State Key Laboratory for Physical Chemistry of Solid Surfaces, iChEM (Collaborative Innovation Center of Chemistry for Energy Materials), Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, China.
State Key Laboratory for Physical Chemistry of Solid Surfaces, iChEM (Collaborative Innovation Center of Chemistry for Energy Materials), Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, China.
Colloids Surf B Biointerfaces. 2017 Nov 1;159:613-619. doi: 10.1016/j.colsurfb.2017.08.007. Epub 2017 Aug 5.
Fullerenes with novel structures find numerous potential applications, particularly in the fields of biology and pharmaceutics. Among various fullerene derivatives, those exhibiting amphiphilic character and capable of self-assembly into vesicles are particularly interesting, being suitable for delayed drug release. Herein, we report the synthesis and self-assembly of biocompatible hollow nanovesicles with bilayer shells from amphiphilic functionalized fullerenes CRCl (R=methyl ester of 4-aminobutyric/glutamic acid or phenylalanine). The thus prepared vesicles exhibit sizes of 80-135nm (depending on R) and can be used as delayed-release carriers of anti-cancer drugs such as 5-fluorouracil, cyclophosphamide, and cisplatin, with the time of 5-fluorouracil release from drug-containing vesicles exceeding that of non-encapsulated forms by a factor of three. We further reveal the effect of R on the loading amount and release rate/amount of vesicle-encapsulated drugs, demonstrating a potential pharmaceutical application of the prepared nanovesicles depending on the nature of R.
具有新颖结构的富勒烯具有众多潜在的应用，特别是在生物学和药物学领域。在各种富勒烯衍生物中，那些具有两亲性并能够自组装成囊泡的衍生物特别有趣，适合于延迟药物释放。在此，我们报告了由两亲性功能化富勒烯 CRCl（R=4-氨基丁酸/谷氨酸或苯丙氨酸的甲酯）合成和自组装具有双层壳的生物相容性中空纳米囊泡。所制备的囊泡的粒径为 80-135nm（取决于 R），可作为抗癌药物如 5-氟尿嘧啶、环磷酰胺和顺铂的延迟释放载体，载药囊泡中 5-氟尿嘧啶的释放时间比未包封形式延长了三倍。我们进一步揭示了 R 对囊泡包封药物的载药量和释放率/量的影响，表明根据 R 的性质，所制备的纳米囊泡具有潜在的药物应用前景。
