Abstract

AbstractTo improve the therapeutic efficiency of paclitaxel (PTX) and reduce its toxicity to normal tissues, a novel hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) derivative has been designed and developed. The polymer (bio‐HP‐β‐CD(NAC)‐PLA) is synthesized by modifying HP‐β‐CD with polylactic acid, cysteine, and biotin. Using bio‐HP‐β‐CD(NAC)‐PLA as the carrier, a PTX‐loaded nanoparticulate system is developed by a modified emulsion solvent evaporation method. The optimized drug‐loaded nanoparticles are obtained with a mean diameter of 162.4 nm and drug loading of 16.1%. In vitro drug release study exhibits that PTX is released in a redox‐dependent manner. Cellular uptake study suggests that the bio‐HP‐β‐CD(NAC)‐PLA nanoparticles can be specifically taken up by MCF‐7 cells via the biotin receptor‐mediated endocytosis. In vitro and in vivo anticancer efficacy evaluations demonstrate the superior antitumor activity and negligible toxicity of the PTX‐loaded nanoparticles. It can be concluded that the proposed polymer bio‐HP‐β‐CD(NAC)‐PLA offers a promising drug delivery system for targeted delivery and controlled release of PTX.

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