Sitruk-Ware R
Medical Department, CIBA-GEIGY LTD, Basle, Switzerland.
Contraception. 1989 Jan;39(1):1-20. doi: 10.1016/0010-7824(89)90012-7.
The advantages of delivering drugs through the skin for systemic therapy have been widely recognized and represent a growing sector in drug development. Transdermal delivery of steroids is also a rapidly expanding field and in various clinical situations where hormonal replacement therapy is needed this route of administration is a real breakthrough, considering the relative toxicity of some steroids when given orally. Various transdermal systems have been designed, all of them aimed at achieving a constant release rate of the molecules contained in their reservoir through the intact skin. The skin itself, and especially the outermost layer, the stratum corneum, can play the roles of a reservoir and a rate-controlling membrane. So far, estradiol, progesterone and testosterone have been demonstrated to be good candidates for transdermal delivery. The effectiveness and the acceptability of transdermal delivery of estradiol in postmenopausal women have been demonstrated. The efficacy of topical administration of progesterone in patients with benign breast disease has also been proved. More recently, the high rate of acceptability and efficacy of transdermal testosterone in male hypogonadism has been demonstrated. The transdermal delivery of steroids is therefore expected to make a significant impact on the quality of patient care both in men and in women.
通过皮肤给药进行全身治疗的优势已得到广泛认可,并且在药物研发领域中所占份额日益增长。类固醇的透皮给药也是一个迅速发展的领域,在各种需要激素替代疗法的临床情况下,考虑到某些类固醇口服时的相对毒性,这种给药途径是一项真正的突破。已经设计了各种透皮系统,所有这些系统的目的都是使储库中所含分子通过完整皮肤实现恒定释放速率。皮肤本身,尤其是最外层的角质层,可以起到储库和速率控制膜的作用。到目前为止,雌二醇、孕酮和睾酮已被证明是透皮给药的良好候选药物。绝经后妇女中雌二醇透皮给药的有效性和可接受性已得到证实。孕酮局部给药对患有良性乳腺疾病患者的疗效也已得到证明。最近,透皮睾酮在男性性腺功能减退中的高接受率和疗效也已得到证实。因此,类固醇的透皮给药有望对男性和女性患者的护理质量产生重大影响。