Abstract

NANOSTUCTURED LIPID BASED DRUG DELIVERY SYSTEM OF LOPINAVIR- OPTIMIZATION AND EVALUATION

*Mr. Sunil Rambhau Sawale, Dr. R. V. Shete, Dr. Vishwas C. Bhagat. and Dr. Madhuri T. Deshmukh

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Abstract

By using the high-shear homogenization method Nanostructured lipid carriers (NLCs) loaded with lopinavir (LOP) were prepared. The LOPNLCs formulations were freeze-dried using POLOXOMER 188 as a cryoprotectant. A burst release is shown by in vitro release studies in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The optimized freeze-dried formulation (LOP-NLC) had a particle size (PS), zeta potential (ZP) and % entrapment efficiency (%EE) of 159.5 _ 3.75 nm, 0.413 _ 0.017, -46 mV and 97.77 _ 4.46%, respectively. A spherical shape was observed in the optimized formulation by transmission and scanning electron microscopes. The absence of chemical interaction between the drug and lipids is observed in Differential scanning Calorimetry study. In vitro study is performed using the bulk-equilibrium reverse dialysis technique, to investigate LOP release from optimized LOP-NLC and pure drug suspension in different media. The optimized formulations stored in amber glass container were found to be physically and chemically stable for three months at room temperature. The bioavailability of LOP following oral administration of LOP-NLC in male Wistar rats was found 4.52-fold higher than the LOP-suspension. So the conclusion is:- for improving the oral bioavailability of lopinavir, the nanostructure lipid carriers are potential carriers.

Keywords: lopinavir; lipid-based formulations; factorial design.