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Glycopolymers Made from Polyrotaxanes Terminated with Bile Acids: Preparation, Self‐Assembly, and Targeting Delivery
Author(s) -
Liu Sa,
Jin Jiahong,
Jia YongGuang,
Wang Jin,
Mo Lina,
Chen Xiaohui,
Qi Dawei,
Chen Yunhua,
Ren Li
Publication year - 2019
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201800478
Subject(s) - micelle , ethylene glycol , chemistry , biocompatibility , drug delivery , peg ratio , conjugated system , dynamic light scattering , nanogel , self healing hydrogels , combinatorial chemistry , targeted drug delivery , bioconjugation , nanotechnology , organic chemistry , polymer , aqueous solution , materials science , nanoparticle , finance , economics
The use of natural compounds to construct biomaterials, including delivery system, is an attractive strategy. In the present study, through threading functional α‐cyclodextrins onto the conjugated macromolecules of poly(ethylene glycol) (PEG) and natural compound bile acid, glycopolymers of polyrotaxanes with the active targeting ability are obtained. These glycopolymers self‐assemble into micelles as evidenced by dynamic light scattering and transmission electron microscopy, in which glucosamine, as an example of targeting groups, is introduced. These micelles after loading doxorubicin (DOX) exhibit the selective recognition with cancer cells 4T1. Meanwhile, the maximal half inhibitory concentration is determined to be ≈2.5 mg L −1 for the DOX‐loaded micelles, close to the value of free DOX·HCl (1.9 mg L −1 ). The cumulative release of DOX at pH 5.5 is faster than at pH 7.4, which may be used as the controlled release system. This drug delivery system assembled by glycopolymers features high drug loading of DOX, superior biocompatibility. The strategy not only utilizes the micellization induced by bile acids, but also overcomes the major limitation of PEG such as the lack of targeting groups. In particular, this drug delivery platform can extend to grafting the other targeting groups, rendering this system more versatile.