Evofem Biosciences, Inc., 12400 High Bluff Drive, Suite 600, San Diego, CA, 92130, USA.
Drug Deliv Transl Res. 2017 Dec;7(6):829-839. doi: 10.1007/s13346-017-0423-2.
Endometriosis and uterine fibroids (also known as uterine leiomyomas) are serious medical conditions affecting large numbers of women worldwide. Many women are asymptomatic but those with symptoms require medical intervention to relieve chronic pain and dysmenorrhea and to address infertility. Drug delivery has played a role in reducing some of the symptoms associated with endometriosis and uterine fibroids. Use of drug delivery systems for both conditions can roughly be divided into two categories: (1) existing systems designed for other indications such as contraception for symptomatic relief and (2) development of novel systems aimed at addressing some of the underlying biochemical changes associated with endometriosis and uterine fibroids such as oxidative stress, angiogenesis, and matrix degradation. The latter drug delivery approaches rely heavily on nanotechnology. Existing systems that deliver estrogens and/or progestins include vaginal rings, transdermal patches, and intrauterine systems. Long-acting implantable contraceptives such as Implanon® and injectables such as Depo-Provera® have found use in treating endometriosis. Similarly, long-acting GnRH products (e.g., Lupron Depot®) are used to treat endometriosis. Other drugs formulated in long-acting formulations include intravaginal rings capable of delivering selective progesterone receptor modulators, androgens such as danazol, and aromatase inhibitors (e.g., anastrozole). Nanoparticles composed of silica, poly(lactic-co-glycolic acid), cerium oxide, dendrimers, and chitosan/polyethyleneamine have all been investigated to improve treatment of endometriosis and to a lesser extent, uterine fibroids.
子宫内膜异位症和子宫肌瘤（也称为子宫平滑肌瘤）是影响全球大量女性的严重医学病症。许多女性无症状，但有症状的女性需要医疗干预来缓解慢性疼痛和痛经，并解决不孕问题。药物输送在减轻与子宫内膜异位症和子宫肌瘤相关的一些症状方面发挥了作用。用于这两种病症的药物输送系统大致可分为两类：（1）为其他适应症设计的现有系统，如避孕以缓解症状，（2）开发旨在解决与子宫内膜异位症和子宫肌瘤相关的一些潜在生化变化的新型系统，如氧化应激、血管生成和基质降解。后者药物输送方法在很大程度上依赖于纳米技术。输送雌激素和/或孕激素的现有系统包括阴道环、透皮贴剂和宫内系统。长效可植入避孕药如 Implanon®和注射剂如 Depo-Provera®已用于治疗子宫内膜异位症。同样，长效 GnRH 产品（如 Lupron Depot®）也用于治疗子宫内膜异位症。其他以长效配方配制的药物包括能够输送选择性孕激素受体调节剂、雄激素如丹那唑和芳香酶抑制剂（如阿那曲唑）的阴道环。由二氧化硅、聚（乳酸-共-乙醇酸）、氧化铈、树枝状大分子和壳聚糖/聚乙烯亚胺组成的纳米颗粒都已被研究用于改善子宫内膜异位症的治疗，在较小程度上也用于子宫肌瘤的治疗。
