The effect of umbrella-type branching on the blood circulation and tumor targeting of star-branched PLA-PMPC copolymer micelles

• Published in: Science China. Technological sciences Vol. 64; no. 1; pp. 71 - 82
• Main Authors: Long, LiXia, Cheng, LinJie, Hou, JingJing, Wang, LiMei, Wang, Xu, He, LiGang, Li, SiDi, Zhao, Jin, Hou, Xin, Kang, ChunSheng, Yuan, XuBo
• Format: Journal Article
• Language: English
• Published: Beijing Science China Press 2021; Springer Nature B.V
• Subjects: Blood circulation; Copolymers; Engineering; In vivo methods and tests; Methacryloyloxyethyl phosphorylcholine; Micelles; Polylactic acid; Self-assembly; Tumors; star-branched copolymers; umbrella-type branching; anti-fouling; prolonged circulation
• ISSN: 1674-7321; 1869-1900
• DOI: 10.1007/s11431-020-1645-6

The effect of branching on the blood circulation and tumor targeting of polymer nanovehicles in vivo was investigated in this study. For the purpose, star-branched poly(lactic acid) and poly(2-methacryloyloxyethyl phosphorylcholine) (PLA-PMPC) copolymers with umbrella-type AB 3 , (AB 3 ) 2 , and (AB 3 ) 3 architecture were synthesized by branching at the PLA core. Micelles self-assembled from these copolymers were used to evaluate the effect of core branching on blood circulation and tumor targeting The results showed that branching changed the behavior of polymeric self-assembly in solution, thereby changing the size and surface anti-fouling performance of the polymeric micelles. Moreover, star-branched copolymer micelles with a higher branching degree allowed their payload to persist better in blood (half-time prolonged from 7.1, 8.6 to 13.8 h) and for a 1.72-fold higher content at the tumor site. These studies suggest that raising the branching degree of amphiphilic copolymer potentially offers a promising strategy for the design of carriers capable of enhanced circulation and targeting in vivo .