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首页> 外文期刊>RSC Advances >Cyclosporine A loaded self-nanoemulsifying drug delivery system (SNEDDS): implication of a functional excipient based co-encapsulation strategy on oral bioavailability and nephrotoxicity
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Cyclosporine A loaded self-nanoemulsifying drug delivery system (SNEDDS): implication of a functional excipient based co-encapsulation strategy on oral bioavailability and nephrotoxicity

机译：环孢菌素A负载的自纳乳化药物递送系统（SNEDDS）：对口腔生物利用度和肾毒性的官能赋形剂的共封装策略的影响

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摘要

The present work focusses on the formulation development and evaluation of a functional excipient (surfactant stabilizer), a vitamin E TPGS loaded self-nanoemulsifying drug delivery system (SNEDDS), for improving the deliverability and safety profile of cyclosporine A (CyA). The saturation solubility of individual bioactive compounds were evaluated in a series of oils and surfactants. In addition, a ternary phase diagram-based exhaustive optimization was performed to identify the nanoemulsification region that yields the desired quality of attributes and maximum loading capacity of CyA and vitamin E TPGS. The optimized formulation exhibited excellent stability in simulated gastrointestinal fluids. In vitro drug release studies revealed significantly higher rapid release of CyA from CyA-TPGS SNEDDS as compared to that of the clinically available counterpart Bioral (R) or in-house CyA-SNEDDS. In vivo pharmacokinetics further demonstrated a 4.48-fold increase in oral bioavailability in the case of the developed formulation as compared to Bioral (R). CyA induced reactive oxygen species (ROS) generation in HEK cell lines was significantly diminished in the case of CyA-TPGS SNEDDS in contrast to that of CyA SNEDDS, Bioral (R) and the CyA + vitamin E TPGS physical mixture. The results were further corroborated by in vivo nephrotoxicity studies wherein the levels of biochemical markers of nephrotoxicity, blood urea nitrogen and serum creatinine levels were comparable to that of a negative control in the case of the developed formulation in contrast to that of Bioral (R). In a /nutshell, the employed strategy of functional excipient loaded SNEDDS poses a viable strategy for developing value-added nanoformulations of CyA.
机译：本作本作对功能性赋形剂（表面活性剂稳定剂）的配方开发和评价，一种维生素E TPGS负载自纳中乳化药物递送系统（SNEDDS），用于改善环孢菌素A（CyA）的可递送和安全性。在一系列油和表面活性剂中评价单个生物活性化合物的饱和溶解度。此外，进行三元相图的详尽优化以鉴定纳米乳化区，从而产生所需的属性质量和CyA和维生素E TPG的最大负载能力。优化的制剂在模拟胃肠液中表现出优异的稳定性。体外药物释放研究显示，与临床上的对应物（R）或内部Cya-SnEdds相比，来自Cya-TPGS Snedds的CyA快速释放显着升高。体内药代动力学进一步证明，与偏振（R）相比，在发育配方的情况下，口服生物利用度的增加4.48倍。在与Cya-TPGS的情况下，与Cya-TPGS，嗜酸剂（R）和CyA +维生素E TPGS物理混合物相反，Cya诱导的HEK细胞系中的活性氧（ROS）产生显着降低。通过体内肾毒性研究进一步证实了结果，其中肾毒性的生化标志物，血尿尿素氮和血清肌酐水平的水平与发育制剂的情况相比，与嗜虫（R）相反，相反。在A / NUTSHELL中，采用的功能赋形剂加载的SNEDDS策略造成了用于开发CYA的增值纳米植物的可行策略。

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  • 来源
    《RSC Advances》 |2015年第61期|共10页
  • 作者

    Jain Sanyog; Kambam Sindhu; Thanki Kaushik; Jain Amit K.;

  • 作者单位

    NIPER Ctr Pharmaceut Nanotechnol Dept Pharmaceut Mohali 160062 Punjab India;

    NIPER Ctr Pharmaceut Nanotechnol Dept Pharmaceut Mohali 160062 Punjab India;

    NIPER Ctr Pharmaceut Nanotechnol Dept Pharmaceut Mohali 160062 Punjab India;

    NIPER Ctr Pharmaceut Nanotechnol Dept Pharmaceut Mohali 160062 Punjab India;

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  • 正文语种 eng
  • 中图分类 化学;
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