期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 424, 期 1-2, 页码 26-32出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2011.12.047
关键词
Nano-aggregates; pH sensitive; Graft copolymers; Release; Paclitaxel
资金
- National Research Foundation of Korea (NRF)
- Korea government (MEST) [2010-0027955]
Polyaspartamide (PASPAM) derivatives grafted with 1-(3-aminopropyl)imidazole (API), O-(2-aminoethyl)-O'-methylpolyethylene glycol (MPEG), and octadecylamine (C18) groups were synthesized and their pH-sensitive structure and Paclitaxel (PTX) load/release properties were investigated. C18/MPEG/API-g-PASPAMs systems synthesized showed a strong pH-dependent phase transition behavior near pH 6.7. Large amount of PTX up to 60-75%, depending on polymer composition, was possibly loaded into the C18/MPEG/API-g-PASPAMs nano-aggregates using a solvent-free protocol. Its pH dependent release pattern was affected correspondingly by the phase transition behavior associated with the composition of graft substituents. The pure C18/MPEG/API-g-PASPAMs systems did not show cell toxicity but the PTX-loaded copolymer systems showed a similar cell toxicity to a Taxol-type PTX. From the in vivo animal study, PTX-loaded nano-aggregates showed the much improved inhibition effect on tumor growth compared to the conventional PTX formulation. (C) 2011 Elsevier B.V. All rights reserved.
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