PEG-derivatized octacosanol as micellar carrier for paclitaxel delivery

International Journal of Pharmaceutics
Bingyang ChuZhiyong Qian

Abstract

In this study, PEG-derivatized octacosanol copolymer was successfully developed to improve the anti-tumor activity and eliminate toxicity of the commercial formulation of paclitaxel (PTX). MPEG2K-C28, the conjugation of monomethoxy Poly(ethylene glycol) 2000 and octacosanol, was readily soluble in aqueous solution and self-assembled to form micelles with small sizes (< 20 nm) that are efficient in encapsulating PTX with a drug loading of 9.38 ± 0.18% and an encapsulation efficiency of 93.90 ± 2.12%. Meanwhile, octacosanol is very safe for humans and amazingly exhibits antitumor activity through inhibition activity of matrix metalloproteinases (MMPs) and translocation of the transcription factor (nuclear factor-kappa B, NF-κB) to the nucleus, which may be able to promote synergistic effects with PTX. A sustained and slower in vitro release behavior was observed in the (PTX micelles) than that of Taxol. PTX micelles exhibited more potent cytotoxicity than Taxol in the 4T1 breast cancer cell line. More interestingly, MPEG2K-C28 selectively inhibited the growth of 4T1 cells rather than the normal cells (HEK293 and L929 cell lines), indicating the antitumor activity of octacosanol remained after conjugation with MPEG. Acute toxicity...Continue Reading

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Citations

Oct 25, 2016·International Journal of Pharmaceutics·Bingyang ChuXiuhua Zhang
Apr 21, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Meishan ChenJianxun Ding
Nov 13, 2019·International Journal of Pharmaceutics·Yao XiongShiyong Song
Dec 10, 2020·International Journal of Nanomedicine·Ze-Liang WuRong Xu
May 5, 2021·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Yi ZhangWenyuan Gao

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