Design, Development and Characterization of Solid Lipid Nanoparticles of Gemcitabine Hydrochloride

Ashwini      S. Mokashi; Namdeo      R. Jadhav; Sheetalnath      B. Rooge

Abstract

Gemcitabine hydrochloride (Gem HCL) is a drug of choice for the treatment of most cancers, as a single or in combination chemotherapy. However, its bioavailability is a major concern because of its short half life and highly hydrophilic nature. To tackle this problem work has been planned to prepare solid lipid nanoparticles (SLN) of Gem HCL and analyzed them for drug carrying capacity and efficacy in vitro. The Gem HCL loaded nanoparticles (SLN) were prepared by microemulsion technique and optimized for drug carrying capacity, entrapment efficiency, stability, and effect of Gem HCL loaded SLN by MTT assay on human lung carcinoma cell lines (NCI-H522). SLN dispersion showed particle diameter ranging from 170 nm to 296 nm. The scanning electron microscopy (SEM) further confirmed the particle size of SLN. All SLN batches showed drug entrapment efficiency ranging from 29.6% to 65.66%. The results of differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) showed that Gem HCL was dispersed in SLN in an amorphous state. The in vitro drug release study of the optimized formulation in phosphate buffer (pH 7.4) showed 56.73% of release of Gem HCL over a period of 24 hrs. Significant enhancement in the cytotoxic effect of Gem HCL loaded SLN, was noted compared to its liposome formulations. SLN mediated delivery can enhance the cytotoxic effects of Gem HCL compared to free drug and its liposomal formulation.

Keywords: Solid lipid nanoparticles, Entrapment efficiency, Drug loading, Drug release, MTT assay, enhanced cytotoxicity, Gem HCL, Liposome, polymeric systems, SLN dispersion, Zeta potential, entrapment efficiency, ELISA, microemulsion, agglomeration