用于递送他克莫司以减少其肾脏摄取和功能性肾毒性的牛血清白蛋白纳米颗粒。
Bovine serum albumin nanoparticles for delivery of tacrolimus to reduce its kidney uptake and functional nephrotoxicity.
作者信息
Zhao Lei, Zhou Yanxia, Gao Yajie, Ma Shujin, Zhang Chao, Li Jinwen, Wang Dishi, Li Xueping, Li Chengwei, Liu Yan, Li Xinru
机构信息
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
出版信息
Int J Pharm. 2015 Apr 10;483(1-2):180-7. doi: 10.1016/j.ijpharm.2015.02.018. Epub 2015 Feb 11.
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.
本研究的目的是开发一种用于递送他克莫司的新型纳米颗粒制剂，以减少其在肾脏的分布和功能性肾毒性。通过乳化分散技术制备了负载他克莫司（TAC）的牛血清白蛋白（BSA）纳米颗粒（TAC-BSA-NPs）。通过动态光散射测定，所获得的TAC-BSA-NPs直径为189.50±7.15 nm，Zeta电位为-20.86±0.45 mV，通过透射电子显微镜观察呈球形。药物负载量和包封率分别为（1.7±0.13）%和（85±3.0）%。TAC-BSA-NPs的体外释放呈现双相药物释放模式，先是初始突释，随后是持续释放。药代动力学分析表明，与普乐可复（Prograf®）相比，TAC-BSA-NPs可提高药物血药浓度并延长循环时间。同时，与普乐可复（Prograf®）相比，TAC-BSA-NPs可向肾脏递送更少的TAC，并同时降低TAC对肾脏的功能性肾毒性。总之，BSA纳米颗粒可能是递送疏水性药物TAC的更安全载体。
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