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用于透皮给药的载盐酸普萘洛尔脂质体凝胶:表征与体内评价。

Propranolol hydrochloride-loaded liposomal gel for transdermal delivery: Characterization and in vivo evaluation.

作者信息

Guan Yuanyuan, Zuo Tiantian, Chang Minglu, Zhang Fang, Wei Ting, Shao Wei, Lin Guimei

机构信息

School of Pharmaceutical Science, Shandong University, Jinan 250012, China.

School of Pharmaceutical Science, Shandong University, Jinan 250012, China.

出版信息

Int J Pharm. 2015 Jun 20;487(1-2):135-41. doi: 10.1016/j.ijpharm.2015.04.023. Epub 2015 Apr 13.

Abstract

This study was to develop propranolol hydrochloride (PRO)-loaded liposomal gel as a topical drug delivery system. Scanning electron microscope (SEM) revealed that the liposomes were spherical and scattered in the surface of the gel. Pseudoplastic flows of PRO liposomal gel were showed after stored at three different temperatures. Besides, PRO liposomal gel showed non-irritating to the skin of rabbit. Skin deposition studies in vivo demonstrated that PRO liposomal gel can apparently increase drug content in skin compared with PRO gel. Histopathology examination showed that PRO liposomal gel could obviously weaken the barrier function of stratum corneum (SC) by comparison with PRO gel. What is more, the plasma pharmacokinetic showed the maximum concentration in plasma was 0.41 μg/mL and 1.17 μg/mL after topical and oral administration respectively. However, tissue distribution study showed PRO liposomal gel obviously changed drug distribution in tissues, significantly increased drug concentration in skin with about 74 folds compared with PRO gel. In conclusion, liposomes-based gel could be a promising vehicle as a transdermal delivery system of PRO.

摘要

本研究旨在开发一种载有盐酸普萘洛尔(PRO)的脂质体凝胶作为局部给药系统。扫描电子显微镜(SEM)显示脂质体呈球形且分散在凝胶表面。在三种不同温度下储存后,PRO脂质体凝胶呈现假塑性流动。此外,PRO脂质体凝胶对兔皮肤无刺激性。体内皮肤沉积研究表明,与PRO凝胶相比,PRO脂质体凝胶能显著增加皮肤中的药物含量。组织病理学检查显示,与PRO凝胶相比,PRO脂质体凝胶能明显削弱角质层(SC)的屏障功能。此外,血浆药代动力学显示,局部给药和口服给药后血浆中的最大浓度分别为0.41μg/mL和1.17μg/mL。然而,组织分布研究表明,PRO脂质体凝胶明显改变了药物在组织中的分布,与PRO凝胶相比,皮肤中的药物浓度显著增加了约74倍。总之,基于脂质体的凝胶作为PRO的透皮给药系统可能是一种有前景的载体。

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