Bovine serum albumin nanoparticles for delivery of tacrolimus to reduce its kidney uptake and functional nephrotoxicity

被引：43

作者：

Zhao, Lei ^{[1
]}

Zhou, Yanxia ^{[1
]}

Gao, Yajie ^{[1
]}

Ma, Shujin ^{[1
]}

Zhang, Chao ^{[1
]}

Li, Jinwen ^{[1
]}

Wang, Dishi ^{[1
]}

Li, Xueping ^{[1
]}

Li, Chengwei ^{[1
]}

Liu, Yan ^{[1
]}

Li, Xinru ^{[1
]}

机构：

[1] Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2015年 / 483卷 / 1-2期

基金：

中国国家自然科学基金;

关键词：

Tacrolimus; Bovine serum albumin nanoparticles; Pharmacokinetics; Nephrotoxicity; Tissue distribution; DRUG-DELIVERY; LIVER-TRANSPLANTATION; IN-VITRO; ORGAN-TRANSPLANTATION; ANTICANCER DRUG; PHARMACOKINETICS; FK506; CYCLOSPORINE; SYSTEMS; RELEASE;

D O I：

10.1016/j.ijpharm.2015.02.018

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The purpose of the present study was to develop a new nanoparticulate formulation for delivery of tacrolimus to reduce its kidney distribution and functional nephrotoxicity. Tacrolimus (TAC)-loaded bovine serum albumin (BSA) nanoparticles (TAC-BSA-NPs) were prepared by emulsification-dispersion technique. The obtained TAC-BSA-NPs, with 189.50 +/- 7.15 nm of diameter and -20.86 +/- 0.45 mV of Zeta potential determined by DLS, were spherical in shape observed by TEM. The drug loading content and encapsulation efficiency were (1.7 +/- 0.13)% and (85 +/- 3.0)%, respectively. The in vitro release of TAC-BSA-NPs exhibited biphasic drug release pattern with an initial burst release and subsequently sustained release. Pharmacokinetic analysis displayed that TAC-BSA-NPs could enhance the drug blood level and prolong the circulation time in comparison to Prograf (R). Meanwhile, compared with Prograf (R), TAC-BSA-NPs could deliver less TAC to kidney and simultaneously reduce the functional nephrotoxicity of TAC to kidney. In conclusion, BSA nanoparticles might be a more safe carrier for delivery of hydrophobic drug TAC. (C) 2015 Elsevier B.V. All rights reserved.

引用

页码：180 / 187

页数：8

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