Fabrication of nanomicelle with enhanced solubility and stability of camptothecin based on alpha,beta-poly[(N-carboxybutyl)-L-aspartamide]-camptothecin conjugate.
This research is aimed to develop a nanomicelle delivery system in order to enhance the solubility and stability of camptothecin (CPT) in aqueous media. In this case, alpha,beta-poly[(N-carboxybutyl)-L-aspartamide] (PBAsp)-CPT was conjugated by the esterification between PBAsp and 20-OH of CPT, and hence used to fabricate nanomicelles with a particle size between the pore size of blood capillary in normal tissue and that in tumor tissue. It was worthy of note that the drug-loaded system of PBAsp-CPT nanomicelle improved the solubility and stability of CPT in aqueous media. However, with an increase of the CPT loading in PBAsp-CPT, the solubility sharply decreased. Meanwhile, the sizes of PBAsp-CPT nanomicelles showed a tendency of increase. Moreover, the drug release of PBAsp-CPT nanomicelles displayed a linear sustaining profile, and hence resulted in the essential decrease of cytotoxicity to L929 cell line. The assembled nanomicelles based on the PBAsp-CPT conjugates showed a great potential as polymer prodrug of tumor therapy, and the controlled nano-scale might achieve the passive tumor targeting.
Fan
Naiqian
N
Institutes for Advanced Interdisciplinary Research, East China Normal University, 3663# North Zhongshan Road, Shanghai 200062, PR China.
Duan
Kongrong
K
Wang
Chengyun
C
Liu
Shunying
S
Luo
Shufang
S
Yu
Jiahui
J
Huang
Jin
J
Li
Yaping
Y
Wang
Daxin
D
D000818:Animals; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008823:Micelles; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D012995:Solubility / Q000187:drug effects; D013056:Spectrophotometry, Ultraviolet; D017550:Spectroscopy, Fourier Transform Infrared
D008823:Micelles; D002166:Camptothecin