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Development of amphotericin B inclusion complex formulation in dissolvable microarray patches for intravaginal
Habiburrahim Burhanuddin1, Cindy Kristina Enggi1, Frederika Tangdilintin1
1Faculty of Pharmacy, Hasanuddin University, Makassar, 90245, Indonesia.
Summary
Amphotericin B (AMB) solubility and vaginal delivery were improved using a novel dissolvable microarray patch (DMP) with a β-cyclodextrin (βCD) inclusion complex. This enhanced drug absorption for vulvovaginal candidiasis treatment.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Mycology
Background:
- Amphotericin B (AMB) is crucial for treating vulvovaginal candidiasis (VVC).
- Poor oral absorption of AMB limits its therapeutic effectiveness.
- β-cyclodextrin (βCD) inclusion complexes enhance AMB solubility.
Purpose of the Study:
- To improve AMB solubility and bioavailability via a βCD inclusion complex.
- To develop a novel dissolvable microarray patch (DMP) for enhanced AMB vaginal delivery.
- To optimize DMP formulation for drug retention, penetration, and controlled release.
Main Methods:
- Molecular docking confirmed AMB-βCD inclusion complex (IC) stability.
- DMP formulated with IC, polyvinyl alcohol (PVA), and polyvinylpyrrolidone (PVP).
- Porcine vaginal mucosa used to evaluate DMP mechanical strength, insertion, and irritation; Differential Scanning Calorimetry (DSC) assessed physicochemical properties.
Main Results:
- AMB solubility increased up to fourfold with the inclusion complex.
- IC-DMP demonstrated excellent mechanical properties and insertion without irritation.
- Formula F3 showed superior retention in porcine vaginal mucosa (AUC: 208.02 ± 0.33 h·µg/cm³, Cmax: 20.05 ± 0.06 µg/cm³), indicating optimal vaginal drug delivery.
Conclusions:
- Integrating IC into DMP significantly boosts AMB solubility and bioavailability for intravaginal application.
- This novel DMP system enhances AMB absorption for VVC treatment.
- Further clinical studies are warranted for this promising drug delivery system.
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