FORMULATION & EVALUATION OF GEMCITABINE HYDROCHLORIDE LOADED SOLID LIPID NANOPARTICLES

Gemcitabine hydrochloride is an antimetabolite (pyrimidine analog) currently being used as drug of first choice in pancreatic metastatic cancer. GEM is a rapidly metabolizing water soluble drug (log p = -1.4) with a short half-life of 42 to 94 mins (short infusions) and 245 to 638 mins (long infusions) respectively. To protect the drug from rapid metabolism and achieve sustained drug release an attempt is made to formulate and evaluate GEM loaded solid lipid nanoparticles. GEM SLNs were prepared using stearic acid and GMS as lipid core, tween 80 as emulsifier and PVA as co- emulsifier by double emulsion method. Parameters investigated includes particle size, zeta potential, drug entrapment efficiency (EE %) and in vitro drug release of the SLNs. Optimized SLNs had particle size of 60.4 nm, zeta potential of -45.7 mV, EE of 78.84% and cumulative percent drug release of 54.72 % in 24 hrs and 63.12 % in 48 hrs. SEM images confirmed that the optimized formulation was smooth, uniformly distributed and roughly spherical in shape. Stability studies indicated that optimized formulations were stable at 2-4°C than at 25°C. It is concluded that GEM loaded SLNs were successfully formulated and evaluated to sustain the drug release by bypassing the first pass ABSTRACT