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基于溶致液晶@硬胶囊的智能相变系统,用于控制亲水性和疏水性药物的释放。

Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs.

机构信息

School of Pharmaceutical Science, Jinan University, Guangzhou, PR China.

School of Pharmaceutical Science, Sun Yat-Sen University, Guangzhou, PR China.

出版信息

Drug Deliv. 2020 Dec;27(1):449-459. doi: 10.1080/10717544.2020.1736210.

Abstract

Smart phase transformation systems@hard capsule (SPTS@hard capsule) based on lyotropic liquid crystalline (LLC) were developed for oral sustained release in this study. Doxycycline hydrochloride (DOXY) and meloxicam (MLX) were used as hydrophilic and hydrophobic model drug, respectively. Two systems were added with different additives, that is, gelucire 39/01, PEG 1000 and Tween 80 to adjust their melting point and release profiles. The phase transformation of these systems could be triggered by water as well as temperature. They could spontaneously transform into cubic phase or hexagonal phase when coming across with water, to achieve the 24 h sustained release profile. In addition, the obtained systems could switch between semisolid state and liquid state when temperature changed within room temperature and body temperature, which facilitated the phase transformation in gastrointestinal tract and during their encapsulation into hard capsules. LLC-based SPTS@hard capsule revealed potential for the industrialization of its oral administration on account of its drugs accommodation with different solubility, controllable release profile and simple preparation process.

摘要

本研究开发了基于溶致液晶(LLC)的智能相变系统@硬胶囊(SPTS@硬胶囊),用于口服缓释。盐酸多西环素(DOXY)和美洛昔康(MLX)分别用作亲水性和疏水性模型药物。两个系统添加了不同的添加剂,即 Gelucire 39/01、PEG 1000 和 Tween 80,以调整其熔点和释放曲线。这些系统的相变可以由水和温度触发。当遇到水时,它们可以自发地转化为立方相或六方相,从而实现 24 小时持续释放曲线。此外,所得系统在室温至体温范围内的温度变化时,可以在半固态和液态之间切换,这有利于在胃肠道内进行相变,以及在将其封装到硬胶囊中时进行相变。基于 LLC 的 SPTS@硬胶囊由于其能够容纳不同溶解度的药物、可控的释放曲线和简单的制备工艺,因此具有口服给药产业化的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4513/7144316/ad3af6d71ee1/IDRD_A_1736210_F0001_C.jpg

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