title: Bovine serum albumin nanoparticles for delivery of tacrolimus to reduce its kidney uptake and functional nephrotoxicity.
abstract: 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(®). Meanwhile, compared with Prograf(®), 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.
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Lei
authors: L
authors: Zhao
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Yanxia
authors: Y
authors: Zhou
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Yajie
authors: Y
authors: Gao
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Shujin
authors: S
authors: Ma
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Chao
authors: C
authors: Zhang
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Jinwen
authors: J
authors: Li
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Dishi
authors: D
authors: Wang
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Xueping
authors: X
authors: Li
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Chengwei
authors: C
authors: Li
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: yanliu@bjmu.edu.cn.
authors: Yan
authors: Y
authors: Liu
authors: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: ll@bjmu.edu.cn.
authors: Xinru
authors: X
authors: Li
mesh_terms: D000818:Animals; D002417:Cattle; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D007668:Kidney / Q000187:drug effects* / Q000503:physiopathology; D008297:Male; D008968:Molecular Conformation; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012710:Serum Albumin, Bovine / Q000737:chemistry*; D016559:Tacrolimus / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity*; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D012710:Serum Albumin, Bovine; D016559:Tacrolimus
keywords: Bovine serum albumin nanoparticles; Nephrotoxicity; Pharmacokinetics; Tacrolimus; Tissue distribution