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首页> 外文期刊>European journal of pharmaceutical sciences >Cationic nanoemulsions with prolonged retention time as promising carriers for ophthalmic delivery of tacrolimus
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Cationic nanoemulsions with prolonged retention time as promising carriers for ophthalmic delivery of tacrolimus

机译：具有延长保留时间的阳离子纳米乳液作为达克兰血症的眼科递送的承诺载体

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Tacrolimus, also known as FK506, is a first-line drug for the topical treatment of immune-mediated inflammatory anterior ocular diseases (IIAODs). However, due to its limited water solubility, hydrophobic nature and relatively high molecular weight, topical application of FK506 features poor bioavailability. Numbers of formulations have been attempted to enhance the erratic bioavailability of FK506 through various techniques. But until now, none of them could satisfy the clinical needs completely. Here, a novel formulation of FK506, FK506-loaded cationic nanoemulsions (FK506 CNE), was developed to prolong the precorneal residence time of FK506, thereby enhancing the bioavailability of FK506 for IIAODs therapy. FK506 CNE was prepared by high-pressure homogenization, and its composition was screened and optimized by single-factor experiments. The FK506 CNE showed spherical morphology with a mean diameter of 178.8 +/- 2.7 nm and a zeta potential of + 25.6 +/- 0.6 mV. Results from in vivo gamma scintigraphy studies proved that the precorneal residence time of FK506 CNE was significantly increased, compared with FK506-loaded neutral nanoemulsions (FK506 NE) and saline. The data of aqueous humor pharmacokinetic study in rabbits showed that the relative bioavailability of FK506 CNE was 1.68-fold and 1.77-fold of FK506 NE and the marketed FK506 eye drops (Talymus (R)), respectively. Finally, hematoxylin and eosin staining images and in vitro cytotoxicity data confirmed the safety of the FK506 CNE. Taking all these into consideration, we propose that FK506 CNE is a promising topical ophthalmic nanoformulation for the management of IIAODs.
机译：Tacrolimus，也称为FK506，是一种用于局部治疗免疫介导的炎症前眼疾病（IIAODS）的一线药物。然而，由于其有限的水溶性，疏水性和相对高的分子量，FK506的局部应用具有差的生物利用度。已经尝试通过各种技术提高FK506的不稳定生物利用度。但到目前为止，他们都不能完全满足临床需求。这里，开发了FK506，FK506负载阳离子纳米乳液（FK506 CNE）的新型制剂，以延长FK506的前甲型停留时间，从而提高FK506的生物利用度进行IIAODS治疗。通过高压均化制备FK506 CNE，通过单因素实验筛选和优化其组合物。 FK506 CNE显示出球形形态，平均直径为178.8 +/- 2.7 nm，Zeta电位为+ 25.6 +/- 0.6 mV。在Vivo Gamma Scintigraphy研究中的结果证明，与FK506负载中性纳米乳液（FK506 Ne）和盐水相比，FK506 CNE的预征障时间明显增加。兔子中湿气药代动力学研究的数据表明，FK506 CNE的相对生物利用度分别为1.68倍和1.77倍的FK506 NE和市场FK506滴眼液（Talymus（R））。最后，苏木精和曙红染色图像和体外细胞毒性数据证实了FK506 CNE的安全性。考虑所有这些，我们建议FK506 CNE是一个有前途的局部眼科纳米型，用于管理IIAODS。

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    Zhang Jialiang; Liu Zhihong; Tao Chun; Lin Xin; Zhang Minxin; Zeng Lingjun; Chen Xu; Song Hongtao;

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    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

    Xiamen Univ Dong Fang Hosp Hosp Joint Logist Team 900 Dept Pharm Sch Med Fuzhou 350025 Peoples;

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  • 正文语种 eng
  • 中图分类 药学;
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