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

作　　者：Si Dong Sheng Ma Zhi-Lin Liu Li-Li Ma Yu Zhang Zhao-Hui Tang Ming-Xiao Deng Wan-Tong Song 

机构地区：[1]College of Chemistry,Northeast Normal University,Changchun 130024,China [2]Key Laboratory of Polymer Ecomaterials,Changchun Institute of Applied Chemistry,Chinese Academy of Sciences,Changchun 130022,China

出　　处：《Chinese Journal of Polymer Science》2021年第7期865-873,共9页高分子科学（英文版）

基　　金：the National Natural Science Foundation of China(Nos.51673185,51973215,51673189,51829302,52003268 and 52025035);as well as the support from the Youth Innovation Promotion Association of Chinese Academy of Sciences(No.2020232).

摘　　要：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-buty1-2-oxazoline-co-2-buteny1-2-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,n-n 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.

关 键 词：Poly(2-oxaozoline) Polymeric micelles Drug loading π-πInteraction Electrostatic interaction 

分 类 号：TQ317[化学工程—高聚物工业] TQ460.4