Journal
PHARMACEUTICS
Volume 14, Issue 6, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics14061295
Keywords
vaginal drug delivery; toxicity; EpiVaginal (TM) tissue model; irritation; resveratrol; liposomes; chitosan hydrogel
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Funding
- Northern Norway Regional Health Authority (HelseNord) RHF [HNF1376-17]
- Terje and Valerie Stadler Jacobsen's research fund [240001/A59078]
- UiT The Arctic University of Norway
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A formulation using liposomes loaded with resveratrol (RES) and incorporated into a chitosan hydrogel has been developed for delivering RES to the vaginal site. In vitro experiments showed that this formulation is non-irritant and biocompatible with vaginal tissue at therapeutic concentrations.
The natural polyphenol resveratrol (RES) has shown great potential as an antimicrobial, including against microbes associated with vaginal infections. To fully exploit the activities of RES, an all-natural ingredients formulation for RES delivery at vaginal site has been developed, namely liposomes loaded with RES, incorporated into a chitosan hydrogel as secondary vehicle. Although considered non-toxic and safe on their own, the compatibility of the final formulation must be evaluated for its biocompatibility and non-irritancy to the vaginal mucosa. As a preclinical safety assessment, the impact of RES formulation on the tissue viability, the effect on barrier function and cell monolayer integrity, and cytotoxicity were evaluated using the cell-based vaginal tissue model, the EpiVaginal (TM) tissue. RES liposomes-in-hydrogel formulations neither affected the mitochondrial activity, nor the integrity of the cell monolayer in RES concentration up to 60 mu g/mL. Moreover, the barrier function was maintained to a greater extent by RES in formulation, emphasizing the benefits of the delivery system. Additionally, none of the tested formulations expressed an increase in lactate dehydrogenase activity compared to the non-treated tissues. The evaluation of the RES delivery system suggests that it is non-irritant and biocompatible with vaginal tissue in vitro in the RES concentrations considered as therapeutic.
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