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使用聚合物透皮水凝胶和固体微针的组合方法改善缬沙坦的透皮递送:一项概念验证研究。

Improved transdermal delivery of valsartan using combinatorial approach of polymeric transdermal hydrogels and solid microneedles: an proof of concept investigation.

作者信息

Enggi Cindy Kristina, Satria Mega Tri, Nirmayanti Nirmayanti, Usman Jesscia Theodor, Nur Julika Fajrika, Asri Rangga Meidianto, Djide Nana Juniarti Natsir, Permana Andi Dian

机构信息

Faculty of Pharmacy, Hasanuddin University, Makassar, Indonesia.

出版信息

J Biomater Sci Polym Ed. 2023 Feb;34(3):334-350. doi: 10.1080/09205063.2022.2121590. Epub 2022 Sep 12.

Abstract

Valsartan (VAL) is used as a first-line agent to treat hypertension. However, VAL exhibits poor absorption and low bioavailability when administrated orally. To overcome these issues, VAL transdermal gel was developed in this study, where Carbopol was used as the gel matrices. Additionally, solid microneedles (Dermaroller) with various needle lengths were combined with transdermal gel to improve its permeation across the stratum corneum as a skin barrier. Developed formulations were further evaluated for various parameters, including pH, viscosity, spreadability, extrudability, gel strength, drug content, permeation, release, occlusivity, and hemolysis. The results showed that all formulations exhibited desired physical characteristics without any potential to cause toxicity. Moreover, this approach showed that using microneedles could significantly enhance the permeation of VAL up to 3 folds compared to untreated skin. The use of microneedles 1.5 mm was found to be the optimum combination to improve VA permeation without affecting skin integrity. As much as 1.69 ± 0.004 mg of VAL permeated after 8 h. Finally, it could be concluded that this work had successfully developed a new approach for VALS drug delivery and could potentially show a significant impact on the treatment of hypertension. Further work should be considered.

摘要

缬沙坦(VAL)用作治疗高血压的一线药物。然而,口服缬沙坦时吸收较差且生物利用度低。为克服这些问题,本研究开发了缬沙坦透皮凝胶,其中卡波姆用作凝胶基质。此外,将具有不同针长的固体微针( Dermaroller)与透皮凝胶相结合,以改善其透过作为皮肤屏障的角质层的渗透性。对所开发的制剂进行了包括pH值、粘度、铺展性、挤出性、凝胶强度、药物含量、渗透性、释放度、封闭性和溶血等各种参数的进一步评估。结果表明,所有制剂均表现出理想的物理特性,且无任何潜在毒性。此外,该方法表明,与未处理的皮肤相比,使用微针可使缬沙坦的渗透性显著提高多达3倍。发现使用1.5毫米的微针是改善缬沙坦渗透性而不影响皮肤完整性的最佳组合。8小时后有多达1.69±0.004毫克的缬沙坦渗透。最后,可以得出结论,这项工作成功开发了一种缬沙坦给药的新方法,可能对高血压治疗产生重大影响。应考虑进一步的工作。

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