Pharmaceutical-technological aspects of therapeutic systems for hormonal contraception

Abstract

The use of therapeutic systems for hormonal contraception (TSHC) represents an important alternative approach for prevention of unintended pregnancies in comparison to oral hormonal contraceptives, whereby the risk of gastrointestinal adverse effects eliminates, the reduction of the therapeutic dose, the frequency of application and the undesired side effects enable and the adherence increases. So far, the marketed therapeutic systems are designed as transdermal patches, subdermal (subcutaneous) implants, vaginal rings, and intrauterine systems (IUS) for progestin-only hormonal contraception (by progesterone, levonorgestrel, etonogestrel, nestorone), or for combined hormonal contraception (ethinyl estradiol + norelgestormin, gestodene + ethinyl estradiol, etonogestrel + ethinyl estradiol, levonorgestrel + ethinyl estradiol, ethinyl estradiol + nestorone, nestorone + estradiol). The article describes the common characteristics of the different types of TSHC as well as specificity in terms of their design, composition and application. The main mechanisms for achieving controlled sustained release of the hormones and the efficiency of the delivery of the active substances in various TSHC are described. The main current approaches to design therapeutic system of this type in order to simplify their application, improve tolerability, acceptability and therapeutic efficiency are presented. The possibility of using novel Multipurpose Prevention Technologies in the development of the therapeutic systems for conception and prevention of human immunodeficiency virus (HIV) infection is described.

Keywords

• therapeutic systems for hormonal contraception
• transdermal patch
• subdermal (subcutaneous) implant
• vaginal ring
• intrauterine system
• progestins
• estrogens
• controlled/sustained release
• multipurpose prevention technologies