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AAPS PharmSciTech ; 25(6): 172, 2024 Jul 24.
Artículo en Inglés | MEDLINE | ID: mdl-39044025

RESUMEN

The goal of the present study was to prepare meloxicam (MX) entrapped hybrid particles (HPs) to enhance intestinal permeation and anti-inflammatory activity. MX-HPs were prepared by nanoprecipitation method using lipid, chitosan, poloxamer, and TPGS. The formulations (MX-HPs1, MX-HPs2, MX-HPs3) were evaluated for particle size, entrapment efficiency, and drug release to select the optimized composition and further evaluated for permeation study, stability study, morphology, interaction study, and anti-inflammatory activity by carrageenan-induced rat paw edema test. The prepared MX-HPs showed nano sized particles (198.5 ± 3.7 to 223.8 ± 2.1 nm) and PDI (<0.3), zeta potential (16.5 ± 2.7 to 29.1 ± 3.6 mV), and high entrapment efficiency (75.1 ± 4.7 to 88.5 ± 3.9%). The surface morphology was assessed by transmission electron microscopy and showed non-aggregated particles. Infra-red (IR) spectroscopy of pure MX as well as formulation revealed no drug-polymer interaction and X-ray diffraction confirmed the conversion of crystalline MX into amorphous form. The release study data revealed prolonged MX release for 24 h. The selected optimized hybrid particles (MX-HPs2) revealed a 2.3-fold improved enhancement ratio than free MX. The storage stability and gastrointestinal stability data demonstrated a stable formulation in SIF as well as SGF. The anti-inflammatory activity showed better therapeutic action than pure MX dispersion. From the study, it can be concluded that the prepared MX-HPs may be a promising delivery system for MX in treating inflammatory disorders.


Asunto(s)
Antiinflamatorios no Esteroideos , Liberación de Fármacos , Meloxicam , Nanopartículas , Tamaño de la Partícula , Meloxicam/administración & dosificación , Meloxicam/farmacología , Meloxicam/química , Animales , Ratas , Nanopartículas/química , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/química , Química Farmacéutica/métodos , Masculino , Portadores de Fármacos/química , Tiazinas/administración & dosificación , Tiazinas/química , Tiazinas/farmacología , Tiazinas/farmacocinética , Poloxámero/química , Tiazoles/química , Tiazoles/farmacología , Quitosano/química , Edema/tratamiento farmacológico , Lípidos/química , Ratas Wistar , Carragenina/química , Vitamina E/química , Vitamina E/farmacología , Estabilidad de Medicamentos
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