Lipid shell modified with combination of lipid and phospholipids in solid lipid nanoparticles for engineered specificity of paclitaxel in tumor bearing mice.

Sidharth Malgounda Patil, Hemant P. Joshi

Abstract


Paclitaxel (PTX) is an anticancer drug belonging to the class of Taxan. It is active against various types of carcinomas. The marketed formulation of paclitaxel is associated with deleterious effects with lack of specificity to tumor. Solid lipid nanoparticles (SLN) are colloidal carriers extensively studied and developed for there potential uses especially for controlled release and site specificity. The present study was designed to develop a formulation of PTX in the form of SLN to be administered via IV route with improved tumor specificity, in which the lipid shell was modified by using combination of lipid with phospholipids. Total eight formulations were prepared and were characterized by various in vitro and in vivo parameters. The microemulsification method was used for the preparation of SLN.The production yield  of resulting process for all SLN was high. Average particle size was ranged between 209 nm to 385 nm. The developed PTX-SLN showed high percentage entrapment efficiency. The zeta potential values showed the good stable feature of the sln.The in vitro dissolution study showed that drug release was more retarded and was found to dependent on concentration of lipids employed. In vitro cytotoxicity study was performed on MCF-7 cancer cell line, which showed that formulation G2 is having more potentiating effect on cancer cell line. Tissue targeting study and tumor growth inhibition studies were performed on mice where the PTX loaded SLN from batch G2 shown more promising outcome. Results obtained from this study indicated strongly that developed SLN are having potential as an efficient drug delivery system for paclitaxel.


Keywords


PTX, SLN, Modified Shell, Lipid and Phospholipids, Stearic Acid SLN

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