Bi-polymeric Spongy Matrices Through Cross-linking Polymerization: Synthesized and Evaluated for Solubility Enhancement of Acyclovir.
In this study, two hydrophilic polymers hydroxypropyl methyl cellulose and beta-cyclodextrin (β-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-βCD-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-βCD-g-poly(AMPS) spongy matrices may be a promising approach for oral delivery of poorly soluble drugs.
['Asghar|Saima|S|', 'Akhtar|Naveed|N|', 'Minhas|Muhammad Usman|MU|', 'Khan|Kifayat Ullah|KU|']
D000178:Acrylamides D000212:Acyclovir D000284:Administration, Oral D000476:Alkanesulfonates D000818:Animals D000998:Antiviral Agents D004353:Drug Evaluation, Preclinical D065347:Hypromellose Derivatives D008297:Male D010316:Particle Size D058105:Polymerization D011108:Polymers D011817:Rabbits D012995:Solubility D017550:Spectroscopy, Fourier Transform Infrared D014961:X-Ray Diffraction D047392:beta-Cyclodextrins
solubility acyclovir spongy bi-polymeric matrices β-cyclodextrin