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用于增强透皮给药的微柱集成溶解微针

Micro-Pillar Integrated Dissolving Microneedles for Enhanced Transdermal Drug Delivery.

作者信息

Lee Seunghee, Fakhraei Lahiji Shayan, Jang Jeesu, Jang Mingyu, Jung Hyungil

机构信息

Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Korea.

Juvic Biotech, Inc., No. 208, Digital-ro 272, Guro-gu, Seoul 08389, Korea.

出版信息

Pharmaceutics. 2019 Aug 10;11(8):402. doi: 10.3390/pharmaceutics11080402.

Abstract

The dissolving microneedle (DMN) patch is a transdermal delivery system, containing arrays of micro-sized polymeric needles capable of encapsulating therapeutic drugs within their matrix and releasing them into the skin. However, the elastic properties of the skin prevent DMNs from complete insertion and accurate delivery of encapsulated compounds into the skin. Moreover, the adhesive materials used in patches may cause skin irritation, inflammation, and redness. Therefore, we developed a patchless, micro-pillar integrated DMN (P-DMN) that is simple to fabricate and enhances transdermal drug delivery compared with traditional DMN patches. The micro-pillars were made of polymethyl methacrylate at a height of 300 μm and a base diameter of 500 μm. To fabricate P-DMNs, we employed hyaluronic acid, which is a widely used derma filler and plays a role in tissue re-epithelialization. We demonstrate that utilizing P-DMNs significantly improves the delivery efficiency of an encapsulated drug surrogate (91.83% ± 7.75%) compared with traditional DMNs (64.86% ± 8.17%). Interestingly, P-DMNs remarkably increase the skin penetration accuracy rate of encapsulated drugs, up to 97.78% ± 2.22%, compared with 44.44% ± 7.85% in traditional DMNs. Our findings suggest that P-DMNs could serve as a highly accurate and efficient platform for transdermal delivery of various types of micro- and macro-biomolecules.

摘要

溶解微针(DMN)贴片是一种经皮给药系统,包含微型聚合物针阵列,能够将治疗药物包裹在其基质中并释放到皮肤中。然而,皮肤的弹性特性阻碍了DMN完全插入并将包裹的化合物准确递送至皮肤。此外,贴片中使用的粘合材料可能会导致皮肤刺激、炎症和发红。因此,我们开发了一种无贴片的微柱集成DMN(P-DMN),其制造简单,与传统的DMN贴片相比,可增强经皮给药。微柱由聚甲基丙烯酸甲酯制成,高度为300μm,基部直径为500μm。为了制造P-DMN,我们使用了透明质酸,它是一种广泛使用的皮肤填充剂,在组织重新上皮化中起作用。我们证明,与传统的DMN(64.86%±8.17%)相比,使用P-DMN可显著提高包裹药物替代物的递送效率(91.83%±7.75%)。有趣的是,与传统DMN的44.44%±7.

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3bc/6724014/4a529f30a47a/pharmaceutics-11-00402-g001.jpg

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