Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/Prof. García González, n.º 2, 41012 Sevilla, Spain.
Departamento de Ingeniería Química, Facultad de Química, Universidad de Sevilla, 41012 Sevilla, Spain.
Int J Mol Sci. 2023 Jan 23;24(3):2281. doi: 10.3390/ijms24032281.
An increase in resistance to key antibiotics has made the need for novel treatments for the gastric colonization of () a matter of the utmost urgency. Recent studies tackling this topic have focused either on the discovery of new compounds to ameliorate therapeutic regimes (such as vonoprazan) or the synthesis of gastroretentive drug delivery systems (GRDDSs) to improve the pharmacokinetics of oral formulations. The use of semi-interpenetrating polymer networks (semi-IPNs) that can act as super-porous hydrogels for this purpose is proposed in the present work, specifically those displaying low ecological footprint, easy synthesis, self-floating properties, high encapsulation efficiency for drugs such as amoxicillin (AMOX), great mucoadhesiveness, and optimal mechanical strength when exposed to stomach-like fluids. To achieve such systems, biodegradable synthetic copolymers containing acid-labile monomers were prepared and interpenetrated with guar gum (GG) in a one-pot polymerization process based on thiol-ene click reactions. The resulting matrices were characterized by SEM, GPC, TGA, NMR, and rheology studies, and the acidic hydrolysis of the acid-sensitive polymers was also studied. Results confirm that some of the obtained matrices are expected to perform optimally as GRDDSs for the sustained release of active pharmaceutical ingredients at the gastrointestinal level, being a priori facilitated by its disaggregation. Therefore, the optimal performance of these systems is assessed by varying the molar ratio of the labile monomer in the matrices.
抗生素耐药性的增加使得迫切需要寻找新的治疗方法来应对()胃部定植的问题。最近针对这一课题的研究主要集中在发现新的化合物来改善治疗方案(如沃诺拉赞)或合成胃滞留型药物传递系统(GRDDS)以改善口服制剂的药代动力学。本工作提出了使用半互穿聚合物网络(semi-IPNs)作为超多孔水凝胶来达到这一目的,特别是那些显示出低生态足迹、易于合成、自浮特性、对阿莫西林(AMOX)等药物具有高包封效率、良好的黏膜粘附性以及在暴露于类似胃部的液体时具有最佳机械强度的 semi-IPNs。为了实现这些系统,我们制备了含有酸敏感单体的可生物降解的合成共聚物,并在基于硫醇-烯点击反应的一锅聚合过程中与瓜尔胶(GG)互穿。通过 SEM、GPC、TGA、NMR 和流变学研究对所得的基质进行了表征,并研究了酸敏感聚合物的酸性水解。结果证实,一些获得的基质有望作为 GRDDS 发挥最佳性能,以在胃肠道水平上实现活性药物成分的持续释放,并且通过其解聚来促进药物释放。因此,通过改变基质中不稳定单体的摩尔比来评估这些系统的最佳性能。