摘要
目的研究经聚乙二醇(PEG)进行表面修饰的端胺基枝状分子(G1.5(NH2)8)作为羟基喜树碱(HCPT)载体的传递系统,对羟基喜树碱的溶解性、释放性能和光敏性等方面的影响。方法用经三氟乙基磺酸单甲氧基(Tresylate)活化的相对分子质量为600的单甲氧基聚乙二醇(Tresylated MPEG-600)对端胺基枝状分子(G1.5(NH2)8)进行修饰,目标产物PEG-600-G1.5(NH2)8枝状大分子用FT-IR、1H NMR进行结构表征。MTT研究其细胞毒性。结果PEG-600-G1.5(NH2)8枝状大分子较之同代G1.5(NH2)8细胞毒指数较低,对HCPT具有更强的增溶作用和更快的释药速度,同时可改善HCPT的光敏性,增加其稳定性。结论G1.5(NH2)8枝状大分子作为HCPT载体是一种很有潜力的新型药物传递系统。
Objective To synthesize PEGylated G1.5(NH2)8 and studyits influence on the solubility, release, cytotoxicity and photo sensitivity of hydroxycamptothecin(HCPT).Methods PEGylated poly(ester-amine) dendrimer was prepared by modifying(G1.5(NH2)8) dendrimer with tresylated MPEG-600.The PEGylated poly(ester-amine) dendrimer(MPEG-600-G1.5(NH2)8) was characterized by FT-IR and 1H NMR.The cytotoxicity of the PEGylated poly(ester-amine) dendrimer was tested by MTT.The potential of the PEGylated poly(ester-amine) dendrimer as an anti-tumor drug carrier was evaluated using HCPT as a model drug.Results PEGylated G1.5(NH2)8 dendrimer exhibits a greater drug host, photostability and release capability as well as a lower cytotoxicity in comparison with non-PEGylated G1.5(NH2)8 dendrimer.Conclusion These studies indicated that PEG-600-G1.5(NH2)8 might be a potential carrier of HCPT as a novel drug delivery system.
作者
吁诚铭
张文智
王艾奇
徐冬梅
YU Chengming;ZHANG Wenzhi;WANG Aiqi;XU Dongmei(Huizhou health Vocational College.,Huizhou 516025,China;College of Chemistry,ChemicalEngineering and Materials Science,Soochow University,Suzhou 215123,China)
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2021年第8期777-781,787,共6页
Journal of Shenyang Pharmaceutical University
基金
辽宁省自然科学基金指导计划(20191344)。
关键词
树枝状大分子
药物载体
羟基喜树碱
增溶
光敏性
dendrimers
drug carrier
hydroxycamptothecin(HCPT)
solubilization
photosensitivity
