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

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

doi:10.1007/s10118-021-2547-6

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

ARTICLE | Updated：2021-05-13

- Functional Amphiphilic Poly(2-oxazoline) Block Copolymers as Drug Carriers: the Relationship between Structure and Drug Loading Capacity
- Chinese Journal of Polymer Science Vol. 39, Issue 7, Pages: 865-873(2021)
- Affiliations：
  
  a.College of Chemistry, Northeast Normal University, Changchun 130024, China
  b.Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China
- Author bio：
  
  dengmx330@nenu.edu.cn (M.X.D.)
  wtsong@ciac.ac.cn (W.T.S.)
- Funds：
- DOI：10.1007/s10118-021-2547-6
  CLC：
- Received：14 November 2020，
  
  Revised：2020-12-22，
  
  Accepted：04 January 2021，
  
  Online First：13 May 2021，
  
  Published：14 May 2021
- Accepted：
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Dong, S.; Ma, S.; Liu, Z. L.; Ma, L. L.; Zhang, Y.; Tang, Z. H.; Deng, M. X.; Song, W. T. Functional amphiphilic poly(2-oxazoline) block copolymers as drug carriers: the relationship between structure and drug loading capacity. Chinese J. Polym. Sci. 2021, 39, 865–873

Si Dong, Sheng Ma, Zhi-Lin Liu, et al. Functional Amphiphilic Poly(2-oxazoline) Block Copolymers as Drug Carriers: the Relationship between Structure and Drug Loading Capacity[J]. Chinese Journal of Polymer Science, 2021, 39(7): 865-873.
Dong, S.; Ma, S.; Liu, Z. L.; Ma, L. L.; Zhang, Y.; Tang, Z. H.; Deng, M. X.; Song, W. T. Functional amphiphilic poly(2-oxazoline) block copolymers as drug carriers: the relationship between structure and drug loading capacity. Chinese J. Polym. Sci. 2021, 39, 865–873 DOI： 10.1007/s10118-021-2547-6.

Si Dong, Sheng Ma, Zhi-Lin Liu, et al. Functional Amphiphilic Poly(2-oxazoline) Block Copolymers as Drug Carriers: the Relationship between Structure and Drug Loading Capacity[J]. Chinese Journal of Polymer Science, 2021, 39(7): 865-873. DOI： 10.1007/s10118-021-2547-6.

摘要

Abstract

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-

-2-butenyl-2-oxazoline) (PMeOx-P(

BuOx-

-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

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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references

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