Insights into the Mechanism of Bile Salt Aggregates Forming in a PEGylated Amphiphilic Polymer/Bile Salt Mixed Micelle
Qinggang Tan; Min Bie; Zihao Wang; Yanyan Chu; Susu Tao; Xiaoyan Xu; Yingbin Liu
Index: 10.1002/slct.201800382
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Abstract
Tailoring the structure of core‐shell interface of amphiphilic copolymer micelles provides a potential to mediate the drug release from micelles. Here, bile salts were used to alter the molecular geometry of core‐shell structured amphiphilic copolymer micelles. With the different sodium deoxycholate (NaDC) addtions in the methoxy polyethylene glycol‐poly(D,L‐lactic acid) (MPEG‐PDLLA) solutions, the NaDC molecule could form different deoxycholic acid (DCA) dimers in the core and shell of micelles. A face‐to‐face DCA dimer structure could form and insert into the core of micelles when a small NaDC addition. This dimer could accelerate the drug release. At a high NaDC addition, a new back‐to‐back DCA dimer could form in the PEG shell region that would reduce the rate of drug release. The results obtained provide fundamental insights into the role of bile salts in adjusting the drug release of amphiphilic copolymer micelles and demonstrate the future potential for controlled drug‐delivery applications.