摘要
Self-assembly is a powerful approach in molecular engineering for biomedical applications,in particu-lar for creating self-assembling prodrugs.Here,we report a self-assembling prodrug of the anticancer drug gemcitabine(Gem)based on amphiphilic dendrimer approach.The prodrug reported in this study demonstrates high drug loading(40%)and robust ability to self-assemble into small nanomicelles,which increase the metabolic stability of Gem and enable entry into cells via endocytosis,hence bypassing transport-mediated uptake.In addition,this prodrug nanosystem exhibited an effective pH-and enzyme-responsive release of Gem,resulting in enhanced anticancer activity and reduced toxicity.Harboring ad-vantageous features of both prodrug-and nanotechnology-based drug delivery,this self-assembling Gem prodrug nanosystem constitutes a promising anticancer candidate.This study also offers new perspectives of the amphiphilic dendrimer nanoplatforms for the development of self-assembling prodrugs.
基金
Financial support was from the National Natural Science Foundation of China (Nos. 81903567, 31600109)
Henan Programs for Science and Technology Development (No. 182102310221)
Xinxiang Innovative Technology Team (No. CXTD17004)
the PhD startup fund of Xinxiang Medical University (No. 505158)
the Ligue Nationale Contre le Cancer