Functionalized hydroxypropyl-β-cyclodextrin derivative as a versatile nanovehicle for delivery of paclitaxel

To 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. Graphical