微针经皮给药:系统综述

Dongare Rohini Suryabhan, Amate Shraddha Balasaheb
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引用次数: 0

摘要

透皮给药的好处是绕过第一关效应,允许药物长期释放。另一方面,角质层(SC)会形成屏障,限制药物的输送。微针是一种无痛、无创、易于使用的经皮给药系统,具有较高的药物生物利用度。由于透皮方法具有绕过第一过效应和允许药物长期释放的优点,因此已对多种药物进行了研究。由于皮肤的强大屏障特性,特别是角质层,许多药物在皮肤上的分布变得困难,只有少数具有适当物理化学性质(分子量500 Da,足够的亲脂性,低熔点)的药物可以有效地通过皮肤传递。另一方面,亲水药物和大分子药物,如肽、DNA和小干扰RNA,则难以运输。药物渗透到SC中可以通过使用各种方法绕过或可逆地破坏SC层来完成。最近有人提出使用微米尺度的针头来改善皮肤的渗透性,并证明它可以大大提高皮肤的渗透性,特别是对大分子。微针(MNs)可以穿过皮肤的SC层,进入活的表皮,避开神经纤维和血管,而神经纤维和血管主要存在于真皮层。皮下注射针、局部药膏和透皮贴剂是最常见的透皮给药方法。微针是一种新型的给药方法,有助于通过这种途径改善药物管理,同时也解决了传统配方带来的问题。其基本机制需要破坏皮肤层,从而形成微米大小的通道,将药物直接引导到表皮或真皮上部区域,在那里药物可以绕过屏障进入体循环。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Microneedles for Transdermal Drug Delivery: A Systematic Review
Transdermal delivery has the benefit of bypassing the first-pass effect and allowing for long-term drug release. The stratum corneum (SC), on the other hand, creates a barrier, which limits drug delivery. Microneedles are a painless, less invasive, and easy-to-use transdermal drug delivery system that has a high drug bioavailability. The transdermal method has been investigated for a variety of drugs because of its advantages of bypassing the first-pass effect and allowing for long-term drug release. The distribution of numerous medicinal substances across the skin has become difficult due to the skin’s strong barrier qualities, particularly the stratum corneum, only a few medications with appropriate physicochemical qualities (molecular weight 500 Da, enough lipophilicity, and low melting point) can be delivered efficiently through the skin. Hydrophilic medicines and macromolecular agents such as peptides, DNA, and small interfering RNA, on the other hand, are difficult to transport. Drug penetration into the SC can be accomplished by bypassing or reversibly disrupting the SC layer using a variety of methods. The use of micron-scale needles in improving skin permeability has recently been proposed and proved to greatly increase permeation, especially for macromolecules. Microneedles (MNs) can pass through the skin’s SC layer and into the live epidermis, avoiding nerve fibers and blood vessels, which are mostly found in the dermal layer. Hypodermic needles, topical creams, and transdermal patches are the most common methods for transdermal drug administration. Microneedles are a novel type of delivery method that helps to improve medication administration through this route while also solving the issues that come with traditional formulations. The fundamental mechanism entails disrupting the skin layer, resulting in micron-sized channels that lead the medication directly to the epidermis or upper dermis region, where it can bypass the barrier and enter the systemic circulation.
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