利拉利汀缓释微粒凝胶透皮给药系统:体外表征和体内评估。

Jiayan Liu, Song Guo, Shuai Hong, Jingshu Piao, Mingguan Piao
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引用次数: 0

摘要

背景:利拉利汀(LNG)生物利用度低,副作用多,严重限制了其使用。透皮给药系统(TDDS)为克服与口服制剂相关的首过效应和胃肠道反应提供了一种潜在的解决方案:本研究旨在开发 LNG 微颗粒凝胶,以提高药物的生物利用度并减轻副作用:方法:采用喷雾干燥法制备了利拉利汀透明质酸(LNG-HA)微颗粒,并通过单因素法对其配方进行了优化。采用浆液法研究了其溶解度和释放度。制备了 LNG-HA 微颗粒凝胶,并通过体外透皮试验对其进行了优化。在糖尿病小鼠身上检测了 LNG-HA 微颗粒凝胶的降血糖效果:结果:结果表明,LNG-HA 微颗粒的包封率为 84.46%。微颗粒凝胶选择了卡波姆作为凝胶基质。与口服原料药相比,微颗粒凝胶制剂表现出明显的双相释放模式。在最初的 30 分钟内,只有 43.56% 的药物被释放,随后药物逐渐释放。这表明该制剂实现了双储层系统的缓释效果。此外,药效学研究表明,液化天然气微粒凝胶配方的持续降糖效果可持续 48 小时:这些研究结果表明,液化天然气微颗粒凝胶在提供持续释放方面具有重要的临床价值,并证明了其实际应用的合理性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: In vitro Characterization and In vivo Evaluation.

Background: Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.

Objective: The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.

Methods: Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.

Results: The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.

Conclusion: These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.

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