Department of Pharmaceutical Technology, A. P, Neplyubin Institute of Pharmacy, I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation (Sechenov University), Moscow, Russia.
Bull Exp Biol Med. 2023 Jan;174(3):337-340. doi: 10.1007/s10517-023-05704-6. Epub 2023 Feb 1.
We studied the potential of using a salt form of chitosan as a pH-sensitive in situ matrix. Among common chitosan salts obtained by heterogeneous synthesis, chitosan formate exhibiting the highest pH-sensitivity was selected. However, the low mucoadhesion strength of the composition, as well as high pH required for the phase transition necessitate designing a polycomponent compound with a poloxamer to additionally provide a thermosensitive phase transition. Compared with the use of pure poloxamer, the chitosan complex demonstrated improved mucoadhesion in in vitro studies, and the phase transition parameters were optimal for intranasal administration. An in vivo study revealed no locally irritating effect of the composition, which allows its further development.
我们研究了使用壳聚糖盐作为 pH 敏感原位基质的潜力。在通过非均相合成获得的常见壳聚糖盐中，选择了具有最高 pH 敏感性的壳聚糖甲酸盐。然而，该组合物的粘膜粘附强度低，以及相变所需的高 pH 值都需要设计一种包含泊洛沙姆的多组分化合物，以额外提供热敏相变。与使用纯泊洛沙姆相比，壳聚糖复合物在体外研究中表现出更好的粘膜粘附性，并且相变参数最适合鼻内给药。体内研究表明该组合物没有局部刺激性，这使其可以进一步开发。
