title: Miconazole-loaded nanostructured lipid carriers (NLC) for local delivery to the oral mucosa: improving antifungal activity.
abstract: Miconazole is a widely used antifungal agent with poor aqueous solubility, which requires the development of drug delivery systems able to improve its therapeutic activity. For this purpose, a miconazole-loaded nanostructured lipid carriers (NLC) dispersion was prepared and characterized. Further, the dispersion was used to prepare a NLC-based hydrogel formulation proposed as an alternative system to improve the local delivery of miconazole to the oral mucosa. NLC dispersion showed particles in the nanometer range (≈ 200 nm) with low polidispersity index (<0.3), good physical stability and high encapsulation efficiency (>87%). A controlled miconazole release was observed from NLC and NLC-based hydrogel formulations, in contrast to a commercial oral gel formulation, which demonstrated a faster release. Additionally, it was observed that the encapsulation of miconazole in the NLC improved its antifungal activity against Candida albicans. Therefore, it was demonstrated that the encapsulation of miconazole in NLC allows for obtaining the same therapeutic effect of a commercial oral gel formulation, using a 17-fold lower dose of miconazole.
authors: Trás-os-Montes and Alto Douro University (UTAD), Apartado 1013, P-5001-801 Vila Real, Portugal.
authors: A I
authors: AI
authors: Mendes
authors: CEBIMED, Faculty of Health Sciences, Fernando Pessoa University, Rua Carlos da Maia, 296, P-4200-1250 Porto, Portugal; Laboratory of Pharmaceutical Technology/Centre of Research in Pharmaceutical Sciences, Faculty of Pharmacy, Porto University, Rua Jorge de Viterbo Ferreira, 228, 4050-313 Porto, Portugal. Electronic address: acsilva@ufp.edu.pt.
authors: A C
authors: AC
authors: Silva
authors: CEBIMED, Faculty of Health Sciences, Fernando Pessoa University, Rua Carlos da Maia, 296, P-4200-1250 Porto, Portugal; Paralab, SA, Porto, Portugal.
authors: J A M
authors: JA
authors: Catita
authors: CEBIMED, Faculty of Health Sciences, Fernando Pessoa University, Rua Carlos da Maia, 296, P-4200-1250 Porto, Portugal; CEQUIMED-UP, Medicinal Chemistry Center, Faculty of Pharmacy, Porto University, Rua Jorge de Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
authors: F
authors: F
authors: Cerqueira
authors: CEBIMED, Faculty of Health Sciences, Fernando Pessoa University, Rua Carlos da Maia, 296, P-4200-1250 Porto, Portugal.
authors: C
authors: C
authors: Gabriel
authors: CEBIMED, Faculty of Health Sciences, Fernando Pessoa University, Rua Carlos da Maia, 296, P-4200-1250 Porto, Portugal; Institute of Biotechnology and Bioengineering, Centre of Genetics and Biotechnology, Trás-os-Montes and Alto Douro University (IBB/CGB-UTAD), Apartado 1013, P-5001-801 Vila Real, Portugal. Electronic address: cmlopes@ufp.edu.pt.
authors: C M
authors: CM
authors: Lopes
mesh_terms: D000935:Antifungal Agents / Q000494:pharmacology*; D002152:Calorimetry, Differential Scanning; D002176:Candida albicans / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D020100:Hydrogels / Q000494:pharmacology; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D008825:Miconazole / Q000494:pharmacology*; D009061:Mouth Mucosa / Q000187:drug effects*; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D010919:Placebos; D012212:Rheology / Q000187:drug effects; D055672:Static Electricity
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D020100:Hydrogels; D008055:Lipids; D010919:Placebos; D008825:Miconazole
keywords: Antifungal activity; Controlled release; Hydrogel; Miconazole; Nanostructured lipid carriers; Oral mucosa