Pecora Tiziana Maria Grazia, Ragazzo Barbara, Bertin Walter, Ragonese Alessia, Mascagni Marco, Maffei Paola, Pignatello Rosario
Labomar SpA, via Nazario Sauro 35/I, Istrana, 31036 Treviso, Italy.
Alfasigma SpA, via Ragazzi del '99, 40133 Bologna, Italy.
J Funct Biomater. 2021 Apr 28;12(2):28. doi: 10.3390/jfb12020028.
: The study aimed at assessing the mucoadhesive properties and the barrier effect of a formulation, labelled as AL2106, containing sodium chondroitin sulfate (ChS), xyloglucan from tamarind seed extract, and glycerol, by evaluating the capacity to adhere to a layer of mucin, the rheological synergism and the barrier effect in comparison to the marketed Esoxx One medical device. AL2106 is a medical device distributed by Alfasigma SpA, Italy with REF FTP57 (Manufacturer: Labomar SpA); it is analogous to Esoxx One medical device: the two products are drinkable solutions that, after swallowing, adhere to the esophageal mucosa, protecting it from the corrosive effect of the gastric acid reflux. AL2106 has been conceived to be better performing in terms of duration of the barrier effect compared to Esoxx One. : The mucoadhesive properties, rheological behavior, buffering capacity against acidity, and film-forming ability with the resultant protecting effect on esophagus mucosa (caffeine permeation test) was compared between the two products. : The mucoadhesivity of the formulations was shown in vitro: both remained adherent to a mucin layer, also when the support was rotated by 90°, and when the film layer was washed with water, intended to simulate the washout due to swallowing. AL2106 showed a good buffering efficacy, being able to absorb at least 50% of its weight of 0.03 M HCl while maintaining the pH above 4. The film-forming effect and barrier properties of AL2106 and Esoxx One were confirmed by an in vitro study on reconstructed human esophageal epithelium. A greater film-forming efficacy of AL2106, lasting for at least 5 h, than Esoxx One was observed. Noteworthy, the barrier function of esophageal tissues was shown to be preserved after the application of both formulations. : The combination of ChS with the mucoadhesive glycerol-xyloglucan complex and other excipients, which contribute to the barrier effect and to mucoadhesion, contained in AL2106, allowed a longer-lasting protective effect than Esoxx One, proving its effectivity and safety for oral use.
该研究旨在通过评估与市售的Esoxx One医疗器械相比，含有硫酸软骨素（ChS）、罗望子种子提取物中的木葡聚糖和甘油的名为AL2106的制剂的粘膜粘附特性和屏障作用，来评估其对粘蛋白层的粘附能力、流变学协同作用和屏障作用。AL2106是一种由意大利的Alfasigma SpA公司经销的医疗器械，产品编号为REF FTP57（制造商：Labomar SpA）；它与Esoxx One医疗器械类似：这两种产品都是可饮用溶液，吞咽后会粘附在食管粘膜上，保护其免受胃酸反流的腐蚀作用。与Esoxx One相比，AL2106在屏障作用持续时间方面表现更佳。比较了两种产品的粘膜粘附特性、流变行为、对酸度的缓冲能力以及形成薄膜的能力及其对食管粘膜的保护作用（咖啡因渗透试验）。两种制剂的粘膜粘附性在体外得到了证明：当载体旋转90°时，以及当薄膜层用水冲洗时（旨在模拟吞咽导致的冲洗），它们都能保持粘附在粘蛋白层上。AL2106显示出良好的缓冲效果，能够吸收至少其重量50%的0.03 M盐酸，同时将pH值保持在4以上。通过对重建的人食管上皮进行体外研究，证实了AL2106和Esoxx One的成膜效果和屏障特性。观察到AL2106的成膜效果更佳，持续至少5小时，优于Esoxx One。值得注意的是，两种制剂应用后食管组织的屏障功能均得以保留。AL'2106中ChS与粘膜粘附性甘油 - 木葡聚糖复合物以及其他有助于屏障作用和粘膜粘附的辅料的组合，产生了比Esoxx One更持久的保护作用，证明了其口服使用的有效性和安全性。
