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Ann Pharm Fr ; 82(5): 813-821, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38604290

RESUMO

INTRODUCTION: Cryptococcal meningitis is a deadly disease with few treatment options. Its incidence is still high and closely linked to the HIV/AIDS epidemic. This study aimed to develop a mucoadhesive microsphere delivery system for fluconazole for the intranasal route. METHOD: Microspheres of mucoadhesive fluconazole formulation variables such as different amounts of drug concentration and polymer concentration were prepared by a simple emulsion-crosslinking method. The prepared microspheres' surface was characterised by SEM (Scanning electron microscopy) and evaluated for particle size, entrapment efficiency, production yield, infrared spectroscopic study, in-vitro muco-adhesion, and in-vitro drug release. RESULTS: The results showed that formula 1 is the optimal mucoadhesive microsphere preparation, with a particle size of 56.375m, a spherical surface shape, an entrapment efficiency of 99.96%, and a greater mucoadhesive capability during 6-hour evaluation. Furthermore, wash-off examination revealed that the mucoadhesive ability of this delivery system has a long duration and may release the active material at the right time. CONCLUSION: The result of the researches suggesting that the formulation of mucoadhesive microspheres of fluconazole could be used to treat cryptococcal meningitis infection in HIV/AIDS patients.


Assuntos
Adesividade , Administração Intranasal , Antifúngicos , Fluconazol , Meningite Criptocócica , Microesferas , Tamanho da Partícula , Fluconazol/administração & dosagem , Fluconazol/uso terapêutico , Antifúngicos/administração & dosagem , Antifúngicos/uso terapêutico , Meningite Criptocócica/tratamento farmacológico , Humanos , Sistemas de Liberação de Medicamentos , Síndrome da Imunodeficiência Adquirida/complicações , Síndrome da Imunodeficiência Adquirida/tratamento farmacológico , Mucosa Nasal/microbiologia , Mucosa Nasal/metabolismo , Animais , Liberação Controlada de Fármacos , Infecções Oportunistas Relacionadas com a AIDS/tratamento farmacológico
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