Innovative Berberine-Loaded Nanoparticle Vaginal Pessaries for Effective Vulvovaginitis Therapy

Abstract

Vulvovaginal candidiasis (VVC) is a common gynecological infection with limited effective treatment options, highlighting the need for novel therapeutic strategies. This study investigated the potential of solid lipid nanoparticles (SLNs) loaded with berberine (BER) for vaginal administration as an innovative antifungal therapy. The research question focused on whether BER-SLN pessaries could enhance drug delivery, physicochemical stability, and antifungal efficacy against Candida infections. A 3² factorial design was employed to optimize SLN formulation using Compritol 888 ATO as the lipid, soy lecithin as the stabilizer, and Tween-80 as the surfactant. Surfactant concentration and drug-to-lipid ratio were selected as independent variables. The optimized formulation was characterized for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, and drug release. Morphological features were confirmed by transmission electron microscopy (TEM), while FT-IR spectroscopy was used to assess chemical compatibility. The selected SLN formulation was incorporated into pessaries, which were evaluated for antifungal activity using the cup-plate technique and validated in vivo in a rat model of VVC. The optimum SLNs formulation (4% Tween-80, 0.1 drug-to-lipid ratio) was F4 (BER.SLNF4) showed acceptable Particle size (225.8 ± 52.62 nm), high EE (77.3 ± 1.53%) and Zeta -potential (-28.5 ± 1.1 mV) and 99.83% drug release within 6 h. Pessaries containing BER-SLNs exhibited potent antifungal activity in vitro and effectively reduced Candida infection in vivo. Short-term storage studies (3 months) indicated acceptable stability under controlled conditions. BER-SLN pessaries represent a promising antifungal delivery system for VVC, combining improved physicochemical stability, enhanced drug release, and therapeutic efficacy.