ACTA Pharmaceutica Sciencia 2011 , Vol 53 , Num 4
SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS (SMEDDS) OF EFAVIRENZ: FORMULATION DESIGN, IN VITRO AND IN VIVO ASSESSMENT
MAHENDRA NAKARANİ, JAYVADAN PATEL, PRİYAL PATEL, SUBHASH VAGHANİ
S.K. Patel College of Pharmaceutical Education and Research, Ganpat University, Gujarat, India Efavirenz SMEDDS formulations containing lipid, surfactant and cosurfactant were developed and evaluated in vitro and in vivo. Pseudo-ternary phase diagrams composed of lipid, cosurfactant, surfactant and water were mapped and the region of microemulsion occurring was plotted. SMEDDS formulations were investigated for microemulsifying properties, clarity, precipitation, % Transmittance, Viscosity, Droplet size/size distribution, Zeta potential and long-term physical stability. The morphology of efavirenz microemulsion was observed by transmission electron microscopy (TEM). The in vitro release profiles of SMEDDS were compared with the release profiles of efavirenz from the conventional tablet and pure efavirenz. The pharmacokinetic study was performed by oral administration of 4.465 mg/kg efavirenz to Albino rats in different formulations. The oral bioavailability of efavirenz in SMEDDS capsules was significantly increased than that of the conventional tablet (p<0.05). The study confirmed that SMEDDS formulation can be used as a possible alternative to traditional oral formulations of efavirenz to improve its bioavailability. Keywords : EFAVIRENZ, SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS, BIOAVAILABILITY, PSEUDO TERNARY PHASE DIAGRAM, DISSOLUTION

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