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1.
Braz. J. Pharm. Sci. (Online) ; 56: e17509, 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1132046

RESUMO

Amphotericin B is a broad spectrum antifungal agent used to treat fungal infections. Organogel is a semisolid preparation in which the apolar phase gets immobilized within spaces of the three-dimensional structure. The current study aimed at the formulation and comparative evaluation of sorbitan monostearate organogels and pluronic lecithin organogels (PLO). Different compositions of span 60 based organogels were prepared by varying the concentrations of the span 60 and PLO gels were prepared by varying the concentration of Pluronic F 127. The developed organogels were subjected to various characteristics such as pH, viscosity, spreadability, extrudability, and drug release studies. The optimized formulations were evaluated against Candida albicans and carried out ex vivo release study. The optimized formulation was selected from span 60 based organogels, and pluronic lecithin organogels were S1 and P1, respectively. The optimized formulation (S1) showed effective inhibition against Candida albicans. The skin irritation test was carried out on albino mice for optimized formulations and results showed that no irritation to the skin. Based on the results, organogels prepared by sorbitan monostearate showed better antifungal activity, and also all the formulations were found to be stable and safe throughout the study period.


Assuntos
Pele , Candida albicans/classificação , Anfotericina B/agonistas , Crescimento e Desenvolvimento , Antifúngicos/análise , Viscosidade , Liberação Controlada de Fármacos , Micoses/patologia
2.
Int J Pharm ; 556: 9-20, 2019 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-30529659

RESUMO

Coenzyme Q10 (CoQ10) is a mitochondrial respiratory cofactor and potent endogenous antioxidant. In CoQ10-deficient patients, early treatment with high-oral doses (5-50 mg/kg/day) can limit the progression of renal disease and the onset of neurological manifestations. Crystalline CoQ10 is lipophilic, water-insoluble, and poorly absorbed in the gut. Here, CoQ10 showed low bulk density, another important disadvantage in solid oral formulations. Thus, we propose the use of oleogels to maintain dissolved a high-dose of CoQ10 in medium-chain triglyceride (MCT) oil, using ethylcellulose (EC) for gelling, and a surfactant (sorbitan monostearate -SMS- or lecithin). "True gels" were only obtained with the surfactant presence. Thermoreversible oleogels with 1 g of dissolved CoQ10 per 5 g-disk were successfully developed with proved stability and solubility for 12 months (25.0 °C). SMS was better than lecithin as a surfactant because it allowed lower syneresis, higher CoQ10 retention for 12 months, and notably higher oxidative-stability of the MCT-oil, best immobilized by its true gel network. Plastic deformation without fracture was determined under compression, emulating the soft deformation behavior inside the mouth. SMS-oleogels allowed loading a maximal solubilized CoQ10 dose with maximal stability, and may be easier to swallow by CoQ10-deficient patients who suffer from secondary dysphagia.


Assuntos
Antioxidantes/administração & dosagem , Celulose/análogos & derivados , Tensoativos/química , Ubiquinona/análogos & derivados , Administração Oral , Antioxidantes/química , Celulose/química , Química Farmacêutica/métodos , Relação Dose-Resposta a Droga , Estabilidade de Medicamentos , Hexoses/química , Lecitinas/química , Compostos Orgânicos , Solubilidade , Triglicerídeos/química , Ubiquinona/administração & dosagem , Ubiquinona/química
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