Production and Ex Vivo Characterization of Melting Lipid Needle Patches Applied for Transdermal Delivery of Lipophilic Drugs

IF 9.6 1区化学 Q1 MATERIALS SCIENCE, MULTIDISCIPLINARY ACS Materials Letters Pub Date : 2024-10-24 DOI:10.1021/acsmaterialslett.4c0168610.1021/acsmaterialslett.4c01686

Matteo Tollemeto*, Lasse Ho̷jlund Eklund Thamdrup, Zhongyang Zhang, Isidro Badillo-Ramirez, Gavrielle R. Untracht, Peter Eskil Andersen, Line Hagner Nielsen and Anja Boisen,

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Abstract

Microneedle patches have gained significant attention for transdermal drug delivery, particularly those made from hydrophilic polymers for hydrophilic drugs. However, delivering poorly water-soluble lipophilic drugs remains a challenge. Our study introduces a lipid-based microneedle patch capable of effectively delivering lipophilic drugs with mechanically robust needles that penetrate physiological barriers like skin. Using a high-yield melt casting method, we produced needles up to 1200 μm in length with tunable melting points and phase transitions by adjusting lipid compositions. These patches release drugs at body temperature (37 °C). In a proof-of-concept experiment, curcumin, a model lipophilic drug, was fully dissolved and uniformly distributed in the needles, with drug loadings up to 50 wt %. Ex vivo studies demonstrated successful needle penetration and drug release in porcine skin. This lipid-based microneedle platform offers an effective solution for the transdermal, transmucosal, and buccal delivery of lipophilic drugs.

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用于亲脂性药物透皮给药的融脂针状贴片的生产和体内外特性分析

微针贴片在透皮给药方面备受关注，尤其是用亲水性聚合物制成的用于亲水性药物的微针贴片。然而，递送水溶性差的亲脂性药物仍然是一项挑战。我们的研究介绍了一种基于脂质的微针贴片，这种贴片能够有效地输送亲脂性药物，其机械坚固的针头能够穿透皮肤等生理屏障。我们采用高产熔铸法生产出了长度达 1200 μm 的针头，通过调整脂质成分可调节熔点和相变。这些贴片可在体温（37 °C）下释放药物。在概念验证实验中，姜黄素（一种亲脂性药物模型）被完全溶解并均匀分布在针头中，药物负载量高达 50 wt %。体内外研究表明，针头能成功穿透猪皮肤并释放药物。这种基于脂质的微针平台为亲脂性药物的透皮、透粘膜和口腔给药提供了有效的解决方案。

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来源期刊

ACS Materials Letters MATERIALS SCIENCE, MULTIDISCIPLINARY-

CiteScore

14.60

自引率

3.50%

发文量

261

期刊介绍： ACS Materials Letters is a journal that publishes high-quality and urgent papers at the forefront of fundamental and applied research in the field of materials science. It aims to bridge the gap between materials and other disciplines such as chemistry, engineering, and biology. The journal encourages multidisciplinary and innovative research that addresses global challenges. Papers submitted to ACS Materials Letters should clearly demonstrate the need for rapid disclosure of key results. The journal is interested in various areas including the design, synthesis, characterization, and evaluation of emerging materials, understanding the relationships between structure, property, and performance, as well as developing materials for applications in energy, environment, biomedical, electronics, and catalysis. The journal has a 2-year impact factor of 11.4 and is dedicated to publishing transformative materials research with fast processing times. The editors and staff of ACS Materials Letters actively participate in major scientific conferences and engage closely with readers and authors. The journal also maintains an active presence on social media to provide authors with greater visibility.