Preparation of Two Types of Polymeric Micelles Based on Polyβ-L-Malic Acid for Antitumor Drug DeliveryReport as inadecuate




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Polymeric micelles represent an effective delivery system for poorly water-soluble anticancer drugs. In this work, two types of CPT-conjugated polymers were synthesized based on polyβ-L-malic acid PMLA derivatives. Folic acid FA was introduced into the polymers as tumor targeting group. The micellization behaviors of these polymers and antitumor activity of different self-assembled micelles were investigated. Results indicate that polyethylene glycol-polyβ-L-malic acid-campotothecin-I PEG-PMLA-CPT-I, P1 is a grafted copolymer, and could form star micelles in aqueous solution with a diameter of about 97 nm, also that PEG-PMLA-CPT-II P2 is an amphiphilic block copolymer, and could form crew cut micelles with a diameter of about 76 nm. Both P1 and P2 micelles could improve the cellular uptake of CPT, especially the FA-modified micelles, while P2 micelles showed higher stability, higher drug loading efficiency, smaller size, and slower drug release rate than that of P1 micelles. These results suggested that the P2 crew cut micelles possess better stability than that of the P1 star micelles and might be a potential drug delivery system for cancer therapy.



Author: Tiehong Yang , Wei Li , Xiao Duan, Lin Zhu, Li Fan, Youbei Qiao, Hong Wu

Source: http://plos.srce.hr/



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