JI Xiping,LIU Xiaoyan,MENG Xiangfu,et al.Synthesis, micellezation and enzymatic controlled drug release of mPEG-Cys-AFC conjugate[J].Journal of Yanbian University,2016,42(03):207-211，251.
mPEG-Cys-AFC偶联体的合成、胶束化行为及酶促控释研究
- Title:
- Synthesis, micellezation and enzymatic controlled drug release of mPEG-Cys-AFC conjugate
- Keywords:
- drug carrier; amphipathic; micelle; enzymatic controlled release
- 分类号:
- O621.2
- 文献标志码:
- A
- 摘要:
- 选择L-半胱氨酸为中心分子,设计合成了两亲性载体mPEG -Cys-AFC偶联体,其中4-三氟甲基-6-氨基香豆素(AFC)为模型药物.通过1H NMR、13C NMR和MALDI-TOF-MASS对化合物结构进行了表征.采用水溶法制备了胶束,利用芘荧光探针法确定了临界胶束浓度(CMC)为92.8 mg/L,测得胶束的平均粒径为141.1 nm, Zeta电位为-6.11 mV.经测定表明,在PGA酶作用下载体化合物能迅速控释模型药物分子.
- Abstract:
- In this paper, L-cysteine was selected as center molecule, amphiphilic carrier conjugate mPEG -Cys-AFC, and AFC(4-trifluoromethyl-6-amino-coumarin)was designed and synthesized as a model drug. The structure of conjugate was characterized via 1H NMR, 13C NMR and MALDI-TOF-MASS. Micelles were prepared by the solution method, and using Pyrene fluorescence probe method the critical micelle concentration(CMC)was determined as 92.8 mg/L. The particle size of the micelles and Zeta potential were 141.1 nm and -6.11 mV, respectively. The results showed it rapidly controlled and released of a model drug molecule under the influence of PGA enzyme.
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备注/Memo
收稿日期: 2016-06-17*通信作者: 金慧娟(1969—),女,教授,研究方向为有机合成.