Preparation and physicochemical characterization of camptothecin conjugated poly amino ester-methyl ether poly ethylene glycol copolymer

喜树碱共轭聚氨基酯-甲醚聚乙二醇共聚物的制备及理化表征

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作者:Ali Fattahi, Nadia Karimi, Fatemeh Rahmati, Yalda Shokoohinia, Komail Sadrjavadi

Abstract

In the present study, camptothecin grafted poly amino ester-methyl ether polyethylene glycol (CPT-PEA-MPEG) as a novel copolymer was synthesized by Michael reaction at different ratios of MPEG and CPT (60 : 40 and 80 : 20). The microemulsion was used to prepare nanomicelles, and in vitro cytotoxicity was performed on the HT29 cell line, and cell survival was measured by MTT assay. The syntheses were confirmed by 1H NMR and FT-IR. Several characterization methods including CMC, particle size, size distribution, and transmission electron microscopy were performed to evaluate features of prepared nanomicelles. Low critical micelle concentration, small particle size and IC50 of 0.1 mg ml-1 at MPEG to CPT ratio of 60 : 40 make this micelle a promising drug delivery carrier. CPT-PAE-MPEG nanomicelles at a MPEG : CPT ratio of 60 : 40 can be a suitable choice to improve the physiochemical properties of CPT and its therapeutic effect, while it can be potentially used as a nano-carrier for other anticancer drugs to purpose a dual drug delivery.

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