Department of Obstetrics and Gynecology, Pontificia Universidad Católica de Chile, School of Medicine, Santiago, Chile.
Nanomedicine. 2012 Sep;8 Suppl 1:S83-9. doi: 10.1016/j.nano.2012.05.008. Epub 2012 May 26.
Nanomedicine is an emerging technology and the first nano-engineered medical products have come to light in the last decade. Transdermal drug delivery has significant advantages compared to other routes of drug administration. Nanoparticles unique physical and chemical properties enable transport of substances directly into the skin. The objective of this paper is to review different aspects of nanoparticle delivery, generally, and discuss its current use for transdermal hormone therapy. Transdermal estrogen therapy remains the most effective treatment for bothersome menopausal symptoms, particularly in those women for whom the potential adverse effects associated with "first pass" hepatic metabolism are to be avoided. Available alternatives for transdermal estrogen delivery include patches, gels, sprays and lotions. Other non-oral therapies which likewise avoid "first pass" hepatic metabolism include: subcutaneous implants and vaginal rings. Some of the transdermal products are associated with mild adverse skin effects such as redness and irritation, but more severe and bothersome consequences include blistering and tattooing. Even the mild adverse skin effects are frequently cited as reasons for discontinuation. Micellar nanoparticle estradiol emulsion (MNPEE) is a lotion-like therapy which constitutes an alternative transdermal delivery system not requiring the permeation enhancers or temporary skin digestion, both of which increase the possibility of irritation. MNPEE's advantages include low fluctuation of plasma estradiol concentrations, infrequent skin related adverse effects, and pleasant cosmetic-like moisturizing properties. The efficacy of MNPEE for management of menopausal vasomotor symptoms has been demonstrated in a randomized placebo controlled trial,(1) and the product is FDA approved for management of moderate to severe vasomotor symptoms. None of the observed adverse effects in the MNPEE group were statistically different from the placebo group.(1) Studies addressing inadvertent transference of estradiol to the male partners of menopausal women using this delivery technology have demonstrated small, but real amounts of transference, which do not exceed the normal physiological male estradiol range. MNPEE is safe and effective for treatment of vasomotor symptoms and represents the commercial validation of nanoparticle technology for transdermal delivery of estrogen therapy (ET) for postmenopausal women with vasomotor symptoms.
纳米医学是一门新兴技术，在过去十年中，第一批纳米工程医疗产品已经问世。与其他给药途径相比，经皮药物输送具有显著优势。纳米粒子独特的物理和化学特性使其能够将物质直接输送到皮肤中。本文的目的是综述纳米粒子输送的各个方面，一般来说，并讨论其目前在经皮激素治疗中的应用。经皮雌激素治疗仍然是治疗烦人的更年期症状的最有效方法，特别是对于那些希望避免与“首过”肝代谢相关的潜在不良反应的女性。经皮雌激素传递的可用替代方法包括贴片、凝胶、喷雾剂和乳液。其他避免“首过”肝代谢的非口服疗法包括：皮下植入物和阴道环。一些经皮产品与轻微的皮肤不良反应有关，如发红和刺激，但更严重和烦人的后果包括起疱和纹身。即使是轻微的皮肤不良反应也常被列为停药的原因。胶束纳米雌二醇乳剂（MNPEE）是一种乳液样治疗剂，构成了一种替代的经皮传递系统，不需要渗透增强剂或暂时的皮肤消化，这两者都增加了刺激的可能性。MNPEE 的优点包括血浆雌二醇浓度波动小、皮肤相关不良反应少、具有令人愉悦的美容保湿特性。MNPEE 治疗更年期血管舒缩症状的疗效已在一项随机安慰剂对照试验中得到证实，(1) 该产品已获得 FDA 批准用于治疗中度至重度血管舒缩症状。(1) 在使用这种传递技术的接受 MNPEE 治疗的更年期女性的男性伴侣中，研究观察到了雌激素的意外转移，但这些转移量很小，没有超过正常的男性生理性雌二醇范围。MNPEE 治疗血管舒缩症状安全有效，为经皮传递雌激素治疗（ET）用于有血管舒缩症状的绝经后妇女提供了纳米技术的商业验证。
