RESUMEN
AIM: Nanostructured lipid carriers in-gel (NLCs-gel) were prepared to enhance and improve the ocular delivery of dexamethasone. Materials & methods: NLCs containing dexamethasone prepared by high-pressure homogenization were characterized and dispersed into thermosensitive gels (Pluronic F127 and F68 as gels material). In vitro drug release studies, ocular irritation tests, ex vivo corneal penetration and drug dynamics of NLCs and NLCs-gel were evaluated in aqueous humor. RESULTS: NLCs-gel exhibited a rapid sol-gel transition at 34.4°C and presented nano-sized, narrowly distributed particles. Corneal penetration studies revealed steady sustained drug release (Ritger-Peppas); NLCs-gel increased ocular bioavailability by prolonging precorneal retention time and improving corneal permeation. CONCLUSION: These findings suggest developing NLCs-gel for potential treatment of posterior segment eye diseases.
Asunto(s)
Dexametasona/administración & dosificación , Oftalmopatías/tratamiento farmacológico , Nanoestructuras/administración & dosificación , Soluciones Oftálmicas/administración & dosificación , Animales , Disponibilidad Biológica , Quitosano/administración & dosificación , Quitosano/química , Córnea/efectos de los fármacos , Córnea/patología , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/química , Dexametasona/química , Portadores de Fármacos/administración & dosificación , Portadores de Fármacos/química , Liberación de Fármacos/efectos de los fármacos , Humanos , Lípidos/administración & dosificación , Lípidos/química , Nanoestructuras/química , Soluciones Oftálmicas/química , ConejosRESUMEN
OBJECTIVE: To study the formulation of Naoxuekang dispersible tablets. METHODS: The formulation was determined by pre-processing leech extractum prior to a series of experiments used to screen excipients like bulking agents and disintegrants and so on, and by adding disintegrants within and without. RESULTS: Microcrystalline cellulose was determined as the bulking agent, and carboxymethyl cellulose and low-substituted hydroxypropyl cellulose were determined as the disintegrants of Naoxuekang dispersible tablet formula. The average disintegration time and nitrogen content of one tablet were 52 seconds and 5.47 milligrams, respectively. Also disperse homogeneity, weight variation and microbial limit all met the requirements in Ch. P. CONCLUSION: The prepared Naoxuekang dispersible tablet is reasonable in formula, feasible in technology, which meets the quality standards.