Nestorone®: clinical applications for contraception and HRT

The vagina has been studied as a suitable site for local and systemic delivery of drugs. There are a large number of vaginal medications on the market. Most of them, however, require frequent applications due to their short vaginal residence time. A prolonged vaginal residence time of formulations is therefore a key parameter for improved therapeutic efficacy. Promising approaches for prolonging the residence time base on mucoadhesion, were in-situ sol-to-gel transition and mechanical fixation. Mucoadhesive drug delivery systems can be tailored to adhere to the vaginal tissue. In-situ gelling systems offer the advantage of increased viscosity in vaginal cavity and consequently reduce outflow from the vagina. Mechanical fixation needs specially shaped drug delivery systems and reduce the frequency of administration significantly. In this review, an overview on these different strategies and systems is provided. Furthermore, the techniques to evaluate the potential of these systems for prolonged vaginal residence time are described. _______________________________________________________________________________________

show abstract

“…The steroids are contained in cores within the ring body. The rings are designed for 1-year efficacy ( Figure 14) (130).…”

Section: Intravaginal Ringsmentioning

confidence: 99%

Strategies to Prolong the Intravaginal Residence Time of Drug Delivery Systems

et al. 2009

View full text Add to dashboard Cite

show abstract

“…60 Another patch is being developed: this patch releases 50 micrograms/day of gestodene and 18 micrograms of EE and was shown to suppress ovulation in all 199 women in a study over two cycles. 62 Nestorone has also undergone preliminary evaluation in the form of both a gel 63 and a spray. 64 In trials with the gel, mean serum levels of 150 pmol/l were observed, achieving 83% ovulation suppression.…”

Section: Transdermal Administrationmentioning

confidence: 99%

New technologies in contraception

Rowlands

2008

BJOG

View full text Add to dashboard Cite

New technologies in both reversible contraception and sterilisation are described. The review includes recent advances in the development of oral contraception, emergency contraception, injectable contraception, vaginal rings, subdermal implants, transdermal contraception, intrauterine devices, spermicides and barrier methods. It also covers methods of transcervical female sterilisation and more easily reversible male sterilisation.The emphasis is on the technology and its safety and effectiveness. Hormonal delivery systems are described in some detail. Mention is also made of research into vaccines and male hormonal methods, where progress has been disappointing.

show abstract

“…NES is not active orally but is rapidly absorbed through the skin. A prior 3-month dose-finding study of a NES gel formulation for transdermal use showed ovulation inhibition in 53%, 64% and 83% of the subjects that received 0.3, 0.6 or 1.2 mg NES [12].…”

Section: Introductionmentioning

confidence: 98%

“…The targeted antiovulatory NES serum threshold was 250 pmol/L, based on data obtained from the above study and a NES-only ring study [12,13]. This formulation was tested in a dose-finding study conducted with the primary objective to establish the minimal dose of NES to ensure ovulation suppression (progesterone levels b 10 nmol/L and no follicle rupture) in 90-95% of the cycles, together with suppressed follicle growth but an E2 dose sufficient to ensure adequate E2 levels (not consistently below 100 pmol/L).…”

Section: Introductionmentioning

confidence: 99%