Folate Conjugated Solid Lipid Nanoparticles of Carboplatin for Targeting Cancer Cells

V.      Sankar; Shalini      Devi Penmetsa; C.      Sabarinath

doi:10.2174/2210304x11202030162

Abstract

The present study investigates the specific drug targeting of anti cancer drugs, such as carboplatin by incorporation into folate conjugated Solid Lipid Nanoparticles (SLN). Our results showed that SLN 5 has the greater entrapment efficiency of 87.50% and slow in-vitro drug release (65.31% of carboplatin was released in 12 hrs) among all the SLN formulations prepared by high speed homogenization using 23 factorial design. Then SLN 5 was further conjugated with folic acid and its mean particle size (312.208 nm) and in-vitro drug release in 12 hrs (63.43 %) were determined. The comparative in-vitro cytotoxicity for market formulation (Kemocarb), SLN and folate conjugated SLN was determined by MTT assay in Hep 2 cell line and the results showed that folate conjugated SLN has greater cytotoxicity of 70.64 % as it can specifically target the cancer cells through the folate receptors. In-vivo studies were carried out in female Wistar rats and the pharmacokinetic parameters were determined for the market formulation and folate conjugated SLN. The increase in the MRT and AUC values reflects the sustained release effect of folate conjugated SLN formulation and it confirms that it acts as a slow release carrier of carboplatin.

Keywords: Cancer, Carboplatin, Folate receptor, Hep 2 cell line, Solid Lipid Nanoparticles, Targeted drug delivery, anti-cancer agents, tumor site, polymer conjugates, polymeric micelles, solid lipid nanoparticles, liposomes, intracellular, Solid Lipid, High Speed Homogenization.