Nanoparticulated Systems Based on Natural Polymers Loaded with Miconazole Nitrate and Lidocaine for the Treatment of Topical Candidiasis

• Published in: AAPS PharmSciTech Vol. 21; no. 7; p. 278
• Main Authors: Tejada, G., Barrera, M. G., García, P., Sortino, M., Lamas, M. C., Lassalle, V., Alvarez, V., Leonardi, D.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 08.10.2020
• Subjects: Antifungal Agents - administration & dosage; Antifungal Agents - chemistry; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Calorimetry, Differential Scanning; Candida albicans - isolation & purification; Candidiasis - drug therapy; Chitosan; Humans; Lidocaine - administration & dosage; Lidocaine - chemistry; Miconazole - administration & dosage; Miconazole - chemistry; Nanoparticles - administration & dosage; Nanoparticles - chemistry; Pharmacology/Toxicology; Pharmacy; Polymers - chemistry; Research Article; X-Ray Diffraction; chitosan; antifungal; nano-particle; gelatin
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-020-01826-6

People with weakened immune systems are at risk of developing candidiasis which is a fungal infection caused by several species of Candid a genus. In this work, polymeric nanoparticles containing miconazole nitrate and the anesthetic lidocaine clorhydrate were developed. Miconazole was chosen as a typical drug to treat buccopharyngeal candidiasis whereas lidocaine may be useful in the management of the pain burning, and pruritus caused by the infection. Nanoparticles were synthesized using chitosan and gelatin at different ratios ranging from 10:90 to 90:10. The nano-systems presented nanometric size (between 80 and 300 nm in water; with polydispersion index ranging from 0.120 to 0.596), and positive Z potential (between 20.11 and 37.12 mV). The determined encapsulation efficiency ranges from 65 to 99% or 34 to 91% for miconazole nitrate and lidocaine clorhydrate, respectively. X-ray diffraction and DSC analysis suggested that both drugs were in amorphous state in the nanoparticles. Finally, the systems fitted best the Korsmeyer–Peppas model showing that the release from the nanoparticles was through diffusion allowing a sustained release of both drugs and prolonged the activity of miconazole nitrate over time against Candida albicans for at least 24 h.