Control morphology and drug release of nanodrugs through templated crystallization of poorly water-soluble compounds

本研究的目的是利用伊立替康的活性代谢物SN-38作为DNA拓扑异构酶i的有效抑制剂，通过模板结晶法设计和制备无载体纳米药物。本研究选择SN-38的几个衍生物作为抗癌部分，并选择约10 nm的Au簇作为模板。采用再沉淀法制备纳米药物。通过调整再沉淀条件，成功制备了不同尺寸的Au/SN38-Chol纳米粒子。紫外可见光谱在550 nm处证实了金在纳米药物中的存在。结果表明，金表面的亲水性影响了杂化纳米药物的形成率。

The purpose of this research is to design and fabricate a carrier-free nanodrug via templated-crystallization method using SN-38, the active metabolite of irinotecan, acts as a potent inhibitor of DNA topoisomerase I. In this work, several derivatives of SN-38 were selected as the anticancer moiety, and Au cluster of ca. 10 nm was selected as a template. The nanodrugs are fabricated by reprecipitation method. The modified Au/SN38-Chol nanoparticles were successfully fabricated in several sizes by adjusting the reprecipitation conditions. The existence of Au in the nanodrugs was confirmed in the UV-Vis spectra with visible absorbance at ca. 550 nm. The formation yield of the hybrid nanodrugs were suggested to be affected by the hydrophilicity of Au surface.