聚合物贴片和固体微针的组合方法改善缬沙坦的透皮给药:概念验证研究

Q3 Biochemistry, Genetics and Molecular Biology

Biointerface Research in Applied Chemistry Pub Date : 2022-09-11 DOI:10.33263/briac134.314

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引用次数: 1

摘要

缬沙坦（VALS）是治疗高血压的一线药物，属于血管紧张素II受体阻滞剂类。VALS目前是口服给药，但其生物利用度低。透皮途径可以是克服这个问题的一种替代方法。然而，由于皮肤上存在角质层，这种途径具有低渗透性。需要使用渗透促进剂。本研究旨在确定PEG400浓度对VALS经皮贴剂物理特性和释放的影响，并确定固体微针对VALS渗透的影响。使用HPMC作为基质和PEG 400作为不同浓度的渗透促进剂制备透皮贴剂配方。评估贴片的物理外观、重量均匀性、厚度、水分含量、耐折叠性、药物含量、体外药物释放、体外药物渗透和离体渗透测试。结果表明，所有制剂都表现出良好的透皮给药特性，PEG400的使用可以增加VALS的渗透性。重要的是，当与固体微针结合时，VALS的渗透性显著提高。总之，VALS贴剂透皮和MNs的结合可以增加VALS的渗透量。

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Combinatorial Approach of Polymeric Patches and Solid Microneedles for Improved Transdermal Delivery of Valsartan: A Proof-of-Concept Study

Valsartan (VALS) is a first-line therapy for hypertension that belong to the Angiotensin II Receptor Blockers class. VALS is currently administered orally, but it is associated with its low bioavailability. The transdermal route can be an alternative to overcome this problem. However, this route has low permeation caused by the presence of stratum corneum on the skin. The use of permeation enhancers is needed. This study aims to determine the effect of PEG 400 concentration on physical characteristics and release of VALS from transdermal patch preparations and determine the effect of solid microneedles on VALS permeation. The transdermal patch formula was made using HPMC as a base and PEG 400 as a permeation enhancer with various concentrations. The patches were evaluated for their physical appearance, weight uniformity, thickness, moisture content, folding endurance, drug content, in vitro drug release, in vitro drug permeation, and ex vivo permeation test. The results showed that all formulations showed good characteristics for transdermal administration, and the use of PEG 400 could increase the permeation of VALS. Importantly, when combined with solid microneedles, the permeation of VALS was significantly improved. To conclude, the combination of VALS patch transdermal and MNs can increase the amount of VALS permeated.

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来源期刊

Biointerface Research in Applied Chemistry CHEMISTRY, APPLIED-

CiteScore

4.80

自引率

0.00%

发文量

256

期刊介绍： Biointerface Research in Applied Chemistry is an international and interdisciplinary research journal that focuses on all aspects of nanoscience, bioscience and applied chemistry. Submissions are solicited in all topical areas, ranging from basic aspects of the science materials to practical applications of such materials. With 6 issues per year, the first one published on the 15th of February of 2011, Biointerface Research in Applied Chemistry is an open-access journal, making all research results freely available online. The aim is to publish original papers, short communications as well as review papers highlighting interdisciplinary research, the potential applications of the molecules and materials in the bio-field. Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible.