Abstract

ABSTRACT Introduction The present study is aimed to develop chitosan nanoparticles for efficient delivery of baicalein to HT29 (colon adenocarcinoma) cells. Chitosan nanoparticles are good drug carriers because of their good biocompatibility and biodegradability and can be readily modified. Methods The Chitosan (CS) nanoparticles, Baicalein loaded chitosan nanoparticles were prepared by emulsification crosslinking method in a W/O emulsion system, using cinnamaldehyde as crosslinking agent. The characterisation of the nanoparticles was confirmed by FTIR, TEM and Zeta potential. The loading efficiency, encapsulation efficiency, cytotoxicity of blank and baicalein loaded nanoparticles and in vitro drug release profile has also been carried out. Results The mean diameter of chitosan nanoparticles decreased with increasing the pH value of the reaction mixture. The FTIR result showed the binding of anticancer compound baicalein to the nanoparticles. The TEM image showed that the particles are spherical in nature and average size to be 200nm. Zeta potential revealed negative charge of the particles. Ultraviolet spectrum analysis described higher loading efficiency and encapsulation efficiency as 9.05% and 97.01% respectively, for nanoparticle with 9µg/mL of baicalein. In vitro baicalein release profile revealed the delivery of baicalein from the CS nanoparticles could be separated into two stages initial burst release in the first four days and remaining slow release in the consecutive 15 days. MTT assay showed cell viability up to 61% for 20 µg/mL baicalein loaded nanoparticles. Conclusion The CS nanoparticles and baicalein loaded CS nanoparticles were prepared by emulsification-crosslinking method using cinnamaldehyde as the crosslinking agent. The two step release of baicalein is the major advantage. The apoptosis rate is high because of the synergistic use of two anti-cancer compounds namely baicalein and cinnamaldehyde. The main advantage is this study is high encapsulation efficiency with controlled release of compounds in vitro with minimal side effects.

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