Abstract
Natural polyphenols, such as resveratrol (RES) or epicatechin (EPI), are attractive for treatments of various diseases, including vaginal infections and inflammation, because of their strong anti-oxidative and anti-inflammatory properties. However, their low solubility and consequent poor bioavailability limit their therapeutic uses. To overcome these limitations, a vaginal delivery system comprising either RES or EPI liposomes-in-hydrogel was developed. This system permits therapeutic action of both liposomal polyphenol (RES or EPI) and chitosan-based hydrogel. Liposomes of around 200 nm and entrapment efficiency of 81% and 77% for RES and EPI, respectively, were incorporated into chitosan hydrogel, respectively. Medium molecular weight chitosan (2.5%, w/w) was found to have optimal texture properties and mucoadhesiveness in ex vivo conditions. The in vitro release studies confirmed the sustained release of polyphenols from the system. Both liposomal polyphenols and polyphenols-in-liposomes-in-hydrogel exhibited only minor effects on cell toxicity. EPI showed superior radical scavenging activity at lower concentrations compared to antioxidants vitamin C and E. Anti-inflammatory activity expressed as the inhibitory activity of formulations on the NO production in the LPS-induced macrophages (RAW 264.7) confirmed the superiority of EPI liposomes-in-hydrogel. The plain liposomes-in-hydrogel also exhibited potent anti-inflammatory activity, suggesting that chitosan hydrogel acts in synergy regarding anti-inflammatory effect of formulation.
Highlights
Transmitted infections (STIs) are a heterogeneous group of infections affecting millions of people
Liposomes as drug delivery system offer numerous advantageous in localized treatment and have been confirmed as suitable carriers for topical skin therapy [27]. Due to their ability to provide sustained and controlled release of entrapped substances, and encapsulate both lipophilic and hydrophilic molecules, liposomes have been proposed as an advanced drug delivery system for vaginal therapy [28]
Liposomes were characterized for size, size distribution, zeta potential and polyphenol entrapment efficiency (Table 1)
Summary
Transmitted infections (STIs) are a heterogeneous group of infections affecting millions of people. Failure to treat or cure STIs leads to severe consequences such as infertility, miscarriage, stillbirth, and transmission of infection from mother to child Those infections are rather a neglected health topic and current therapies fail to manage the treatment effectively. We have been focused on two approaches to address the failure of management of STIs, namely the development of advanced delivery systems for optimized localized vaginal therapy and use of natural origin substances as antimicrobial and anti-inflammatory agents [3,4,5]. Resveratrol (RES) is one of the polyphenols of natural origin, mainly from blueberry or red grapes, with multifunctional therapeutic effects It is a member of stilbene family, widely studied for its biological properties, mostly attributed to its anti-oxidative, anti-inflammatory, and immune-modulating effects [6]. Liposomes were stored in a refrigerator for at least 6 h prior to further use
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