National Center for Radiation Research and Technology (NCRRT), Atomic Energy Authority, P.O. Box 29, Nasr City, Cairo, Egypt.
Drug Deliv Transl Res. 2018 Jun;8(3):525-535. doi: 10.1007/s13346-017-0468-2.
In the present study, L-arginine/acrylic acid (Arg/AAc) batch hydrogel was successfully prepared by gamma irradiation for transdermal delivery of propranolol HCl in hypertensive rats. The resulted system has been characterized by FTIR to confirm the hydrogel formation. The swelling behavior of the prepared hydrogels was investigated as a function of time and pH. The kinetics of swelling has been investigated. In vivo pharmacokinetics evaluation, skin irritation test, and histopathological studies were investigated. Furthermore, the antihypertensive efficacy of transdermal propranolol-loaded Arg/AAc hydrogel on methyl prednisolone acetate-induced hypertensive rats was evaluated. It was found that the prepared patches exhibited a sustained release of the drug into systemic circulation over oral route which is subjected to hepatic first-pass metabolism, coupled with a short plasma half-life. Transdermal administration displayed a prolonged antihypertensive effect in spontaneously hypertensive rats. Moreover, the skin irritation test and histopathological examination indicated that the prepared patches are not irritant and can be safely applied on the skin. These results indicated that the hydrogel system composed of Arg and AAc has potential as a transdermal delivery system.
在本研究中，通过γ辐照成功制备了 L-精氨酸/丙烯酸（Arg/AAc）批凝胶，用于盐酸普萘洛尔在高血压大鼠中的透皮给药。通过傅里叶变换红外光谱（FTIR）对所得系统进行了表征，以确认水凝胶的形成。研究了制备的水凝胶的溶胀行为随时间和 pH 值的变化。研究了溶胀动力学。进行了体内药代动力学评价、皮肤刺激性试验和组织病理学研究。此外，还评估了经皮负载盐酸普萘洛尔的 Arg/AAc 水凝胶对醋酸甲基强的松龙诱导的高血压大鼠的降压效果。结果发现，与口服途径下受肝脏首过代谢影响且血浆半衰期较短的药物相比，制备的贴片在全身循环中表现出药物的持续释放。经皮给药在自发性高血压大鼠中显示出延长的降压作用。此外，皮肤刺激性试验和组织病理学检查表明，所制备的贴片无刺激性，可安全应用于皮肤。这些结果表明，由 Arg 和 AAc 组成的水凝胶系统具有作为透皮给药系统的潜力。
