Application of Biodegradable Nanoparticles in Liver Targeting of Tacrolimus

摘要: Tacrolimus is a potent immunosuppressant used in liver transplantation to avoid graft rejection. has narrow therapeutic index and variable pharmacokinetics, making dose adjustment drug monitoring complicated task. Increasing the occurrence of adverse effects, especially nephrotoxicity are another concerns. In rejection, antigen presentation occurs lymphatics. Therefore, by targeting tacrolimus spleen, survival could be achieved with decrease nephrotoxicity. Poly(lactide) nanoparticles (PLA‐TAC‐NP) were formulated characterized aim spleen therefore decreasing its To evaluate efficiency PLA‐TAC‐NP, rats divided into two groups. They intravenously injected either PLA‐TAC‐NP or free tacrolimus. At assigned time intervals, blood, liver, kidney samples collected from each rat. Drug extraction HPLC analysis tissue distribution consequently prepared PLA‐TAC‐NP. proved their success showing significantly higher amounts compared increased concentration 24 fold 1.94 whereas kidneys decreased 7.12 fold. Transmission electron microscopy (TEM) was examine section, obtained rat that received TEM images showed Kupffer cell sinusoids. promising delivery systems for achieving localized immunosuppression minimizing transplant patients.