1. Fabrication of nanomicelle with enhanced solubility and stability of camptothecin based on alpha,beta-poly[(N-carboxybutyl)-L-aspartamide]-camptothecin conjugate.
- Author
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Fan N, Duan K, Wang C, Liu S, Luo S, Yu J, Huang J, Li Y, and Wang D
- Subjects
- Animals, Camptothecin chemical synthesis, Camptothecin pharmacology, Cell Death drug effects, Cell Line, Cell Survival drug effects, Drug Stability, Hydrogen-Ion Concentration drug effects, Magnetic Resonance Spectroscopy, Mice, Nanostructures ultrastructure, Particle Size, Solubility drug effects, Spectrophotometry, Ultraviolet, Spectroscopy, Fourier Transform Infrared, Camptothecin analogs & derivatives, Camptothecin chemistry, Micelles, Nanostructures chemistry
- Abstract
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.
- Published
- 2010
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