DRUG DELIVERY SYSTEMS .6. TRANSDERMAL DRUG DELIVERY
DRUG DELIVERY SYSTEMS .6. TRANSDERMAL DRUG DELIVERY
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DOI：
10.1002/j.1552-4604.1991.tb01895.x
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发表时间：
1991-05-01
影响因子：
2.9
通讯作者：
RANADE, VV
中科院分区：
文献类型：
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作者：
RANADE, VV
经皮给药系统已经存在了很长时间。过去，最常用的系统是用于皮肤病的局部应用的乳膏和软膏。这些制剂中的一些的全身性副作用的发生指示通过皮肤吸收。许多药物已被应用于皮肤进行全身治疗。在广义上，术语透皮递送系统包括旨在将活性成分递送到全身循环中的所有局部施用的药物制剂。透皮治疗系统已经被设计成提供药物经由皮肤到体循环的受控连续递送。皮肤的相对不渗透性是众所周知的，这与其作为防止微生物入侵和防止生理必需物质如水损失的双重保护屏障的功能有关。有助于这种不渗透性的因素的阐明使得使用皮肤作为受控全身药物递送的途径成为可能。基本上，有四种系统可以使药物有效地通过皮肤吸收。微密封系统是一种分配控制的递送系统，其包含药物储库，药物在水混溶性溶剂中的饱和悬浮液均匀分散在硅酮弹性体基质中。第二个系统是基质扩散控制系统。第三种也是最广泛使用的透皮给药系统是膜渗透控制系统。第四个系统，最近可用，是梯度充电系统。此外，先进的透皮载体包括系统，例如离子电渗和超声促渗系统、热固性凝胶、前药和脂质体。许多药物已经被配制成透皮系统，并且正在检查其他药物以这种方式递送的可行性（例如，尼古丁抗组胺药、β-阻断剂、钙通道阻断剂、非甾体抗炎药、避孕药、抗抑郁药、胰岛素、抗病毒药、激素、α-干扰素和癌症化疗剂）。研究还继续对各种化学渗透增强剂，可以允许治疗物质的输送。例如，渗透增强剂如Azone可以允许递送较大尺寸的分子如蛋白质和多肽。
Transdermal drug delivery system has been in existence for a long time. In the past, the most commonly applied systems were topically applied creams and ointments for dermatological disorders. The occurrence of systemic side-effects with some of these formulations is indicative of absorption through the skin. A number of drugs have been applied to the skin for systemic treatment. In a broad sense, the term transdermal delivery system includes all topically administered drug formulations intended to deliver the active ingredient into the general circulation. Transdermal therapeutic systems have been designed to provide controlled continuous delivery of drugs via the skin to the systemic circulation. The relative impermeability of skin is well known, and this is associated with its functions as a dual protective barrier against invasion by micro-organisms and the prevention of the loss of physiologically essential substances such as water. Elucidation of factors that contribute to this impermeability has made the use of skin as a route for controlled systemic drug delivery possible. Basically, four systems are available that allow for effective absorption of drugs across the skin. The microsealed system is a partition-controlled delivery system that contains a drug reservoir with a saturated suspension of drug in a water-miscible solvent homogeneously dispersed in a silicone elastomer matrix. A second system is the matrix-diffusion controlled system. The third and most widely used system for transdermal drug delivery is the membrane-permeation controlled system. A fourth system, recently made available, is the gradient-charged system. Additionally, advanced transdermal carriers include systems such as iontophoretic and sonophoretic systems, thermosetting gels, prodrugs, and liposomes. Many drugs have been formulated in transdermal systems, and others are being examined for the feasibility of their delivery in this manner (e.g., nicotine antihistamines, beta-blockers, calcium channel blockers, non-steroidal anti-inflammatory drugs, contraceptives, anti-arrhythmic drugs, insulin, antivirals, hormones, alpha-interferon, and cancer chemotherapeutic agents). Research also continues on various chemical penetration enhancers that may allow delivery of therapeutic substances. For example, penetration enhancers such as Azone may allow delivery of larger-sized molecules such as proteins and polypeptides.