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AAPS PharmSciTech ; 22(5): 181, 2021 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-34129154

RESUMEN

In this study, two hydrophilic polymers hydroxypropyl methyl cellulose and beta-cyclodextrin (ß-CD) are used to synthesize highly responsive and spongy polymeric matrices. Porous and stimulus-responsive polymeric network was developed to improve the solubility of acyclovir (ACV) at significant level. Grafting was successfully carried out by free radical polymerization technique. Spongy matrices were characterized by percentage entrapment efficiency, drug loading, solubility studies, FTIR, powder X-ray diffraction, TGA, DSC, XRD, SEM, swelling studies, and in vitro studies. Acute oral toxicity studies were conducted to determine the safety of oral administration of prepared HPMC-ßCD-g-poly(AMPS) formulation. Porous and spongy structures were depicted in SEM images. Complex formation and thermal stability of constituents and drug (ACV) were analyzed by FTIR, TGA, and DSC spectra. XRD analysis revealed reduction in acyclovir crystallinity in spongy matrices. Particle size of optimized formulation was found in the range of 197 ± 2.55 nm. The momentous difference with reference product committed that drug solubility and release characteristics were markedly enhanced by the developed spongy matrices. Toxicity studies endorsed that developed spongy matrices were non-toxic and compatible to biological system. The efficient method of preparation, enhanced solubility, excellent physico-chemical characteristics, high dissolution, and non-toxic HPMC-ßCD-g-poly(AMPS) spongy matrices may be a promising approach for oral delivery of poorly soluble drugs.


Asunto(s)
Acrilamidas/síntesis química , Aciclovir/síntesis química , Alcanosulfonatos/síntesis química , Derivados de la Hipromelosa/síntesis química , Polimerizacion , beta-Ciclodextrinas/síntesis química , Acrilamidas/administración & dosificación , Aciclovir/administración & dosificación , Administración Oral , Alcanosulfonatos/administración & dosificación , Animales , Antivirales/administración & dosificación , Antivirales/síntesis química , Evaluación Preclínica de Medicamentos/métodos , Derivados de la Hipromelosa/administración & dosificación , Masculino , Tamaño de la Partícula , Polímeros/administración & dosificación , Polímeros/síntesis química , Conejos , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Difracción de Rayos X/métodos , beta-Ciclodextrinas/administración & dosificación
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