4.5 Article

Functional Amphiphilic Poly(2-oxazoline) Block Copolymers as Drug Carriers: the Relationship between Structure and Drug Loading Capacity

期刊

CHINESE JOURNAL OF POLYMER SCIENCE
卷 39, 期 7, 页码 865-873

出版社

SPRINGER
DOI: 10.1007/s10118-021-2547-6

关键词

Poly(2-oxaozoline); Polymeric micelles; Drug loading; π -π Interaction; Electrostatic interaction

资金

  1. National Natural Science Foundation of China [51673185, 51973215, 51673189, 51829302, 52003268, 52025035]
  2. Youth Innovation Promotion Association of Chinese Academy of Sciences [2020232]

向作者/读者索取更多资源

Poly(2-oxazoline) (POx) is a type of polymeric amide with promising cyto- and hemo-compatibility, and it can be used as drug carriers. The drug loading capacity (DLC) of POx can be improved by modifying functional groups, and a series of functional POxs provide options for various drug loadings. The encapsulation of drugs with different characteristics can be achieved by selecting suitable functional POxs.
Poly(2-oxazoline) (POx) is a kind of polymeric amides that can be viewed as conformational isomers of polypeptides with excellent cyto- and hemo-compatibility, and is promising to be used as drug carriers. However, the drug loading capacity (DLC) of POx for many drugs is still low except several hydrophobic ones including paclitaxel (PTX). Herein, we prepared a series of amphiphilic POx block copolymers with various functional groups, and investigated the relationship between functional structures and the DLC. Functional POxs with benzyl, carboxyl, and amino groups in the side-chain were synthesized based on a poly(2-methyl-2-oxazoline)-block-poly(2-butyl-2-oxazoline-co-2-butenyl-2-oxazoline) (PMeOx-P(nBuOx-co-ButenOx), PMBEOx) precursor, followed by click reaction between vinyl and the 2-phenylethanethiol, thioglycolic acid and cysteamine. Using thin-film hydration method, eight commonly used drugs with various characteristics were encapsulated within these functional POx polymers. We found that amine-containing drugs were more easily encapsulated by POx with carboxyl groups, while amine functionalities in POx enhanced the loading capacity of drugs with carboxyl groups. In addition, pi-pi interactions resulted in enhanced DLC of most drugs, except several hydrophobic drugs with aromatic to total carbon ratios less than 0.5. In general, we could successfully encapsulate all the selected drugs with a DLC% over 10% using properly selected functional POxs. The above results confirm that the DLC of polymeric carriers can be adjusted by modifying the functional groups, and the prepared series of functional POxs provide an option for various drug loadings.

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