Abstract
In order to overcome the limitations associated with vaginal administration of drugs, e.g., the short contact time of the drug form with the mucosa or continuous carrier wash-out, the development of new carriers for gynecological use is necessary. Furthermore, high individual anatomical and physiological variability resulting in unsatisfactory therapeutic efficacy of lipophilic active substances requires application of multicompartment drug delivery systems. This manuscript provides an up-to-date comprehensive review of the literature on emulsion-based vaginal dosage forms (EVDF) including macroemulsions, microemulsions, nanoemulsions, multiple emulsions and self-emulsifying drug delivery systems. The first part of the paper discusses (i) the influence of anatomical-physiological conditions on therapeutic efficacy of drug forms after local and systemic administration, (ii) characterization of EVDF components and the manufacturing techniques of these dosage forms and (iii) methods used to evaluate the physicochemical and pharmaceutical properties of emulsion-based vaginal dosage forms. The second part of the paper presents (iv) the results of biological and in vivo studies as well as (v) clinical evaluation of EVDF safety and therapeutic efficacy across different indications.
Highlights
The vaginal route of drug administration has been commonly used for many years in contraceptive delivery methods and the treatment of local vaginal infections in the form of vaginal solutions, ointments, pessaries, rings, suppositories and tablets [1]
In order to overcome limitations related to intravaginal drug administration, i.e., short contact time with mucosa, constant washing-out by vaginal discharge, low volume of vaginal discharge and high individual anatomical and physiological variability, there is a need for novel gynecological formulations development, such as hydrogels, films, micro- and nanoemulsions or nanoparticles-based drug delivery systems [2,3,4,5,6,7,8,9,10]
This review aims at providing the readers with a comprehensive analysis of the composition, manufacturing methods and evaluation methodology of emulsion-based vaginal dosage forms as well as the therapeutic effects achieved after administration of these formulations
Summary
The vaginal route of drug administration has been commonly used for many years in contraceptive delivery methods and the treatment of local vaginal infections in the form of vaginal solutions, ointments, pessaries, rings, suppositories and tablets [1]. In order to overcome limitations related to intravaginal drug administration, i.e., short contact time with mucosa, constant washing-out by vaginal discharge, low volume of vaginal discharge and high individual anatomical and physiological variability, there is a need for novel gynecological formulations development, such as hydrogels, films, micro- and nanoemulsions or nanoparticles-based drug delivery systems [2,3,4,5,6,7,8,9,10]. Emulsion-based vaginal dosage forms (EVDF) in comparison to hydrophilic carriers exhibit favorable formulation properties for vaginal administration, i.e., increased retention time at the application site and controlled penetration of active substances through the vaginal mucosa [2,3,5,6,10]
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