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Carbohydr Polym ; 269: 118327, 2021 Oct 01.
Article in English | MEDLINE | ID: mdl-34294339

ABSTRACT

In this study, a novel polymer based on aggregation-induced emission (AIE) fluorogen, biotin and disulfide bonds modified chitosan (TPE-bi(SS-CS-Bio)) was designed and synthesized. The polymer could self-assemble into micelles in aqueous media and encapsulate paclitaxel (PTX) into the core with high drug loading. Fluorescence study indicated that the micelles exhibited excellent AIE feature with intense blue fluorescence emitted. In vitro drug release study indicated that the micelles could disassemble rapidly in the presence of high level of glutathione. The modification by biotin could enhance the cellular uptake of the micelles. The drug-loaded micelles possessed remarkable cytotoxicity against MCF-7 cells, and their distribution in the cells could be traced due to the excellent AIE feature. In vivo antitumor efficacy study demonstrated the superior antitumor activity of the PTX-loaded TPE-bi(SS-CS-Bio) micelles. These results indicated that TPE-bi(SS-CS-Bio) has the ability of biological imaging and can be used as a potential carrier for PTX.


Subject(s)
Antineoplastic Agents/therapeutic use , Chitosan/analogs & derivatives , Drug Carriers/chemistry , Fluorescent Dyes/chemistry , Micelles , Neoplasms/drug therapy , Paclitaxel/therapeutic use , Animals , Antineoplastic Agents/pharmacology , Carbohydrate Sequence , Cell Line, Tumor , Chitosan/chemical synthesis , Drug Carriers/chemical synthesis , Drug Liberation , Female , Fluorescent Dyes/chemical synthesis , Humans , Mice , Neoplasms/diagnostic imaging , Neoplasms/pathology , Paclitaxel/pharmacology
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