Department of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Punjab, Pakistan.
College of Pharmacy, University of Sargodha, Sargodha, Punjab, Pakistan.
AAPS PharmSciTech. 2021 Jun 15;22(5):181. doi: 10.1208/s12249-021-02054-2.
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.
在这项研究中，两种亲水性聚合物羟丙基甲基纤维素和β-环糊精（β-CD）被用于合成对响应性和海绵状聚合物基质。多孔和刺激响应性聚合物网络的开发是为了显著提高阿昔洛韦（ACV）的溶解度。通过自由基聚合技术成功地进行了接枝。通过百分比包封效率、药物负载、溶解度研究、FTIR、粉末 X 射线衍射、TGA、DSC、XRD、SEM、溶胀研究和体外研究对海绵状基质进行了表征。进行急性口服毒性研究以确定制备的 HPMC-βCD-g-poly(AMPS)制剂口服给药的安全性。在 SEM 图像中描绘了多孔和海绵状结构。通过 FTIR、TGA 和 DSC 光谱分析了成分和药物（ACV）的络合和热稳定性。XRD 分析表明海绵状基质中阿昔洛韦的结晶度降低。优化制剂的粒径在 197 ± 2.55nm 范围内。与参比产品的显著差异表明，开发的海绵状基质显著增强了药物的溶解度和释放特性。毒性研究证实，开发的海绵状基质是非毒性的，与生物系统相容。高效的制备方法、增强的溶解度、优异的物理化学特性、高溶解率和非毒性的 HPMC-βCD-g-poly(AMPS)海绵状基质可能是一种有前途的用于口服递送难溶性药物的方法。
