Carrier Polymer-Free Dissolvable Microneedles Enable Superhigh Drug Payload for Percutaneous Protein Delivery

IF 8.7 1区化学 Q1 MATERIALS SCIENCE, MULTIDISCIPLINARY ACS Materials Letters Pub Date : 2024-10-07 DOI:10.1021/acsmaterialslett.4c01164

Zhao Wang, Lin Liu, Ergang Liu*, Rongli Chen, Yongzhuo Huang* and Qianbin Li*,

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Abstract

Microneedle (MN) patches present a painless alternative for transdermal delivery of monoclonal antibodies (mAbs), yet existing dissolvable MNs are hindered by a low drug-loading capacity (DLC). This study introduces a carrier-free approach for fabricating mAb MNs by a solution-casting method, providing a superhigh drug-payload MN platform (DLC around 70%). Additionally, the use of concentrated proteins prevents interpenetration between the backing layer and the tip, assuring the dosage accuracy of the therapeutic antibodies. Physicochemical characteristics, including mechanical strength, dissolvability, and skin permeability, were evaluated and compared with conventional PVP K17 (poly(vinylpyrrolidone), K17) microneedles. Finally, the transdermal performance of protein dMNs was assessed using IL-17A (Iinterleukin-17A) antibody as a model protein drug, with in vivo therapeutic efficacy evaluated in a psoriatic mouse model. The results demonstrate the feasibility and effectiveness of excipient-free dMNs for mAb delivery, significantly improving the drug-loading capacity, while mitigating safety concerns associated with carrier polymers.

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不含载体聚合物的可溶解性微针可实现超高载药量的经皮蛋白质递送

微针（MN）贴片是单克隆抗体（mAbs）透皮给药的无痛替代品，但现有的可溶解 MN 受制于低药物负载能力（DLC）。本研究介绍了一种通过溶液浇铸法制造 mAb MN 的无载体方法，提供了一种超高药物负载 MN 平台（DLC 约为 70%）。此外，浓缩蛋白质的使用可防止背衬层和尖端之间的相互渗透，从而确保治疗性抗体的剂量准确性。对机械强度、溶解性和皮肤渗透性等理化特性进行了评估，并与传统的 PVP K17（聚乙烯吡咯烷酮，K17）微针进行了比较。最后，以 IL-17A（白细胞介素-17A）抗体作为蛋白质药物模型，评估了蛋白质 dMNs 的透皮性能，并在银屑病小鼠模型中评估了其体内疗效。研究结果证明了不含赋形剂的 dMNs 用于 mAb 给药的可行性和有效性，大大提高了药物负载能力，同时减轻了与载体聚合物相关的安全问题。

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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.