Design and Evaluation of Ophthalmic Thermosensitive In Situ Gel of Compound Salvia

IF 4 4区医学 Q2 PHARMACOLOGY & PHARMACY AAPS PharmSciTech Pub Date : 2024-08-20 DOI:10.1208/s12249-024-02913-8

Yanqiu Long, Fang Lei, Jie Hu, Zhiyun Zheng, Shuangying Gui, Ning He

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Abstract

The compound Salvia Recipe has been shown to have a relatively significant curative effect in management of cardiovascular and cerebrovascular diseases. This work aimed to prepare a thermosensitive in situ gel (ISG) delivery system that utilizes Poloxamer 407, Poloxamer 188, and hydroxypropyl methylcellulose for ocular administration of the compound Salvia recipe to treat cardiovascular and cerebrovascular diseases. The central composite design-response surface method was utilized to improve the prescription of the gel. The formulated gel was characterized and assessed in terms of stability, retention time, in vitro release, rheology, ocular irritation, pharmacokinetics studies, and tissue distribution. The gel was a liquid solution at room temperature and became semisolid at physiological temperature, prolonging its stay time in the eye. Pharmacokinetics and tissue distribution experiments indicated that thermosensitive ISG had enhanced targeting of heart and brain tissues. Additionally, it could lower drug toxicity and side effects in the lungs and kidneys. The compound Salvia ophthalmic thermosensitive ISG is a promising drug delivery system for the management of cardiovascular and cerebrovascular illnesses.

Graphical Abstract

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复方丹参眼科热敏原位凝胶的设计与评估

化合物丹参配方已被证明在治疗心脑血管疾病方面具有较为显著的疗效。本研究旨在利用 Poloxamer 407、Poloxamer 188 和羟丙基甲基纤维素制备一种热敏原位凝胶（ISG）给药系统，用于眼部给药复方丹参配方治疗心脑血管疾病。利用中心复合设计-响应面法改进了凝胶的处方。配制的凝胶在稳定性、保留时间、体外释放、流变学、眼刺激性、药代动力学研究和组织分布等方面进行了表征和评估。凝胶在室温下为液态溶液，在生理温度下变为半固态，延长了在眼内的停留时间。药代动力学和组织分布实验表明，热敏 ISG 对心脏和脑组织的靶向性更强。此外，它还能降低药物在肺部和肾脏的毒性和副作用。复方丹参眼用热敏 ISG 是一种治疗心脑血管疾病的前景看好的给药系统。

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文献相关原料

公司名称

产品信息

阿拉丁

Puerarin

阿拉丁

Formic acid

阿拉丁

Borneol

来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.