A gellan gum derivative as in-situ gelling cationic polymer for nasal drug delivery

黏膜黏附 结冷胶 化学 Zeta电位 聚合物 极限抗拉强度 赋形剂 泊洛沙姆 药物输送 粘附 生物物理学 高分子化学 材料科学 色谱法 有机化学 毒品携带者 纳米技术 复合材料 共聚物 食品科学 纳米颗粒 生物
作者
Max Jelkmann,Christina Leichner,Sergey Zaichik,Flavia Laffleur,Andreas Bernkop‐Schnürch
出处
期刊:International Journal of Biological Macromolecules [Elsevier]
卷期号:158: 1037-1046 被引量:40
标识
DOI:10.1016/j.ijbiomac.2020.04.114
摘要

The aim of the present study was the development of a novel gellan gum derivative exhibiting mucoadhesive properties for nasal application. Accomplishing this, amino groups have been introduced to the polymeric backbone. The resulting synthesis products were characterized in terms of the amount of attached amino groups, regarding hydration, zeta potential and gel characteristics. Mucoadhesiveness was assessed studying rheological synergism, by rotating cylinder and regarding tensile studies. Next to erythrocyte-/cytotoxicity evaluation, the impact on ciliary beat frequency of nasal epithelial cells was investigated. Results revealed coupling rates up to 1259.50 ± 75.98 μmol/g polymer as well as accelerated hydration of the derivatives. Comparing aminated with unmodified gellan, enhanced mucoadhesion was verified by a 32-fold increase in viscosity of polymer/mucus mixtures and by a 14-fold extended mucosal adhesion time. Tensile studies demonstrated a 9-fold higher total work of adhesion and a 3.75-fold elevated maximum detachment force. Cellular membrane was not seriously impaired. CBF studies proved a reversible inhibition due to the application of the novel derivative. According to the outlined findings, aminated gellan gum can be considered as a promising excipient for nasal dosage forms improving drug bioavailability by superior adhesive features.
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