title: The aspect ratio effect of drug nanocrystals on cellular internalization efficiency, uptake mechanisms, and in vitro and in vivo anticancer efficiencies.
abstract: In this paper, we investigated the aspect ratio (AR) effect of anticancer drug nanocrystals (NCs) on their cellular internalization efficiency, uptake mechanisms, biodistributions as well as in vitro and in vivo antitumor efficiencies. Both confocal imaging and flow cytometry show that shorter NCs with AR = 1.3 have a much faster cellular uptake rate and a much higher anticancer efficacy than longer NCs. All NCs with different ARs were found to enter the cells via an energy-dependent clathrin-mediated pathway. In vivo experiments indicate that NCs with higher ARs have a shorter half-life and are more easily captured by the liver, while the corresponding tumor uptake decreased. We also observed that NCs with the smallest AR have the highest therapeutic efficacy with appreciably less weight loss. These results would assist in the future design of drug NCs and may lead to the development of new drug nanostructures for biomedical applications.
authors: Functional Nano & Soft Materials Laboratory (FUNSOM) and Collaborative Innovation Center of Suzhou Nano Science and Technology Jiangsu Key Laboratory for Carbon-Based Functional Materials & Devices, Soochow University, Suzhou, Jiangsu 215123, China. xjzhang@suda.edu.cn xiaohong_zhang@suda.edu.cn.
authors: Baishun
authors: B
authors: Tian
authors: Xiujuan
authors: X
authors: Zhang
authors: Caitong
authors: C
authors: Yu
authors: Mengjiao
authors: M
authors: Zhou
authors: Xiaohong
authors: X
authors: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D002166:Camptothecin / Q000031:analogs & derivatives / Q000737:chemistry; D004337:Drug Carriers; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008099:Liver / Q000187:drug effects; D051379:Mice; D008807:Mice, Inbred BALB C; D018613:Microscopy, Confocal; D050997:Nanomedicine / Q000379:methods*; D053758:Nanoparticles / Q000737:chemistry*; D009368:Neoplasm Transplantation; D009369:Neoplasms / Q000378:metabolism; D011092:Polyethylene Glycols / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D011092:Polyethylene Glycols; C028098:10-hydroxycamptothecin; D002166:Camptothecin