Al-Tabakha Moawia M, Khan Shujaat Ali, Ashames Akram, Ullah Hamid, Ullah Kaleem, Murtaza Ghulam, Hassan Nageeb
College of Pharmacy and Health Sciences, Ajman University, P.O. Box 346, Ajman, United Arab Emirates.
Center of Medical and Bio-Allied Health Sciences Research, Ajman University, P.O. Box 346, Ajman, United Arab Emirates.
Pharmaceuticals (Basel). 2021 Mar 8;14(3):234. doi: 10.3390/ph14030234.
Conventional formulations of antiviral drug acyclovir have various limitations such as low bioavailability. The current study was aimed at developing polymeric matrices for the controlled delivery of acyclovir using sericin as polymer and acrylic acid (AA) as a monomer. The free radical polymerization technique was used for hydrogel formulation. Briefly, sericin was chemically cross-linked with acrylic acid. '-'-methylene bis-acrylamide (MBA) and ammonium persulfate (APS) were used as cross-linker and initiator, respectively. FTIR spectra showed that acyclovir was successfully loaded into sericin hydrogel. SEM micrographs revealed that the outer surface was solid-like and smooth. According to DSC thermograms, the developed polymeric network was thermally stable. Amorphous nature of acyclovir was observed in XRD. The pH of medium and reactants' concentration affected swelling dynamics and acyclovir release pattern. In addition, drug release occurred through a diffusion-controlled process. Sericin hydrogel suspension was well tolerable up to 3800 mg/kg of rabbits' body weight. Haematology and serum chemistry results were well within the range signifying normal liver and kidney functions. Similarly, histopathology slides of the rabbit's vital organs were also in normal condition without causing any histopathological change. It was concluded from the findings that sericin-co-AA polymeric matrices are ideal for the pH-dependent delivery of acyclovir.
抗病毒药物阿昔洛韦的传统制剂存在各种局限性，如生物利用度低。当前的研究旨在开发以丝胶蛋白为聚合物、丙烯酸（AA）为单体的用于阿昔洛韦控释的聚合物基质。采用自由基聚合技术制备水凝胶。简要地说，丝胶蛋白与丙烯酸进行化学交联。N,N'-亚甲基双丙烯酰胺（MBA）和过硫酸铵（APS）分别用作交联剂和引发剂。傅里叶变换红外光谱（FTIR）表明阿昔洛韦成功负载到丝胶蛋白水凝胶中。扫描电子显微镜（SEM）显微照片显示其外表面呈固体状且光滑。根据差示扫描量热法（DSC）热重曲线，所开发的聚合物网络具有热稳定性。X射线衍射（XRD）显示阿昔洛韦为无定形性质。介质的pH值和反应物浓度影响溶胀动力学和阿昔洛韦的释放模式。此外，药物释放通过扩散控制过程发生。丝胶蛋白水凝胶悬浮液在高达3800 mg/kg兔体重时耐受性良好。血液学和血清化学结果完全在表明肝肾功能正常的范围内。同样，兔重要器官的组织病理学切片也处于正常状态，未引起任何组织病理学变化。从这些发现得出结论，丝胶蛋白-共-AA聚合物基质是阿昔洛韦pH依赖型递送的理想选择。
