A stepwise optimization strategy to formulate in situ gelling formulations comprising fluconazole-hydroxypropyl-beta-cyclodextrin complex loaded niosomal vesicles and Eudragit nanoparticles for enhanced antifungal activity and prolonged ocular delivery

作     者：Heba Elmotasem Ghada E.A.Awad Heba Elmotasem;Ghada E.A.Awad

作者机构：Pharmaceutical Technology DepartmentNational Research CentreCairo 12622Egypt Chemistry of Natural and Microbial Product DepartmentNational Research CentreCairo 12622Egypt 

出 版 物：《Asian Journal of Pharmaceutical Sciences》 (亚洲药物制剂科学（英文）)

年 卷 期：2020年第15卷第5期

页      面：617-636页

核心收录：

学科分类：100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1002[医学-临床医学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：the National Research Centre Cairo Egypt for all the facilities and supports 

主　　题：Fluconazole Ocular Eudragit nanoparticles Cyclodextrin Niosomes In situ gel 

摘      要：Fungal keratitis and endopthalmitis are serious eye ***(FL)is indicated for their treatment,but suffers from poor topical ocular *** study was intended to improve and prolong its ocular *** niosomal vesicles were prepared using span ***,polymeric nanoparticles were prepared using cationic Eudragit RS100 and Eudragit *** investigated particles had adequate entrapment efficiency(EE%),nanoscale particle size and high zeta ***,formulations were optimized using full factorial ***-HP-β-CD complex was encapsulated in selected Eudragit nanoprticles(FL-CD-ERS1)and niosmal *** niosomes were further coated with cationic and bioadhesive chitosan(FL-CD-Nios-ch).EE%for FL-CD-ERS1 and FL-CD-Niosch formulations were 76.4%and 61.7%;particle sizes were 151.1 and 392 nm;also,they exhibited satisfactory zeta potential+40.1 and+28.5 m *** situ gels were prepared by poloxamer P407,HPMC and chitosan and evaluated for gelling capacity,rheological behavior and gelling *** increase the precorneal residence time,free drug and selected nano-formulations were incorporated in the selected in situ *** study revealed sustained release within 24 *** through excised rabbits corneas demonstrated enhanced drug flux and large AUC0-6 h in comparison to plain *** permeation of selected formulations labeled with Rhodamine B was visualized by Confocal laser *** study and in vivo tolerance test evidenced *** vivo susceptibility test using Candida albicans depicted enhanced growth inhibition and sustained *** this study the adopted stepwise optimization strategy combined cylodextrin complexation,drug nano-encapsulation and loading within thermosenstive in situ ***,the developed innovated formulations displayed boosted corneal permeation,enhanced antifungal activity and prolonged action.