Insight into the in vivo fate of intravenous herpetrione amorphous nanosuspensions by aggregation-caused quenching probes

作     者：Lingyu Hang Chengying Shen Baode Shen Hailong Yuan Lingyu Hang;Chengying Shen;Baode Shen;Hailong Yuan

作者机构：Department of PharmacyAir Force Medical CenterPLABeijing 100142China College of PharmacyJiangxi University of Chinese MedicineNanchang 330004China Department of PharmacyJiangxi Provincial People's HospitalNanchang 330006China 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2022年第33卷第11期

页      面：4948-4951页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 07[理学] 070205[理学-凝聚态物理] 0703[理学-化学] 0702[理学-物理学] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(Nos.81873092 81573697 82174074 81803741)。 

主　　题：Amorphous nanosuspensions Herpetrione In vivo fate Intravenous delivery Aggregation-caused quenching 

摘      要：Intravenous nanosuspensions are attracted growing attention as a viable strategy for development of intravenous formulations of poorly water-soluble drugs.However,only few information about the biological fate of intravenous nanosuspensions is currently known,especially amorphous nanosuspensions are not reported yet.In this study,the in vivo fate of herpetrione(HPE)amorphous nanosuspensions following intravenous administration was explored by using an aggregation-caused quenching(ACQ)probe and HPLC methods.The ACQ probe is physically embedded into HPE nanoparticles via anti-solvent method to form HPE hybrid nanosuspensions(HPE-HNSs)for bioimaging.HPE-HNSs emit strong and stable fluorescence,but fluorescence quenches immediately upon the dissolution of HPE-HNSs,confirming the selfdiscrimination of HPE-HNSs.Following intravenous administration of HPE-HNSs,integral HPE-HNSs and HPE show similar degradation and biodistribution,with rapid clearance from blood circulation and obvious accumulation in liver and lung.Due to the slower dissolution and enhanced recognition by reticuloendothelial system,450 nm HPE-HNSs accumulate more in liver,lung and spleen than that of 200 nm HPE-HNSs.These results demonstrate that integral HPE-HNSs determine the in vivo performance of HPEHNSs.This study provides insight into the in vivo fate of intravenous amorphous nanosuspensions.