ANTI-DIABETIC BIOACTIVE TAILORED TRANSFERSOMES: AS A POTENTIAL CARRIER FOR ENHANCED TRANSDERMAL DELIVERY: FORMULATION DESIGN AND CHARACTERIZATION
Rashmi Haldkar* and Kriti Sood
ABSTRACT
Diabetes mellitus is a group of metabolic disorder characterized by a complete lackof insulin, a relative lack of insulin, or insulin resistance. In response to the need forbetter control of diabetes, several new classes’ antidiabetic drugs were introduced.Miglitol is a second-generation-glycosidase inhibitor with a chemical structure of1-desoxynojiromycin. It acts as a potent competitive inhibitor of the alfaglycosidase in the microvilli of the intestinal brush border. Miglitol has a shortbiological half-life (2 h) and its bioavailability is>90%. Moreover, the site ofabsorption of miglitol is in the intestine. Transfersomes are particularly optimized,ultradeformable (ultraflexible) lipid supramolecular aggregates, which are able topenetrate the mammalian skin intact. Transfersome is a type of carrier systemwhich is capable of transdermal delivery of low as well as high molecular weightdrugs. Transfersomes penetrate through the pores of stratum corneum which aresmaller than its size and get into the underlying viable skin in intact form. The aimof the present study was to investigate the potential of transfersomal gelformulations for transdermal delivery of Miglitol and to evaluate the effect of lipidconcentration, ethanol concentration, drug concentration and stirrer time.Characterization of transfersomes performed by vesicle size, surface charge,entrapment efficiency and stability study. Characterization of transfersomescontaining gel performed by the measurement of viscosity, pH measurements, drugcontent, extrudability study, spreadability and in vitro drug diffusion study. It wasfound that viscosity of prepared gel MG-12 was 3350cps, % assay was 99.45±0.45,extrudability was 147g and spreadability (g.cm/sec) was found that 13.25(g.cm/sec)respectively. In vitro drug release from transfersomes gel was carried out usingFranz diffusion cell method and found 92.23% in 12 hr. In first 30 min it was 23.36% drug release which slightly high. It was due to the release of free drug present inbag after leaching from transfersomes. Drug release from transferosomal gelformulation was found in very sustained and controlled manner. The prepared gelcontaining miglitol-loaded transfersomal formulation was optimized and can be usefor topical preparation for its antidiabetic affect. The results were obtained whichshowed that transfersomal gel was a promising candidate for transdermal deliverywith targeted and prolonged release of a drug. It also enhances skin permeation ofmany drugs.
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