Two pH-sensitive Glycopolymers with the same components but with different construction tailored biotin functionalities were developed for controlled release of bortezomib (BTZ).The initiator brominate biotin and glyco-monomer were synthesized precedently to produce the block-and random-biotinylated poly (2-Gluconamidoethyl methacrylate)-poly (2-Diethylaminoethyl methacrylate) (block/random Biotin-PGAMA-PDEA) via atom transfer radical polymerization (ATRP). The construction and composition of compounds and polymers were characterized by 1H NMR Spectroscopy. The block copolymer self-assembled into micelle according to the pH-response ability of the copolymer while the random one did not under certain conditions.
Detailed studies were performed to probe the effects of the cross-linking layer microstructure of pH-responsive shell cross-linked (SCL) micelles on the loading capacity of doxorubicin (DOX). Well-defined poly [(ethylene glycol)-block-2-(dimethylamino) ethyl methacrylate-block-2-(diethylamino) methacrylate] (PEG-b-P(DMA- co-QDMA)-b-PDEA) copolymer with “clickable” moieties in the middle block by the quaternization with propargyl bromide dissolved molecularly in acidic solution; micellization occurred at alkaline solution to form three-layer “onionlike” micelles constituting PDEA cores, P(DMA-co-QDMA) inner shells, and PEG coronas. Two types of cross-linker bearing azide group: 1,6-bisazidehexane and bis-(azidoethyl) disulfide were utilized to prepare the SCL micelles with different cross-linking layer microstructure via click chemistry at basic aqueous media. The results showed that two types of SCL micelles possessed excellent stability. In neutral solution, these SCL micelles still maintained structural integrity, and the average hydrodynamic diameter of SCL micelles 1 and SCL micelles 2 increased to 80 nm and 90 nm, respectively. In the acidic solution, due to the complete protonated of the PDEA core, the sizes of the two types of SCL micelles increased to 95 nm and 110 nm, respectively, which were favorable for the diffusion of the encapsulated drug in the core. Moreover, the cross-linking degree had no effect on the size of SCL micelles. The loading efficiency and loading content of the SCL micelles were significantly better than those of the uncross-linked micelles, and loading capacity did not vary with degree of cross-linking. However, the SCL micelles 1 demonstrated better loading capacity. This study could be a guidance for the future research on the effects of the cross-linking layer microstructure on controlled doxorubicin release.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.