evaluated on Muller-Hinton agar as described by the Clinical and Laboratory Standards Institute (CLSI). The tetracyclineresistant strains (TET-R) were screened by polymerase chain reaction (PCR) for the presence of four common tetracycline resistance determinants, viz, tet(K), tet(L), tet(M) and tet(O). Results: Sixty (46.0 %) of these isolates were methicillin-resistant S. aureus (MRSA) while 70 (54.0 %) were methicillin-susceptible S. aureus (MSSA). Seventy four (56.9 %) strains were resistant to tetracycline (TET-R), 30 (23.1 %) to minocycline and 23 (17.7 %) to doxycycline. A majority of the MRSA were resistant to tetracyclines and all the MSSA were sensitive to doxycycline and minocycline. The tet(K) gene was found in 58 isolates and tet(L) in one isolate. No tet(M) and tet(O) were detected. Conclusion: This study indicates that resistance to tetracyclines is mainly by efflux pumps mediated by tet(K) in S. aureus in northwestern Pakistan.
35 citations
TL;DR: In this article, the authors demonstrate eco-friendly biosynthesis of gold nanoparticles by Enterobacteriaceae by using pure colonies of nine different bacteria from the Enterobacteriaiaceae family.
Abstract: Purpose: To demonstrate eco-friendly biosynthesis of gold nanoparticles by Enterobacteriaceae.Methods: Pure colonies of nine different bacteria from the Enterobacteriaceae family were separated from water and cultured in Luria Bertani broth medium. Their respective supernatants were examined forability to produce gold nanoparticles. In this step, 1 mM solution of Gold(III) chloride trihydrate H(AuCl4) added to reaction matrices (supernatant) separately. The reaction was performed in a dark environment at 37 oC. After 24 h, it was observed that the color of the solutions turned to dark purple from light yellow. The gold nanoparticles were characterized by UV-Visible spectroscopy, dynamic light scattering,scanning electron microscopy and Fourier transform infrared spectroscopy (FTIR) for yield, particle size, shape and presence of different functional groups, respectively. The nanoparticles were centrifuged and re-dispersed in double distilled water thrice to purify them for FTIR studies.Results: The gold nanoparticles were fairly uniform in size, spherical in shape and with Z-average diameter ranging from 11.8 to 459 nm depending on the bacteria used. FTIR spectra revealed the presence of various functional groups in the gold nanoparticles which were also present in the bacterial extract.Conclusion: The current approach suggests that rapid synthesis of nanoparticles would be feasible in developing a biological process for mass scale production of gold nanoparticles.Keywords: Biosynthesis, Enterobacteriaceae, Gold nanoparticles
TL;DR: In this paper, the content of phenols, flavonoids and anthocyanins of the ethanol, ethanol-water (50/50,v/v) and water extracts of black mulberry were determined using spectrophotometric methods.
Abstract: Purpose: To evaluate the content of phenolic compounds (flavonoids and anthocyanins) of Morus nigra L. fruit (black mulberry) as well as the antioxidant activities of its extracts. Methods: The contents of phenols, flavonoids and anthocyanins of the ethanol, ethanol-water (50/50,v/v) and water extracts of black mullbery were determined using spectrophotometric methods. Antioxidant assay was based on the measurement of 2,2-diphenyl-1-picrylhydrazyl (DPPH) absorbance at 517 nm caused by the reaction of DPPH with the test sample, and also on the measurement of 2,2'azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) absorbance at 734 nm caused by the reaction of ABTS with the test sample. Results: Spectrophotometric analysis indicates that the content of total phenol compounds in the extracts varied from 90.26 to 118.84 mg GAE/100 g of fresh mulberry fruit. The content of anthocyanins ranged from 114.83 to 128.68 mg of cyanidin-3-O-glucoside/100 g of fresh fruit (ff). The fruit extract (0.1 ml) showed high antioxidant activity with DPPH radical transformation value of 71.41 % in ethanol-water (50/50, v/v)) extract and good antioxidant activity (relative to trolox equivalent as standard) with ABTS of 55.43 % in the water extract. Conclusion: The high phenolic content and high antioxidant activity of black mulberry from Southeast Serbia underline the nutritive and phytomedicinal potentials of the fruit. Further studies are, however, required before the fruit extract can be exploited in the production of health foods and as an antioxidant carrier in the food and pharmaceutical industries.
TL;DR: In this article, the effect of various surfactants and cosurfactants, and their ratio on microemulsions prepared with isopropyl palmitate (IPP) was investigated.
Abstract: Purpose: To investigate the effect of various surfactants and cosurfactants, and their ratio on microemulsions prepared with isopropyl palmitate (IPP) Methods: Tween 20, 40, 60, and 80 were used separately as surfactant with methanol, ethanol, 1propanol, 1-butanol or 1-pentanol as cosurfactant, and IPP as oil phase to prepare various microemulsions. Various surfactant to cosurfactant ratios (1:1, 2:1, 3:1, 4:1, and 1:0) were used in the preparation. Pseudoternary phase diagram was used to define the microemulsion area, and samples from the best combinations, i.e., those that produced the largest volume of microemulsion, were subjected to further characterization by polarized light microscopy, differential scanning calorimetry (DSC), zetasizer, rheometer, and for stability. Results: Based on the microemulsion areas produced in the pseudoternary phase diagrams, the the surfactants were ranked in the following order of effectiveness: Tween 80 > 60 > 40 > 20 while the alcohols (co-surfactants) were ranked as follows: 1-butanol > 1-pentanol > 1-propanol > ethanol = methanol. The best surfactant to cosurfactant ratio for microemulsion preparation was 3:1. Conclusion: The selected surfactant/co-surfactant combination (i.e., Tween 80:1-butanol, 3:1) produces a stable microemulsion possesses a good potential as a drug delivery system
TL;DR: In this paper, a floating microsphere of curcumin for prolonged gastric residence time and increased drug bioavailability has been developed by using emulsion solvent diffusion method, using hydroxylpropyl methylcellulose (HPMC), ethyl cellulose (EC), Eudragit S 100 polymer in varying ratios.
Abstract: Purpose : To prepare and evaluate floating microspheres of curcumin for prolonged gastric residence time and increased drug bioavailability. Methods : Floating microsphere were prepared by emulsion solvent diffusion method, using hydroxylpropyl methylcellulose (HPMC), ethyl cellulose (EC), Eudragit S 100 polymer in varying ratios. Ethanol/dichloromethane blend was used as solvent in a ratio of 1:1. The floating microspheres were evaluated for flow properties, particle size, incorporation efficiency, as well as in-vitro floatability and drug release. The shape and surface morphology of the microspheres were characterised by optical and scanning electron microscopy. Result : The floating microspheres showed particle size, buoyancy, drug entrapment efficiency and yield in the ranges of 251 - 387 im, 74.6 - 90.6 %, and 72.6 - 83.5 %, and 45.5 - 82.0 %, respectively. Maximum drug release after 20 h was 47.1, 55.7, 69.4 and 81.3 % for formulations F1, F2, F3 and F4, respectively. Scanning electron micrographs indicate pores both on the surface and interior of the microspheres. Conclusion : The developed curcumin microsphere system is a promising floating drug delivery system for oral sustained administration of curcumin. Keywords : Gastro-retentive, Sustained release, Curcumin, Floating microspheres; Ethyl cellulose, Hydroxylpropyl methylcellulose, Eudragit
TL;DR: In this paper, the authors evaluated antiglycation and antioxidant properties of Boswellia sacra resins using HPTLC analysis and showed that the results indicated the presence of 11-keto-β-boswellic acid (KBA) and 3-O-acetyl-11-ketoenacetyl11-kk-k-boswellic acids (AKBA) along with some other terpenoids.
Abstract: Purpose : To evaluate antiglycation and antioxidant activities as undertake HPTLC analysis of Boswellia sacra resin. Methods : Sub-fractionation of the crude methanol extract of Hougari regular (HR) grade resin of Boswellia sacra was carried out by vacuum liquid chromatography. Free radical scavenging and antiglycation activities of sub-fractions were characterized in order to assess their anti-aging properties. Furthermore, high performance thin layer chromatography (HPTLC) analysis of Boswellia sacra resins was also carried out. Results: Polar fractions of the extract obtained exhibited the highest antiglycation activity while nonpolar fractions showed more than 50 % inhibition in superoxide anion scavenging assay. Scavenging activity of reactive oxygen species results indicate that non-polar sub-fractions showed > 50 % inhibition, except Shabi frankincense (SF) oil which showed 33 % inhibition. Dichloromethane (CH 2 Cl 2 ) fraction, 40 % dichloromethane (CH 2 Cl 2 )/n-hexane sub-fraction, and SF oil showed moderate activity in di(phenyl)-(2,4,6-trinitrophenyl) iminoazanium (DPPH) assay. Furthermore, HPTLC analysis indicates the presence of 11-keto- β-boswellic acid (KBA) and 3-O-acetyl-11-keto-β-boswellic acid (AKBA) along with some other terpenoids. Conclusion : Various sub-fractions of Boswellia sacra exert effective antiglycation and antioxidant activities. The extracts should be studied further for possible formulation into pharmaceutical products. Keywords: Frankincense, Boswellia sacra, Terpenoids, HPTLC, Antioxidant, Antiglycation
TL;DR: The aim of the present paper is to present an extensive review of the plants in this genus including their traditional uses, chemical constituents and pharmacology.
Abstract: Distribution, traditional uses, isolated chemical constituents and pharmacological activities of some common species of the genus Araucaria are reviewed in this paper. Almost 19 species belong to the genus, Araucaria. It is indigenous to North America. Biflavanoid, diterpene, phenyl propanoid and lignans are abundant in the genus. The most common pharmacological activity of Araucaria in modern medicines is anti-inflammatory. It also possesses other pharmacological activities such as antiulcer, antiviral, neuro-protective, anti-depressant and anti-coagulant. The aim of the present paper is to present an extensive review of the plants in this genus including their traditional uses, chemical constituents and pharmacology. Keywords : Araucaria, Ethnopharmacology, Phytochemistry, Biflavanoids, Diterpene
TL;DR: In this article, the authors investigated the crude n-hexane, ethyl acetate and methanol extracts of Aphanamixis polystachya fruit for their cytotoxic, antimicrobial, antioxidant and thrombolytic activities.
Abstract: Purpose: To investigate the crude n-hexane, ethyl acetate and methanol extracts of Aphanamixis polystachya fruit for their cytotoxic, antimicrobial, antioxidant and thrombolytic activities. Methods: The fruit extracts were screened for major phytochemical compounds using in vitro established procedures. Antimicrobial and cytotoxic studies of the fruit extracts were conducted using disc diffusion and brine shrimp lethality bioassay methods, respectively, while an in vitro thrombolytic model was used to assess the clot lysis effect of the extracts with streptokinase as positive control. Antioxidant activity was evaluated by free radical scavenging activity using 2, 2-diphenyl-1picrylhydrazyl (DPPH) and nitric oxide assay as well as total phenolic content. Results: The fruit extracts were a rich source of phytochemicals and among the extracts n-hexane extract showed highest antimicrobial activity against Shigella dysenteriae (zone of inhibition: 9.7±0.2 mm) and Candida albicans (zone of inhibition: 8.8±0.3 mm) at a concentration of 1000µg/disc, whereas at the same concentration methanol extract showed highest zone of inhibition, 10.1±0.4mm, against Staphylococcus aureus. Compared to potassium permanganate with a median lethal concentration (LC 50 ) of 13.23 µg/ml in the brine shrimp lethality assay, the LC 50 of n-hexane, ethyl acetate and methanol extracts were 15.77, 17.51 and 141.37 µg/ml, respectively. All the extracts showed significant clot lysis activity (p < 0.001) with reference to negative control and % clot lysis of the extracts were approximately 13. Notable antioxidant activity of the methanol extract was observed unlike the other extracts. Conclusion: The results of the study demonstrated the potential cytotoxic, thrombolytic and antioxidant activities of the fruit extracts of A. polystachya and therefore further studies on the isolation and identification of active principles are required.
TL;DR: A review of the antimicrobial activity of HOCl and its methods of analysis is presented in this paper, where the authors consider a broad range of microorganisms that are resistant to HOCl.
Abstract: Hypochlorous acid (HOCl) is produced by the human body’s immune cells to fight infections. It is effective against a broad range of microorganisms. It is non-toxic, non-irritant and non-corrosive at proper usage concentrations. There are some available commercial products that contain HOCl. However, its low storage stability constitutes a major challenge. This review considers the antimicrobial activity of HOCl and its methods of analysis.
TL;DR: The study showed that fluoroquinolones and aminoglycosides could be used as first line AMs for the effective management of LRTI in a hospital setting.
Abstract: Purpose: To undertake an audit of the antimicrobial (AM) sensitivity pattern of bacterial isolates in the intensive care units (ICU) of a tertiary hospital of Bhavnagar, India. Methods: Retrospective analysis of the indoor case papers of ICUs from January 2010 to 31st March 2011 was carried out at Department of Pharmacology, Govt. Medical College and Sir Takhtsinhji General Hospital, Bhavnagar, India. Information collected include demographic data of the patient, admission unit, duration of hospital stay, diagnosis, type of infection, empirical treatment, indication of the use of the antimicrobials (AMs). Others include collected specimen, causative agent, sensitivity pattern, and treatment changes based on the sensitivity pattern in a case record form. AM sensitivity testing was performed by the modified Kirby Baur method as recommended by clinical and laboratory standard institute (CLSI). Internal and external quality control were maintained for culture and sensitivity method. Results: The most commonly isolated organisms were Klebsiella pneumoniae (28.6 %) and Pseudomonas aeruginosa (16.3 %). Lower respiratory tract infection (LRTI) was the most common infection. Imipenem, meropenem and levofloxacin were the most effective antimicrobials for Gramnegative isolates (GNIs) while vancomycin ciprofloxacin, and gentamicin were the most efficacious antimicrobials for Gram-positive isolates (GPIs). Widespread resistance to third generation cephalosporins and cloxacillin was noted for GNIs and GPIs, respectively. Meropenem (100 %) > levofloxacin (100 %) > sparfloxacin (94.4 %) > gentamicin (83.3 %) was the rank order of antimicrobial activity against LRTI. Conclusion: GNIs were the predominant cause of infection in ICUs. Third generation cephalosporinsresistant GNIs were the predominant resistant organisms. The study showed that fluoroquinolones and aminoglycosides could be used as first line AMs for the effective management of LRTI in a hospital setting.
TL;DR: The findings obtained indicate that the essential oil of C. gracile has potentials for use in the control of A. albopictus larvae and could be useful in the search for new, safer and more effective natural compounds as larvicides.
Abstract: Purpose: To determine larvicidal activity of essential oil derived from Clinopodium gracile (Benth.) Matsum. (Labiatae) aerial parts against the larvae of Aedes albopictus Skuse． Methods: Essential oil of C. gracile aerial parts was obtained by hydrodistillation and analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The activity of the essential oil was evaluated, using World Health Organization (WHO) procedures, against the fourth larvae of A. albopictus for 24 h and larval mortality recorded at a various essential oil concentrations ranging from 12.5 – 200.0 μg/mL. Results: A total of 34 components of the essential oil of C. gracile were identified. The essential oil has higher content of sesquiterpenoids (70.49 %) than monoterpenoids (12.21 %). The other principal compounds of the essential oil were germacrene D (20.59 %), nootkatone (8.22 %), morillol (7.74 %), βelemene (7.38 %), α-bergamotene (6.08 %), cis-β-farnesene (5.47 %) and caryophyllene (5.17 %). The essential oil exhibited larvicidal activity against A. albopictus with a median lethal concentration (LC50) of 42.56 μg/mL. Conclusion: The findings obtained indicate that the essential oil of C. gracile has potentials for use in the control of A. albopictus larvae and could be useful in the search for new, safer and more effective natural compounds as larvicides.
TL;DR: In this paper, a simple, precise and rapid high-performance liquid chromatographic technique coupled with photodiode array detection (DAD) method for the simultaneous determination of rutin, quercetin, luteolin, genistein, galangin and curcumin in propolis was developed.
Abstract: Purpose: To develop a simple, precise and rapid high-performance liquid chromatographic technique coupled with photodiode array detection (DAD) method for the simultaneous determination of rutin, quercetin, luteolin, genistein, galangin and curcumin in propolis. Methods: Ultrasound-assisted extraction was applied to isolate six antioxidant phenolic compounds from propolis samples. Chromatographic separation was performed using an Eclipse XDB-C18 column (150 mm×4.6 mm, 5 The mobile phase consisted of phosphate buffered saline (pH = 4.5) and methanol (40/60, v/v). The flow rate was set at 0.8 ml/min and the effluent was monitored using a DAD set at 260 nm. Results: Excellent linear correlation coefficient was observed in the range of 0.9977 to 0.9997. The reproducibility of the method was 1.58 % (RSD) and accuracy was confirmed with average recovery ranging from 95.71 to 104.26 %. Six antioxidant phenolic compounds in propolis samples were successfully determined within 50 min. Conclusion: The proposed isocratic LC method gave good separation and accurate determination of rutin, quercetin, luteolin, genistein, galangin and curcumin in propolis. The proposed method showed good sensitivity, linearity, repeatability and accuracy.
TL;DR: In this article, solid dispersions of praziquantel (PZQ) with sodium starch glycolate (SSG) for enhanced drug solubility were developed and characterized.
Abstract: Purpose: To develop and characterize solid dispersions of praziquantel (PZQ) with sodium starch glycolate (SSG) for enhanced drug solubility. Methods: PZQ solid dispersion (SD) was prepared using co-precipitation method by solvent evaporation. The ratios of PZQ to SSG were 2:1, 1:1, 1:2, 1:3 (w/w). PZQ solubility was evaluated in purified water, and PZQ dissolution test was carried out in 0.1N HCl. Structural characterization of the dispersions was accomplished by x-ray diffraction (XRD) and infrared spectroscopy (FTIR) while the external morphology of the SDs, SSG and PZQ were studied by scanning electron microscopy (SEM). Mucoadhesion properties of the SD (1:3) and SSG, on mucin disks were examined using texture profile analysis. Results: The highest solubility was obtained with 1:3 solid dispersion, with PZQ solubility of 97.31 %, which is 3.65-fold greater than the solubility of pure PZQ and physical misture (PM, 1:3). XRD results indicate a reduction in PZQ crystallinity while infrared spectra showed that the functional groups of PZQ and SSG were preserved. SEM showed that the physical structure of PZQ was modified from crystalline to amorphous. The amount of PZQ in PM and SD (1:3) that dissolved in 60 min was 70 and 88 %, respectively, and these values increased to 76 and 96 %, respectively. The solid dispersion reduced the mucoadhesive property of the glycolate. Conclusion: Solid dispersion formulation using SSG is a good alternative approach for increasing the dissolution rate of PZQ.
TL;DR: The current review is an update on the reported pharmacological activities and phytochemical constituents of T. crispa.
Abstract: Tinospora crispa Beumee, a herbaceous climber, has been widely used in traditional medicine for treating various ailments such as contusion, septicaemia, fever, fracture, scabies and other tropical ulcers. A wide range of secondary metabolites such as alkaloids, diterpenes, flavones, phenolics, and triterpenes have been isolated, some of which have also shown corresponding biological activities. The current review is an update on the reported pharmacological activities and phytochemical constituents of T. crispa.
TL;DR: In this article, the effect of millet dietary fibre fermentation on the production of short chain fatty acids (SCFA) by four probiotics was studied, and the quantity of different SCFAs produced was in the rank order: acetate > propionate > butyrate.
Abstract: Purpose : To enhance the in vitro synthesis of short chain fatty acids through millet dietary fibre fermentation by human faecal probiotic bacteria. Methods : The effect of millet dietary fibre fermentation on production of short chain fatty acids (SCFA) by four probiotics was studied. Dietary fibre was extracted from two millet varieties viz Pearl millet, Pennisetum glaucum (PM) and Foxtail millet (FxM, Setaria italica), and separated into total dietary fibre (TDF), insoluble dietary fibre (IDF) and soluble dietary fibre (SDF). Four probiotic bacteria (Lactobacillus rhamnosus, Lactobacillus acidophilus, Bifidobacterium longum and Bifidobacterium bifidus) were grown on specific medium containing IDF, SDF and TDF. SCFA production by the probiotics was measured at 0, 6, 24, and 48 h using gas liquid chromatography. Results : SCFA production in the fibre fractions followed the rank order, TDF > SDF > IDF, irrespective of millet variety, indicating that TDF is the best possible dietary fibre for SCFA production. Lactobacillus and Bifidobacteria spp. digested 60 – 80 and 75 – 85 % of the millet fibre fractions from both millet samples, respectively. The quantity of different SCFAs produced was in the rank order: acetate > propionate > butyrate. Conclusion : The results from this study suggest that millet dietary fibre has a potential for conversion into new nutraceuticals. Keywords : Probiotic, Millet, Short chain fatty acid, Prebiotic, Probiotic, Dietary fibre
TL;DR: The n-hexane fraction of Viola betonicifolia (VBHF) has some analgesic and anti-inflammatory activities that justifies its use in traditional medicine for pain of management.
Abstract: Purpose: To evaluate the analgesic and anti-inflammatory activities of n-hexane extract of the whole plant of Viola betonicifolia Sm, family: Violaceace.Methods: The n-hexane fraction of Viola betonicifolia (VBHF) was tested for its analgesic and antiinflammatory activities (carrageenan-induced and histamine-induced edema models) in BALB/c mice.Results: VBHF exhibited significant (p < 0.01) analgesic and anti-inflammatory activity at test doses of 100, 200 and 300 mg/kg. The analgesic effect of VBHF was dose-dependent in acetic acid pain modelwhile the extract was a weak analgesic at the dose of 300 mg/kg in hot plate and tail immersion test. Diclofenac sodium and tramadol showed better analgesic properties to the extract. Analgesia was not antagonized by naloxone in the hot plate model. Anti-inflammatory activity against carrageenan-induced edema was 60.8 %; however, histamine-induced inflammation was not antogonised by the extract.Conclusions: The extract has some analgesic and anti-inflammatory activities. This justifies its use in traditional medicine for pain of management.Keywords: Viola betonicifolia, Analgesic, Anti-inflammatory.
TL;DR: It is demonstrated that pharmacists can play a pivotal role in improving glycemic control in diabetic patients and that involvement of pharmacists in diabetic clinics is beneficial to the patients in terms of medication adherence and promotion of healthy lifestyle.
Abstract: Purpose: To assess the impact of pharmacist-led multifactorial interventions on health parameters, medication adherence, and disease-related knowledge among type 2 diabetic patients in southern Punjab, Pakistan. Methods: The effect of intervention was evaluated by randomly assigning patients into control group (n = 170), receiving conventional medical care, and intervention group (n = 178), receiving predefined specialized care. The primary outcome of this intervention study was improvement in glycemic control which was assessed by measuring fasting blood glucose and glycosylated haemoglobin (HbA1c) values. Results: The outcomes obtained clearly show the role of pharmacist counseling in the control of type 2 diabetes while improving fasting blood glucose (FBG) and HbA1c levels, reduction in Body Mass Index (BMI), improvement in disease knowledge as well as reduction in smoking. The intervention significantly reduced BMI and waist circumference by a difference of 1.87 (p = 0.014) and 1.27 (p = 0.002) between control and intervention groups. Glycemic control was significant within the intervention group, as evident by a reduction in fasting blood glucose level {-19.26 mg/dL (p = 0.003)} and HbA1c level {-1.01 % (p < 0.001)} compared to control group. The mean difference in glycemic control between both groups was insignificant but mild reductions were seen in fasting blood glucose (-11.95 mg/dL, p = 0.11) and HbA1c (-0.43 %, p = 0.12). A significant increase in disease-related knowledge was seen in the intervention group, compared to the control group which was evident by mean differences in compliance (p = 0.003), foot-care (p < 0.001) and self-monitoring of blood glucose (p = 0.001). Conclusion: The purpose of study was achieved in that it demonstrates that pharmacists can play a pivotal role in improving glycemic control in diabetic patients and that involvement of pharmacists in diabetic clinics is beneficial to the patients in terms of medication adherence and promotion of healthy lifestyle.
TL;DR: Three plants including Boesenbergia pandurata, Eleutherine americana, and Rhodomyrtus tomentosa exhibited good antibacterial activity against all S. pyogenes isolates and produced similar activities against different tested isolates.
Abstract: Purpose: To evaluate the anti-Streptococcus pyogenes activity of selected medicinal plants used in Thai traditional medicine. Methods: Sixty-nine extracts of 51 selected Thai medicinal plant species were tested for anti-S. pyogenes activity by paper disc agar diffusion and broth microdilution methods. Results: Ten plants including Boesenbergia pandurata (Roxb.) Schltr., Cinnamomum bejolghota (Buch.-Ham.) Sweet, Cinnamomum porrectum (Roxb) Kosterm, Eleutherine americana Merr., Gymnopetalum cochinchinensis (Lour.) Kurz, Piper betle L., Quercus infectoria G. Olivier, Quisqualis indica L, Rhodomyrtus tomentosa (Aiton) Hassk., and Walsura robusta Roxb. demonstrated good antibacterial activity against S. pyogenes NPRC 101. These plants were selected and further evaluated for their anti-S. pyogenes activity against 11 isolates of S. pyogenes from patients with upper respiratory tract infections. Three plants including Boesenbergia pandurata, Eleutherine americana, and Rhodomyrtus tomentosa exhibited good antibacterial activity against all S. pyogenes isolates and produced similar activities against different tested isolates. Boesenbergia pandurata and Rhodomyrtus tomentosa demonstrated antibacterial activity with the same minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) range of 3.91 - 31.25 µg/ml whereas Eleutherine americana displayed MIC and MBC values of 250 and 250-500 µg/ml against all S. pyogenes isolates. Conclusion: Boesenbergia pandurata, Eleutherine americana, and Rhodomyrtus tomentosa have great antibacterial potentials against S. pyogenes.
TL;DR: Investigation of solid lipid nanoparticle systems containing dextran sulfate or sodium alginate as anionic polymers for the delivery of clindamycin phosphate as a model hydrophilic cationic drug revealed that incorporation of anionics increased drug loading of the SLNs.
Abstract: Purpose: To develop and characterize solid lipid nanoparticle (SLN) systems containing dextran sulfate or sodium alginate as anionic polymers for the delivery of clindamycin phosphate as a model hydrophilic cationic drug. Methods: A multi-level factorial design was used for the preparation and optimization of clindamycin SLNs. Polymers (dextran sulfate and sodium alginate), Tween 80, and Pluronic F68 were chosen as the independent variables. The SLNs were prepared using stearic acid as the lipid matrix by an emulsion congealing technique with cold homogenization. Particle size and drug loading were evaluated as the primary responses. The morphology and drug release rate of the selected formulations were also determined. Results: The results revealed that incorporation of anionic polymers increased drug loading of the SLNs. Dextran sulfate had a greater effect on drug loading, increasing it from 1.32 to 18.19 %, compared to the 6.73 % achieved using sodium alginate. Dextran sulfate also reduced drug release rate by half compared with sodium alginate, probably due to the higher charge density, lower molecular weight and lower branching density of the ionic polymer. Conclusion: Incorporation of anionic polymers can increase the loading of clindamycin phosphate into SLNs. Drug release from SLNs is also dependent on the polymer type.
TL;DR: It seems that the aqueous-methanol extract of Berberis orthobotrys possesses active compounds which may be responsible for the antihypertensive and negative chronotropic effects in rats.
Abstract: Purpose: To investigate the hypotensive potential of Berberis orthobotrys Bien Ex Aitch (Family: Berberidaceae) in both normotensive and hypertensive rats. Methods: Aqueous-methanol (70:30) extract of Berberis orthobotrys at doses of 25, 50, 75 and 100 mg/kg was evaluated for its effect on blood pressure and heart rate using non-invasive blood pressure measuring apparatus. After initial screening, 100 mg/kg dose that produced a maximum effect was selected for the antihypertensive study. Median lethal dose (LD 50 ) and sub-chronic toxicity of the extract were also determined. Various biochemical parameters and organ weight were measured using standard procedures. Results: The extract produced a significant (p < 0.01) decrease in systolic blood pressure (SBP), mean blood pressure (MBP), diastolic blood pressure (DBP) and heart rate of normotensive rats at all test doses with maximum effect at 100 mg/kg. Similarly, a significant antihypertensive and negative chronotropic effect was observed in both hypertensive models. LD 50 of the extract was 200 mg/kg in mice. The extract also exhibited a reduction (p < 0.05) in serum alanine transaminase (ALT), aspartate aminotransaminase (AST), alkaline phosphatase (ALP), triglycerides and low density lipoprotein (LDL) levels while a significant (p < 0.05) increase in high density lipoproteins (HDL) level was observed. Conclusion: It seems that the aqueous-methanol extract of Berberis orthobotrys possesses active compounds which may be responsible for the antihypertensive and negative chronotropic effects in rats.
TL;DR: Entrapment of ibuprofen in glutaraldehyde-cross-linked chitosan microparticles can be exploited to target and control the release of the drug and possibly reduce its gastro-erosive side effects.
Abstract: Tropical Journal of Pharmaceutical Research is indexed by Science Citation Index (Purpose: Toformulate glutaraldehyde-cross-linked chitosan-based microparticles and evaluate its suitability for the delivery of ibuprofen, a BCS class II drug. Methods : Ibuprofen-loaded chitosan microparticles were prepared by emulsification-cross-linking technique using glutaraldehyde saturated toluene (GST) as the cross-linking agent. The microparticles were characterized with respect to morphology, particle size, microparticle yield and entrapment efficiency. The swelling behaviour of the particles and ibuprofen release were assessed in both simulated gastric fluid (SGF) without pepsin (pH 1.2) and simulated intestinal fluid (SIF) without pancreatin (pH 7.4). Results : Discrete and free-flowing microparticles of size range 100.05 ± 8.82 to 326.70 ± 10.43 im were obtained. The microparticles had a high yield (69.2 to 99.2 %) and exhibited greater water sorption capacity in SIF (122.2 %) than in SGF (60 %). Furthermore, the microparticles cross-linked with 10 ml of GST entrapped the highest amount of drug (23.32 ± 0.97 %) while those cross-linked with 25 ml GST had the highest yield of the microparticles (99.19 % ), and highest water sorption in SIF (122.2 %). Up to 93.6 % of the entrapped drug was released in SIF from microparticles cross-linked with 25 ml of GST. Drug release from microparticles cross-linked with 20 and 30 ml each of GST showed a biphasic pattern. Conclusions : Entrapment of ibuprofen in glutaraldehyde-cross-linked chitosan microparticles can be exploited to target and control the release of the drug and possibly reduce its gastro-erosive side effects. Keywords : Chitosan microparticles, Ibuprofen, Oral delivery, Gastrointestinal, Glutaraldehyde.