Abstract
The formulation of an ideal vaginal drug delivery system (DDS), with the requisite properties, with respect to safety, efficacy, patient compliance, aesthetics, harmonization with the regulatory requirements, and cost, requires a meticulous selection of the active ingredients and the excipients used. Novel excipients defined by diversity and multifunctionality are used in order to ameliorate drug delivery attributes. Synthetic and natural polymers are broadly used in pharmaceutical vaginal formulations (solid, semi-solid dosage forms, implantable devices, and nanomedicines) with a promising perspective in improving stability and compatibility issues when administered topically or systemically. Moreover, the use of biopolymers is aiming towards formulating novel bioactive, biocompatible, and biodegradable DDSs with a controllable drug release rate. Overviewing vaginal microenvironment, which is described by variable and perplexed features, a perceptive choice of excipients is essential. This review summarizes the recent advances on the excipients used in modified vaginal drug delivery formulations, in an attempt to aid the formulation scientist in selecting the optimal excipients for the preparation of vaginal products.
Highlights
Academic Editor: Daniela IannazzoDrug dosage forms involve excipients to offer properties to the active substance, such as physical stability, enhanced solubility, protection from microbial contamination, delivery optimization, and improved pharmacokinetics and/or bioavailability
Other absorption pathways that can occur through this route are passive diffusion and active transportation, which are defined by permeability and absorption characteristics, such as the molecular weight (MW), the extent of ionization, the lipophilicity, and the dissolution properties of active substances [10]
The results revealed that the association of chitosan and pectin can generate polyelectrolyte complexes and produced a robust system with mucoadhesion residence time on vaginal mucosa and a controlled release of tenofovir for four days, the time corresponding to vaginal turnover [45]
Summary
Drug dosage forms involve excipients to offer properties to the active substance, such as physical stability, enhanced solubility, protection from microbial contamination, delivery optimization, and improved pharmacokinetics and/or bioavailability. The appropriate dosage form design involves consideration of the physicochemical and biological aspects of the active substance and the excipients, as they all must be compatible with each other [1]. Safety and efficacy of vaginal administration have been well documented for local, and systemic effects. This review examines the utility of novel excipients in formulating vaginal delivery systems. The selection of research studies was conducted under the aspect of fabricating multifunctional pharmaceutical formulations by incorporating novel excipient combinations, targeting in patient compliance and side effects improvements characterized by safety and efficacy parameters.
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