ABSTRACT
The present investigation reports the evaluation of potential use of Carbomer gel bearing methotrexate loaded nanostructured lipid carriers for topical application of methotrexate for possible therapy of psoriasis in comparison to solid lipid nanoparticles. These were evaluated for various parameters such as particle size, surface charge, entrapment efficiency, shape and surface morphology, thermal analysis, in-vitro drug release through skin (Franz diffusion cell) and drug deposition study, fluorescence microscopy, particle-skin interaction study, skin-irritation testing and storage stability. The formulation (NLC5) showed the best entrapment efficiency (62.72⯱â¯0.94%) while SLN showed only 26.84⯱â¯0.64% with particle size of 221⯱â¯14nm and 212⯱â¯11nm, respectively. Skin permeation study of MTX loaded SLN and NLC5 hydrogels showed prolonged drug release up to 24â¯h. The skin drug deposition study showed the greatest deposition of drug enriched NLC5 hydrogel (28.8%) when compared to plain drug enriched hydrogel (11.4%) and drug enriched SLN hydrogel (18.6%). Fluorescence microscopy suggested the localization effect of these lipid based systems to deeper skin region. The primary skin irritation studies indicated that MTX loaded SLN or NLC5 hydrogels resulted no erythema. It can be concluded that NLC represents a promising particulate carrier having prolonged drug release, improved skin permeation.
Subject(s)
Drug Delivery Systems , Methotrexate/administration & dosage , Psoriasis/drug therapy , Skin/drug effects , Acrylic Resins/administration & dosage , Acrylic Resins/chemistry , Administration, Cutaneous , Animals , Humans , Hydrogels/administration & dosage , Hydrogels/chemistry , Lipids/administration & dosage , Lipids/chemistry , Methotrexate/chemistry , Nanoparticles/administration & dosage , Nanoparticles/chemistry , Particle Size , Psoriasis/pathology , Rabbits , Skin Absorption/drug effectsABSTRACT
BACKGROUND: Tamarindus is a monotypic genus and belongs to the subfamily Caesalpinioideae of the family Leguminosae (Fabaceae), Tamarindus indica L., commonly known as Tamarind tree is one of the most important multipurpose tropical fruit tree species in the India, Sudan, Nigeria, Bangladesh and entire subcontinent. METHODS: Hydroethanolic seed coat extract of Tamarindus indica (HETI) was assessed for presence of phytoconstituents and selection of optimum dose through acute and sub acute toxicity study. The single and multidose (14 days) study were conducted to evaluate antidiabetic potential of HETI in alloxan induced rats via determine of blood glucose level, body weight, hematological profile, extra-pancreatic glucose utilization of isolated rat hemi-diaphragm as well as histopathology of rat pancreas. RESULTS: Phytochemical analysis of HETI showed the presence of polyphenol like flavonoids. Single and multidose of HETI significantly (p<0.05; p<0.001) reduced blood glucose level in normoglycaemic, glucose loaded and alloxan induced hyperglycaemic animals. HETI exerts the protective effect on pancreatic ß-cells as per results obtained from histopathology of animals. Moreover, HETI increased glucose uptake in isolated rat hemi-diaphragm and prevents decrease in body weight along with recovery of altered hematological parameters. CONCLUSIONS: The study revealed that HETI have potent hypoglycaemic action by virtue of its phytoconstituents and it can be used as a herbal medicine for diabetes.
Subject(s)
Alloxan/adverse effects , Diabetes Mellitus, Experimental/chemically induced , Diabetes Mellitus, Experimental/drug therapy , Hypoglycemic Agents/pharmacology , Polyphenols/pharmacology , Seeds/chemistry , Tamarindus/chemistry , Animals , Bangladesh , Blood Glucose/drug effects , Diabetes Mellitus, Experimental/metabolism , Fabaceae/chemistry , Female , Flavonoids/pharmacology , Fruit/chemistry , India , Insulin-Secreting Cells/drug effects , Male , Phytotherapy/methods , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Rats , Rats, WistarABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Phyllanthus amarus Schum. & Thonn. belongs to the family Euphorbiaceae is a small herb well known for its medicinal properties and widely used worldwide. P. amarus is an important plant of Indian Ayurvedic system of medicine which is used in the problems of stomach, genitourinary system, liver, kidney and spleen. It is bitter, astringent, stomachic, diuretic, febrifuge and antiseptic. The whole plant is used in gonorrhea, menorrhagia and other genital affections. It is useful in gastropathy, diarrhoea, dysentery, intermittent fevers, ophthalmopathy, scabies, ulcers and wounds. MATERIALS AND METHODS: The present review covers a literature across from 1980 to 2011. Some information collected from traditional Ayurvedic texts and published literature on ethanomedicinal uses of Phyllanthus amarus in different countries worldwide. RESULTS: Phytochemical studies have shown the presence of many valuable compounds such as lignans, flavonoids, hydrolysable tannins (ellagitannins), polyphenols, triterpenes, sterols and alkaloids. The extracts and the compounds isolated from P. amarus show a wide spectrum of pharmacological activities including antiviral, antibacterial, antiplasmodial, anti-inflammatory, antimalarial, antimicrobial, anticancer, antidiabetic, hypolipidemic, antioxidant, hepatoprotective nephroprotective and diurectic properties. CONCLUSION: The present review summarizes information concerning the morphology, ecology, ethnopharmacology, phytochemistry, biological activities, clinical applications and toxicological reports of P. amarus. This review aims at gathering the research work undertaken till date on this plant in order to provide sufficient baseline information for future works and commercial exploitation.
