Institute of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.
Institute of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.
Eur J Pharm Sci. 2023 Oct 1;189:106555. doi: 10.1016/j.ejps.2023.106555. Epub 2023 Aug 4.
pH-responsive hydrogels have become effective and attractive materials for the controlled release of drugs at pre-determined destinations. In the present study, a novel hydrogel system based on Prunus armeniaca gum (PAG) and acrylic acid (AA) was prepared by a free radical mechanism using N, N-methylene bisacrylamide (MBA) as cross-linker and potassium persulfate (KPS) as initiator. A series of hydrogels varying PAG, AA, and MBA concentration was developed to determine the impact of these components. Formulated hydrogels were characterized for pH-responsive swelling, drug release, gel content, and porosity. Structural analysis was performed by FTIR, XRD, and SEM analysis. TGA study was applied to assess thermal stability. Oral acute toxicity and in vivo drug release were performed in rabbits. Hydrogels exhibited pH-dependent swelling and drug release. Swelling, drug loading and release, and porosity increased by increasing PAG and AA concentration while decreased by increasing MBA. The gel content of formulations was increased by increasing all three components. FTIR studies confirmed the development of copolymeric networks and the loading of drug. XRD studies revealed that hydrogels were amorphous, and the crystalline drug was changed into an amorphous form during loading. TGA results indicated that hydrogels were stable up to 600 °C. Acute oral toxicity results confirm that hydrogels were nontoxic up to a dose of 2 g/kg body weight in rabbits. The pharmacokinetic evaluation revealed that hydrogels prolonged the availability of the drug and the peak plasma concentration of the drug was obtained in 6 h as compared to the oral solution of the drug. Tramadol hydrochloride (THC) was used as a model drug. Hence, pH-responsive swelling and release, nontoxic nature and improved pharmacokinetics support that PAG-based hydrogels may be considered as potential controlled-release polymeric carriers.
pH 响应水凝胶已成为在预定部位控制药物释放的有效且有吸引力的材料。在本研究中，通过自由基机制，使用 N，N-亚甲基双丙烯酰胺（MBA）作为交联剂和过硫酸钾（KPS）作为引发剂，制备了基于杏树胶（PAG）和丙烯酸（AA）的新型水凝胶系统。制备了一系列具有不同 PAG、AA 和 MBA 浓度的水凝胶，以确定这些成分的影响。对配方水凝胶进行了 pH 响应溶胀、药物释放、凝胶含量和孔隙率的特性研究。通过 FTIR、XRD 和 SEM 分析进行结构分析。TGA 研究用于评估热稳定性。在兔子中进行了口服急性毒性和体内药物释放研究。水凝胶表现出 pH 依赖性溶胀和药物释放。通过增加 PAG 和 AA 的浓度，溶胀、药物负载和释放以及孔隙率增加，而通过增加 MBA 则降低。所有三种成分的增加都增加了制剂的凝胶含量。FTIR 研究证实了共聚物网络的发展和药物的负载。XRD 研究表明水凝胶为无定形，药物在负载过程中由结晶态转变为无定形态。TGA 结果表明水凝胶在 600°C 以下稳定。急性口服毒性结果证实，水凝胶在兔子中高达 2g/kg 体重的剂量下无毒性。药代动力学评价表明，水凝胶延长了药物的有效性，与药物的口服溶液相比，药物的峰值血浆浓度在 6 小时内获得。盐酸曲马多（THC）被用作模型药物。因此，pH 响应溶胀和释放、无毒性质和改善的药代动力学表明，基于 PAG 的水凝胶可用作潜在的控释聚合物载体。
