Miconazole Nitrate Microparticles in Lidocaine Loaded Films as a Treatment for Oropharyngeal Candidiasis
Guillermo Tejada,
Natalia L. Calvo,
Mauro Morri,
Maximiliano Sortino,
Celina Lamas,
Vera A. Álvarez,
Darío Leonardi
Affiliations
Guillermo Tejada
Grupo Materiales Compuestos Termoplásticos, Instituto de Investigaciones en Ciencia y Tecnología de Materiales, Av. Colón 10850, Mar Del Plata 7600, Argentina
Natalia L. Calvo
Instituto de Química Rosario, Suipacha 570, Rosario 2000, Argentina
Mauro Morri
Planta Piloto de Producción de Medicamentos, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, Rosario 2000, Argentina
Maximiliano Sortino
Centro de Referencia de Micología, Área Farmacognosia, Departamento Química Orgánica, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, Rosario 2000, Argentina
Celina Lamas
Instituto de Química Rosario, Suipacha 570, Rosario 2000, Argentina
Vera A. Álvarez
Grupo Materiales Compuestos Termoplásticos, Instituto de Investigaciones en Ciencia y Tecnología de Materiales, Av. Colón 10850, Mar Del Plata 7600, Argentina
Darío Leonardi
Instituto de Química Rosario, Suipacha 570, Rosario 2000, Argentina
Oral candidiasis is an opportunistic infection that affects mainly individuals with weakened immune system. Devices used in the oral area to treat this condition include buccal films, which present advantages over both oral tablets and gels. Since candidiasis causes pain, burning, and itching, the purpose of this work was to develop buccal films loaded with both lidocaine (anesthetic) and miconazole nitrate (MN, antifungal) to treat this pathology topically. MN was loaded in microparticles based on different natural polymers, and then, these microparticles were loaded in hydroxypropyl methylcellulose-gelatin-based films containing lidocaine. All developed films showed adequate adhesiveness and thickness. DSC and XRD tests suggested that the drugs were in an amorphous state in the therapeutic systems. Microparticles based on chitosan-alginate showed the highest MN encapsulation. Among the films, those containing the mentioned microparticles presented the highest tensile strength and the lowest elongation at break, possibly due to the strong interactions between both polymers. These films allowed a fast release of lidocaine and a controlled release of MN. Due to the latter, these systems showed antifungal activity for 24 h. Therefore, the treatment of oropharyngeal candidiasis with these films could reduce the number of daily applications with respect to conventional treatments.