生物利用度
药理学
体内
壳聚糖
胶束
化学
跨细胞
并行传输
药代动力学
药物输送
药品
前药
口服
医学
水溶液
生物化学
有机化学
生物
生物技术
磁导率
膜
作者
Jie Huang,Xianfeng Tang,Zhendong Yang,Jianqiu Chen,Kun Wang,Chunlei Shi,Zihan Liu,Ming Wu,Qian Du
标识
DOI:10.1016/j.colsurfb.2023.113736
摘要
Irinotecan (CPT-11) is used as a first or second-line chemotherapy drug for the treatment and management of colorectal cancers. In vitro studies have shown that 7-ethyl-10-hydroxycamptothecin (SN38), the active metabolite of CPT-11, displays promising anticancer efficacy. However, its poor aqueous solubility and hydrolytic degradation result in its lower oral bioavailability and impracticable clinical application. To overcome these limitations, a novel amphiphilic chitosan derivative, deoxycholic acid decorated N’-nonyl-trimethyl chitosan, was synthesized. Nano-micelles loaded with SN38 were subsequently prepared to enhance the bioavailability and anti-tumor efficacy of the drug through oral administration. The nano-micelles demonstrated improved dilution stability, enhanced greater mucosal adherence, significant P-gp efflux inhibition, and increased drug transport in the intestine by paracellular and transcellular pathways. Consequently, both the in vivo pharmacokinetic profile and therapeutic efficacy of SN38 against cancer were substantially improved via the micellar system. Thus, the developed polymeric micelles can potentially enhance the SN38 oral absorption for cancer therapy, offering prospective avenues for further exploration.
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