SMEDDS elf Micro Emulsifying Drug Delivery Systems Based Drug Delivery of Some Antidiabetic Bioactives

Abstract

newline The current research work was executed with an aim to explore and promote the potential of self-microemusifying drug delivery systems (SMEDDS) in the form of tablets, in order to enhance solubility and oral bioavailability of poorly aqueous soluble drugs Repaglinide (RPG) and Pioglitazone (PGZ). RPG loaded liquid SMEDDS were developed consisting Labrafil M 1944CS, Kolliphor EL and Propylene glycol as lipid, surfactant and cosurfactant, whereas PGZ loaded liquid SMEDDS were developed consisting Capryol 90, Cremophor ELP and Transcutol HP as lipid, surfactant and cosurfactant which were then characterized on various parameters. After characterization and optimization, RPG liquid SMEDDS were converted into solid form by adsorbing on Aeroperl® 300 pharma and polyplasdoneTM XL and PGZ liquid SMEDDS were converted into solid form by adsorbing on Syloid 244FP and Kollidon CL-SF. Further, selection of suitable excipients was done and mixed with prepared solidified SMEDDS powder followed by preparation of self-microemulsifying tablets (SMET s) by wet granulation-compression method. SMET s were subjected to various characterization parameters like surface morphology, differential scanning calorimetry (DSC) , particle x-ray diffraction (RXRD) studies etc, results of which indicated transformation of crystalline structure of RPG and PGZ both because of dispersion of RPG and PGZ at molecular level in liquid SMEDDS. This was further assured by micrographs obtained from scanning electron microscope. RPG SMET s shown more than 85% (30min) of in-vitro drug release in contrast to conventional marketed tablets (13% and 32%) and pure drug (3.2% and 18.4%) whereas PGZ SMET s shown more than 80% (30min) of in-vitro drug release in contrast to conventional marketed tablets (15% and 41%) and pure drug (2.9% and 20.2%) in simulated gastric fluid and simulated intestinal fluid. Results of in-vivo studies furnished that RPG SMET s had shown marked decrease in blood glucose level and prolonged duration of action (up to 8hrs) in comp