Abstract
The vagina is a promising site for both local and systemic drug delivery and represents an interesting administration route for compounds with poor oral bioavailability. Whereas most of the currently marketed dosage forms were designed as immediate release formulations, intravaginal rings (IVRs) offer the possibility of a controlled vaginal drug delivery over several weeks or months. For a long time, the development of IVRs was limited to steroid-releasing formulations. Recently, IVRs have witnessed a surge of new interest as promising delivery systems for microbicides. Therefore, various novel IVR designs have been introduced. To ensure that only safe and effective IVRs will be administered to patients, it is important to properly distinguish between IVRs with desired and undesired release performance. In vitro methods for evaluating drug release of IVRs that present with sufficient predictive capacity for in vivo drug release, and discriminatory power with regard to IVRs quality, are an essential tool for this purpose. The objective of the present review article is to present the current status of in vitro drug release testing of IVRs and to critically discuss current compendial and non-official in vitro drug release methods with regard to their discriminatory power and in vivo predictivity.
Highlights
The female vagina is well known as a genital organ with functions related to conception
There are no approved microbicides available yet, but currently, it looks like the first microbicide to be submitted for regulatory approval will be a silicone-based membrane-type intravaginal rings (IVRs) developed by the International Partnership for Microbicides (IPM)
By reviewing the official drug release methods available in international pharmacopoeias and guidelines, and the in vitro methods for assessing drug release of IVRs described in the literature, it became obvious that, to date, neither a standardized in vitro drug release method for quality control (QC), nor a biopredictive in vitro method for IVRs had been described
Summary
The female vagina is well known as a genital organ with functions related to conception. Different types of vaginal dosage forms for both local and systemic action are available on the market or in clinical development. Whereas most of the currently marketed dosage forms were designed as immediate release (IR) formulations, vaginal rings, called intravaginal rings (IVRs) offer the possibility of a controlled vaginal drug delivery over several weeks or months. There are no approved microbicides available yet, but currently, it looks like the first microbicide to be submitted for regulatory approval will be a silicone-based membrane-type IVR developed by the International Partnership for Microbicides (IPM) This IVR releases dapivirine for local action in the vagina over the duration of one month [14]. The objective of the present review article is to present the current status of in vitro drug release testing of IVRs and to critically discuss current compendial and non-official in vitro drug release methods with regard to their discriminatory power and in vivo predictivity
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