• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

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.

DOI:10.1080/09205063.2022.2121590
PMID:36063003
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。

相似文献

1
Improved transdermal delivery of valsartan using combinatorial approach of polymeric transdermal hydrogels and solid microneedles: an proof of concept investigation.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。
J Biomater Sci Polym Ed. 2023 Feb;34(3):334-350. doi: 10.1080/09205063.2022.2121590. Epub 2022 Sep 12.
2
Combinatorial Approach of Thermosensitive Hydrogels and Solid Microneedles to Improve Transdermal Delivery of Valsartan: an In Vivo Proof of Concept Study.温敏水凝胶与固体微针联合应用提高缬沙坦经皮传递:体内概念验证研究。
AAPS PharmSciTech. 2022 Nov 29;24(1):5. doi: 10.1208/s12249-022-02462-y.
3
Combination of transdermal patches and solid microneedles for improved transdermal delivery of primaquine.经皮贴片与固体微针联合应用提高伯氨喹的经皮传递
Int J Pharm. 2021 Nov 20;609:121204. doi: 10.1016/j.ijpharm.2021.121204. Epub 2021 Oct 16.
4
Transdermal drug delivery of rizatriptan using microneedles array patch: preparation, characterization and ex-vivo/in-vivo study.经皮给药系统中使用微针贴片传递利扎曲普坦:制备、表征和在体/体内研究。
Pharm Dev Technol. 2024 Sep;29(7):776-789. doi: 10.1080/10837450.2024.2393218. Epub 2024 Aug 24.
5
Enhancement of skin localization of β-carotene from red fruit (Pandanus conoideus Lam.) using solid dispersion-thermoresponsive gel delivered via polymeric solid microneedles.利用固体分散体-温敏凝胶递送至聚合物固体微针增强红色水果(露兜树)中β-胡萝卜素的皮肤定位。
Int J Pharm. 2024 Jul 20;660:124307. doi: 10.1016/j.ijpharm.2024.124307. Epub 2024 Jun 8.
6
Enhanced skin localization of metronidazole using solid lipid microparticles incorporated into polymeric hydrogels for potential improved of rosacea treatment: An ex vivo proof of concept investigation.利用固体脂质微球增强甲硝唑在聚合物水凝胶中的皮肤定位,以潜在改善酒渣鼻治疗:体外概念验证研究。
Int J Pharm. 2022 Nov 25;628:122327. doi: 10.1016/j.ijpharm.2022.122327. Epub 2022 Oct 21.
7
Development of Hydrogels for Microneedle-Assisted Transdermal Delivery of Naloxone for Opioid-Induced Pruritus.水凝胶用于经皮给药微针辅助递送纳洛酮治疗阿片类药物诱导瘙痒的研究进展。
J Pharm Sci. 2019 Nov;108(11):3695-3703. doi: 10.1016/j.xphs.2019.08.025. Epub 2019 Aug 30.
8
Design, formulation and optimization of valsartan transdermal gel containing iso-eucalyptol as novel permeation enhancer: preclinical assessment of pharmacokinetics in Wistar albino rats.含异桉叶油醇作为新型渗透促进剂的缬沙坦透皮凝胶的设计、配方及优化:Wistar白化大鼠药代动力学的临床前评估
Expert Opin Drug Deliv. 2014 Aug;11(8):1149-62. doi: 10.1517/17425247.2014.914027. Epub 2014 May 15.
9
Investigation of antihypertensive activity of carbopol valsartan transdermal gel containing 1,8-cineole.含 1,8-桉叶素的卡波姆缬沙坦透皮凝胶的降压活性研究。
Int J Biol Macromol. 2014 Mar;64:144-9. doi: 10.1016/j.ijbiomac.2013.11.018. Epub 2013 Dec 1.
10
Development of hydrogel-forming microneedles for transdermal delivery of albendazole from liquid reservoir.水凝胶形成型微针的研制及其在阿苯达唑经皮给药中的应用(从液体储库中)。
J Biomater Sci Polym Ed. 2023 Jun;34(8):1101-1120. doi: 10.1080/09205063.2022.2157671. Epub 2022 Dec 18.

引用本文的文献

1
Multifunctional Hydrogel Microneedles (HMNs) in Drug Delivery and Diagnostics.用于药物递送与诊断的多功能水凝胶微针
Gels. 2025 Mar 15;11(3):206. doi: 10.3390/gels11030206.
2
Enhanced and Sustained Transdermal Delivery of Oxypurinol Using Thermosensitive Gel Combined with Polymeric Solid Microneedles.使用热敏凝胶与聚合物固体微针相结合实现氧嘌呤醇的增强和持续透皮给药。
ACS Omega. 2024 Dec 20;10(4):3500-3510. doi: 10.1021/acsomega.4c07716. eCollection 2025 Feb 4.
3
Microneedles and Their Application in Transdermal Delivery of Antihypertensive Drugs-A Review.
微针及其在抗高血压药物经皮给药中的应用——综述
Pharmaceutics. 2023 Jul 27;15(8):2029. doi: 10.3390/pharmaceutics15082029.