Preparation Characterization and Evaluation of Receptor Mediated Nanoparticles of Paclitaxel

Abstract

This study focuses on the preparation of polymeric nanoparticles made of pegylated PLGA and further decorated with folate for targeted delivery. In this study, double emulsion solvent evaporation as well as a single emulsion solvent evaporation method were employed to formulate the folate surface engineered polylactic glycolic acid - polyethylene glycol (PLGA-PEG) nanoparticles (PPF) with polyvinyl alcohol (PVA) and Soluplus as the surfactant. A well-known benefit of paclitaxel (PTX) is its effectiveness in the treatment of cancer. There is a solubility problem with this compound, which can be resolved by adding ethanol and Cremophor EL to it, and it is commercially available under the name Taxol. Nevertheless, Cremophor EL has serious side effects, which makes it imperative to make use of some other approaches or delivery systems to improve its antitumor activity as well as to avoid the side effects. In the formulations, the drug polymer ratio has been optimized. For that several ratios of drug and polymer were evaluated in preliminary small batches. newlinePreliminary evaluations demonstrated a drug polymer ration of 1:2 as the optimum ratio. Both PLGA as well as PPF nanoparticles were prepared for the purpose of newlineloading PTX into the nanoparticles and then characterized for their particle size, newlinepolydispersity index, zeta potential, drug loading, drug entrapment efficiency, and in vitro drug release efficiency. Based on the in vitro drug release characteristics, the best formulation F4 was selected for observing its surface morphology by scanning electron microscope (SEM) and transmission electron microscope (TEM). In vitro release kinetics analysis reveals that the delivery system follows a Korsmeyer-Peppas model that suggests a quotFickian diffusionquot mechanism. Furthermore, in vitro cytotoxicity studies were performed using MCF 7 breast cancer cell lines and the results demonstrated significantly higher cytotoxicity by the PPF-NPs. Paclitaxel encapsulated PLGA-NPs nanoparticles (PLGA-NPs) and blank PPF-NPs on breast can