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Development of an Antifungal Denture Adhesive Film for Oral Candidiasis Utilizing Hot Melt Extrusion Technology

Identifieur interne : 001B54 ( Main/Exploration ); précédent : 001B53; suivant : 001B55

Development of an Antifungal Denture Adhesive Film for Oral Candidiasis Utilizing Hot Melt Extrusion Technology

Auteurs : Jun-Bom Park [États-Unis] ; Suneela Prodduturi [États-Unis] ; Joe Morott [États-Unis] ; Vijay I. Kulkarni [États-Unis] ; Melissa R. Jacob [États-Unis] ; Shabana I. Khan [États-Unis] ; Steven P. Stodghill [États-Unis] ; Michael A. Repka [États-Unis]

Source :

Expert opinion on drug delivery [ 1742-5247 ] ; 2014.

RBID : PMC:5629914

Abstract

Objectives

The overall goal of this research was to produce a stable hot-melt extruded “Antifungal Denture Adhesive film” (ADA) system for the treatment of oral candidiasis.

Methods

The ADA systems with hydroxypropyl cellulose (HPC) and/or polyethylene oxide (PEO) containing clotrimazole (10%) or nystatin (10%) were extruded utilizing a lab scale twin-screw hot-melt extruder. Rolls of the antifungal-containing films were collected and subsequently die-cut into shapes adapted for a maxillary (upper) and mandibular (lower) denture.

Results

DSC and PXRD results indicated that the crystallinity of both APIs was changed to amorphous phase after hot-melt extrusion. The ADA system, containing blends of HPC and PEO, enhanced the effectiveness of the antimicrobials a maximum of 5-fold toward the inhibition of cell adherence of C. albicans to mammalian cells/Vero cells. Remarkably, a combination of the two polymers without drug also demonstrated a 38% decrease in cell adhesion to the fungi due to the viscosity and the flexibility of the polymers. Drug-release profiles indicated that both drug concentrations were above the minimum inhibitory concentration (MIC) for C. albicans within 10 minutes and was maintained for over 10 hours. In addition, based on the IC₅₀ and MIC values, it was observed that the antifungal activities of both drugs were increased significantly in the ADA systems.

Conclusions

Based on these findings, the ADA system may be used for primary, prophylaxis or adjunct treatment of oral or pharyngeal candidiasis via controlled-release of the antifungal agent from the polymer matrix.

Url:

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5629914

DOI: 10.1517/17425247.2014.949235
PubMed: 25169007
PubMed Central: 5629914

Affiliations:

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<front><div type="abstract" xml:lang="en"><sec id="S1"><title>Objectives</title>
<p id="P1">The overall goal of this research was to produce a stable hot-melt extruded “Antifungal Denture Adhesive film” (ADA) system for the treatment of oral candidiasis.</p>
</sec>
<sec id="S2"><title>Methods</title>
<p id="P2">The ADA systems with hydroxypropyl cellulose (HPC) and/or polyethylene oxide (PEO) containing clotrimazole (10%) or nystatin (10%) were extruded utilizing a lab scale twin-screw hot-melt extruder. Rolls of the antifungal-containing films were collected and subsequently die-cut into shapes adapted for a maxillary (upper) and mandibular (lower) denture.</p>
</sec>
<sec id="S3"><title>Results</title>
<p id="P3">DSC and PXRD results indicated that the crystallinity of both APIs was changed to amorphous phase after hot-melt extrusion. The ADA system, containing blends of HPC and PEO, enhanced the effectiveness of the antimicrobials a maximum of 5-fold toward the inhibition of cell adherence of <italic>C. albicans</italic>
 to mammalian cells/Vero cells. Remarkably, a combination of the two polymers without drug also demonstrated a 38% decrease in cell adhesion to the fungi due to the viscosity and the flexibility of the polymers. Drug-release profiles indicated that both drug concentrations were above the minimum inhibitory concentration (MIC) for <italic>C. albicans</italic>
 within 10 minutes and was maintained for over 10 hours. In addition, based on the IC<sub>50</sub>
 and MIC values, it was observed that the antifungal activities of both drugs were increased significantly in the ADA systems.</p>
</sec>
<sec id="S4"><title>Conclusions</title>
<p id="P4">Based on these findings, the ADA system may be used for primary, prophylaxis or adjunct treatment of oral or pharyngeal candidiasis via controlled-release of the antifungal agent from the polymer matrix.</p>
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Development of an Antifungal Denture Adhesive Film for Oral Candidiasis Utilizing Hot Melt Extrusion Technology

Development of an Antifungal Denture Adhesive Film for Oral Candidiasis Utilizing Hot Melt Extrusion Technology

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