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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.

Daru : Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
|December 11, 2024
PubMed
Abstract

Insights

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.
Keywords:
Amphotericin BDissolvable microarray patchesInclusion complexIntravaginal drug deliveryβ-cyclodextrin

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