Department of Drug Form Technology, Wroclaw Medical University, Borowska 211 A, 50-556 Wroclaw, Poland.
Int J Mol Sci. 2021 Jun 16;22(12):6455. doi: 10.3390/ijms22126455.
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.
为了克服与阴道给药相关的限制,例如药物剂型与黏膜的短接触时间或载体的持续冲洗,有必要开发新的妇科用载体。此外,个体解剖和生理的高度变异性导致亲脂性活性物质的治疗效果不理想,需要应用多腔室药物传递系统。本文对基于乳剂的阴道给药剂型(EVDF)的文献进行了最新的综述,包括宏观乳液、微乳液、纳米乳液、多重乳液和自乳化药物传递系统。本文的第一部分讨论了(i)局部和全身给药后药物剂型治疗效果的解剖-生理条件的影响,(ii)EVDF 成分的表征以及这些剂型的制造技术,以及(iii)用于评估基于乳剂的阴道给药剂型的物理化学和药物性质的方法。本文的第二部分介绍了(iv)生物和体内研究的结果,以及(v)不同适应症下 EVDF 的安全性和治疗效果的临床评估。