P 25 Vesicle-based resveratrol formulation for the topical treatment of Trichomonas vaginalis caused vaginal infection and inflammation

Abstract

Introduction Untreated vaginal inflammation can cause miscarriage, preterm labour, placental dysfunction and perinatal complications. Trichomonas vaginalis infection and inflammation are of serious concerns due to lipophosphoglycan (LPG) which triggers selective up regulation of cytokines, especially IL-8, in the female reproductive tract [1] . There are several anti-inflammatory and anti-microbial drugs currently available on the market, however, there is no general consensus regarding safe formulation especially for use in early pregnancy and considering microbial resistance. Resveratrol, a natural polyphenol, showed promising results comparing to clinically used drug metronidazole [2] . However, due to poor solubility and low bioavailability of resveratrol, its clinical application remains challenging. Our aim was to develop a non-teratogenic and non-toxic formulation which can be used in early pregnancy for the treatment of Trichomonas infection and inflammation. Methods Liposomes carrying resveratrol were characterized for their stability, size and entrapment efficiency. Antioxidant activities were evaluated by DPPH/ABTS+ and SOD activities. Antioxidant and anti-inflammatory activities of resveratrol and their corresponding vesicle-based formulation were compared. Anti-inflammatory activities were evaluated by measuring LPS-induced NO and pro-inflammatory cytokines such as IL-1β, TNF-α, IL-8 in macrophages (J774.1) and LPG-induced cytokines IL-8 in human vaginal cells lines (VK2/E6E7). Results Phospholipid-based vesicles, liposomes, of average size around 100 nm were found to be stable with a high resveratrol load (77%). Liposomal resveratrol was found to be 3 folds more potent than resveratrol in inhibiting NO production and up to 30% pro-inflammatory cytokines in macrophages were inhibited. IL-8 was inhibited up to 36% by the liposomal resveratrol in human vaginal cell lines VK2/E6E7 as compared to resveratrol. Conclusion Standardized liposomal resveratrol might be an appropriate, effective and safe topical formulation for the treatment of vaginal infection and inflammation against trichomoniasis in early pregnancy.