A well-designed drug delivery platform improves the pharmacological properties of therapeutics. Here, we report a biodegradable interpenetrating polymer network (IPN) microbeads delivery technology developed by crosslinking a polymer blend of poly(vinyl alcohol), xanthan gum, and sodium alginate to enhance the solubility of poorly soluble drugs. The microbeads effectively improve the solubility of a model BCS Class IV drug, norfloxacin, known for its low solubility and low permeability. Differential scanning calorimetry, powdered X-ray diffractometry, and FT-IR data showed that the IPN microbeads solubilised and encapsulated the drug within the network. We found over 83% encapsulation efficiency for norfloxacin and this efficiency increases with the concentration of polymer. Ex vivo experiments using caprine intestine revealed that the IPN microbeads adhered to the intestinal epithelium, a mucoadhesive behaviour that could be beneficial to the drug pharmacokinetics while in vitro experiments in phosphate buffer show that the IPN enables significant drug release. We believe that these IPN microbeadsare an excellent drug delivery system to solubilise norfloxacin, ensure adhesion to the intestinal wall, thereby localising the drug release to enhance bioavailability of poorly soluble drugs.

Graphical abstract

精心设计的给药平台可改善治疗剂的药理特性。在这里，我们报告通过交联聚乙烯醇，黄原胶和海藻酸钠的聚合物共混物以提高难溶性药物的溶解度而开发的可生物降解的互穿聚合物网络（IPN）微珠递送技术。微珠可有效提高模型BCS IV类药物诺氟沙星的溶解度，该药物以其低溶解度和低渗透性而闻名。差示扫描量热法，X射线粉末衍射法和FT-IR数据表明，IPN微珠溶解并封装了网络中的药物。我们发现诺氟沙星的包封率超过83％，并且该效率随聚合物浓度的增加而增加。使用山羊肠的离体实验显示IPN微珠粘附在肠上皮上，这种粘膜粘附行为可能对药物的药代动力学有利，而在磷酸盐缓冲液中进行的体外实验表明IPN可以显着释放药物。我们认为这些IPN微珠是出色的药物递送系统，可溶解诺氟沙星，确保与肠壁的粘附，从而使药物释放局部化，从而提高难溶性药物的生物利用度。

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