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Mucopenetrating polymer - Lipid hybrid nanovesicles as subunits in alginate beads as an oral formulation.
Journal of Controlled Release ( IF 10.5 ) Pub Date : 2020-03-31 , DOI: 10.1016/j.jconrel.2020.03.047 Essi Taipaleenmäki 1 , Gustav Christensen 1 , Edit Brodszkij 1 , Sidsel A Mouritzen 1 , Noga Gal 1 , Sidsel Madsen 2 , Mette Skou Hedemann 2 , Tine Ahrendt Knudsen 3 , Henrik Max Jensen 3 , Sofie Laage Christiansen 3 , Flemming Vang Sparsø 3 , Brigitte Städler 1
Journal of Controlled Release ( IF 10.5 ) Pub Date : 2020-03-31 , DOI: 10.1016/j.jconrel.2020.03.047 Essi Taipaleenmäki 1 , Gustav Christensen 1 , Edit Brodszkij 1 , Sidsel A Mouritzen 1 , Noga Gal 1 , Sidsel Madsen 2 , Mette Skou Hedemann 2 , Tine Ahrendt Knudsen 3 , Henrik Max Jensen 3 , Sofie Laage Christiansen 3 , Flemming Vang Sparsø 3 , Brigitte Städler 1
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Crossing the intestinal mucus layer remains a great hurdle in oral drug delivery. The viscous mucus gel protects the body from pathogens but simultaneously traps many types of delivery vehicles, limiting their therapeutic efficacy. We report the assembly of mucopenetrating PEG-based polymer-lipid hybrid vesicles encapsulated in mucoadhesive alginate carriers aiming to increase their residence time in the intestine. The stability of the formulations was evaluated in simulated gastrointestinal conditions, showing negligible subunit leakage in the gastric fluid but a substantial release in the intestinal fluid. Mucopenetration of the free and encapsulated subunits was first demonstrated in vitro in a microfluidic set-up filled with reconstituted porcine mucus and in a mucus-covered co-culture of Caco-2 cells and HT29-MTX-E12 cells. Finally, the free and encapsulated subunits remained adhered in close proximity to the intestinal epithelium after oral administration to rats while the alginate carriers were washed away. In conclusion, the double-encapsulated system with combined mucoadhesive and mucopenetrating properties is a promising alternative drug carrier for oral delivery.
中文翻译：
粘膜渗透性聚合物-藻类微珠中脂质杂合纳米囊泡的亚单位，口服制剂。
穿过肠道粘液层仍然是口服药物递送的一大障碍。粘性粘液凝胶可保护人体免受病原体侵害，但同时会诱捕许多类型的输送媒介，从而限制了其治疗功效。我们报道了组装在黏膜黏附藻酸盐载体中的黏膜渗透性PEG基聚合物-脂质杂化囊泡的组装，旨在增加其在肠道中的停留时间。在模拟胃肠道条件下评估制剂的稳定性，显示在胃液中亚单位的渗漏可忽略不计，但在肠液中大量释放。游离和封装的亚基的粘膜渗透率首先在体外以重组猪粘液填充的微流体装置中以及在粘液覆盖的Caco-2细胞和HT29-MTX-E12细胞的共培养物中证明。最后，口服给予大鼠后，海藻酸盐载体被洗去时，游离的和包封的亚基仍紧密粘附在肠上皮上。总之，具有粘膜粘附和粘膜渗透特性相结合的双囊封系统是一种有希望的口服药物替代载体。
更新日期：2020-03-31
中文翻译：
粘膜渗透性聚合物-藻类微珠中脂质杂合纳米囊泡的亚单位，口服制剂。
穿过肠道粘液层仍然是口服药物递送的一大障碍。粘性粘液凝胶可保护人体免受病原体侵害，但同时会诱捕许多类型的输送媒介，从而限制了其治疗功效。我们报道了组装在黏膜黏附藻酸盐载体中的黏膜渗透性PEG基聚合物-脂质杂化囊泡的组装，旨在增加其在肠道中的停留时间。在模拟胃肠道条件下评估制剂的稳定性，显示在胃液中亚单位的渗漏可忽略不计，但在肠液中大量释放。游离和封装的亚基的粘膜渗透率首先在体外以重组猪粘液填充的微流体装置中以及在粘液覆盖的Caco-2细胞和HT29-MTX-E12细胞的共培养物中证明。最后，口服给予大鼠后，海藻酸盐载体被洗去时，游离的和包封的亚基仍紧密粘附在肠上皮上。总之，具有粘膜粘附和粘膜渗透特性相结合的双囊封系统是一种有希望的口服药物替代载体。
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