Improved oral bioavailability of the anticancer drug catechin using chitosomes: Design, in-vitro appraisal and in-vivo studies

被引:72
作者
Ezzat, Hadeer M. [1 ]
Elnaggar, Yosra S. R. [1 ,2 ]
Abdallah, Ossama Y. [1 ]
机构
[1] Alexandria Univ, Fac Pharm, Dept Pharmaceut, 1 Khartoum Sq,Messalla PO,POB 21521, Alexandria, Egypt
[2] Pharos Univ Alexandria, Fac Pharm & Drug Mfg, Dept Pharmaceut, Alexandria, Egypt
关键词
Chitosomes (CHS); Catechin hydrate; Oral; Digestive stability; Ex vivo permeation; In vivo pharmacokinetics; LIQUID-CRYSTALLINE NANOPARTICLES; BIOPOLYMER-COATED LIPOSOMES; EX-VIVO; DELIVERY-SYSTEMS; HPLC METHOD; BILE-SALTS; BLACK TEA; STABILITY; GREEN; FORMULATION;
D O I
10.1016/j.ijpharm.2019.05.034
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Catechin hydrate is a phytopharmaceutical with promising anticancer effects but poor bioavailability. This study aimed to elaborate catechin loaded chitosan-tethered liposomes (chitosomes) to enhance catechin oral bioavailability. Nanocarriers were optimized via ethanol injection method followed by physicochemical, ex vivo and biological appraisal in male Wistar albino rats. Results demonstrated that chitosomes possessed excellent nanosize of 137 nm, monodispersity (PDI < 0.2) and high Zeta potential of + 36.8 mV. Additionally, chitosomes showed significant improvement in digestive stability against bile salt with enhanced ex-vivo intestinal permeation. Pharmacokinetic studies revealed the significant potential of chitosomes to enhance catechin bioavailability (AUC, Cmax) and sustain its effect (Tmax). In conclusion, elaborated chitosomes are promising nanoplatforms to enhance catechin oral efficacy with lower dose, side effects, administration frequency and higher patient compliance.
引用
收藏
页码:488 / 498
页数:11
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