Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM, Jammu campus, Jammu 180001, India.
Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India.
Eur J Pharm Sci. 2018 Mar 1;114:217-227. doi: 10.1016/j.ejps.2017.12.017. Epub 2017 Dec 22.
From the current trends, tacrolimus (TAC) has become an important therapeutic option for the optimal individualization of immunosuppressive therapy especially in case of transplant recipients. TAC is used most frequently in comparison to other immunosuppressants because it offers better safety profile with increased long-term survival in patients especially in children and adolescents. This drug has developed an immense interest in the research field owing to its potential pharmacological scope but due to its poor water solubility, need of concomitant steroids and higher incidences of nephrotoxicity, there comes a need for future research to minimize such limitations and decipher maximum use of the drug. In addition, there are number of formulations attempted to enhance its erratic bioavailability through various techniques namely solid dispersions, inclusion complexes, prodrug approach, SMEDDS etc. The present review aims to acknowledge the TAC pharmacokinetic profile and novel drug delivery systems in multiple diseased conditions by particularly enhancing its poor biopharmaceutical issues as well as dose related toxicity. Collectively, we have updated the data pertaining to the drug delivery prospects of TAC for the period of last 8-10years.
从目前的趋势来看，他克莫司（TAC）已成为免疫抑制治疗个体化的重要治疗选择，特别是在移植受者中。与其他免疫抑制剂相比，TAC 应用最为广泛，因为它在提高患者特别是儿童和青少年的长期生存率方面具有更好的安全性。由于其潜在的药理作用范围，这种药物在研究领域引起了极大的兴趣，但由于其水溶性差、需要同时使用类固醇以及肾毒性发生率较高，因此需要进行未来的研究来最小化这些限制并最大限度地利用这种药物。此外，已经尝试了多种制剂来通过各种技术（例如固体分散体、包合物、前药方法、SMEDDS 等）来提高其不稳定的生物利用度。本综述旨在通过特别改善其较差的生物制药问题以及与剂量相关的毒性，来了解 TAC 在多种疾病状态下的药代动力学特征和新型药物传递系统。总的来说，我们更新了过去 8-10 年 TAC 药物传递前景的数据。
