Department of Drug Sciences, University of Pavia, Viale Taramelli, 12 Pavia, Italy.
Mar Drugs. 2019 Feb 12;17(2):112. doi: 10.3390/md17020112.
Oral mucositis and esophagitis represent the most frequent and clinically significant complications of cytoreductive chemotherapy and radiotherapy, which severely compromise the patient quality of life. The local application of polymeric gels could protect the injured tissues, alleviating the most painful symptoms. The present work aims at developing in situ gelling formulations for the treatment of oral mucositis and esophagitis. To reach these targets, κ-carrageenan (κ-CG) was selected as a polymer having wound healing properties and able to gelify in the presence of saliva ions, while hydroxypropyl cellulose (HPC) was used to improve the mucoadhesive properties of the formulations. CaCl₂ was identified as a salt able to enhance the interaction between κ-CG and saliva ions. Different salt and polymer concentrations were investigated in order to obtain a formulation having the following features: (i) low viscosity at room temperature to facilitate administration, (ii) marked elastic properties at 37 °C, functional to a protective action towards damaged tissues, and (iii) mucoadhesive properties. Prototypes characterized by different κ-CG, HPC, and CaCl₂ concentrations were subjected to a thorough rheological characterization and to in vitro mucoadhesion and washability tests. The overall results pointed out the ability of the developed formulations to produce a gel able to interact with saliva ions and to adhere to the biological substrates.
口腔黏膜炎和食管炎是细胞减灭化疗和放疗最常见和最具临床意义的并发症,严重影响患者的生活质量。聚合凝胶的局部应用可以保护受损组织,缓解最疼痛的症状。本工作旨在开发用于治疗口腔黏膜炎和食管炎的原位凝胶制剂。为了达到这些目标,κ-卡拉胶(κ-CG)被选择为具有伤口愈合特性的聚合物,并且能够在唾液离子存在下胶凝,而羟丙基纤维素(HPC)用于改善制剂的粘膜粘附特性。氯化钙被确定为一种能够增强κ-CG 和唾液离子之间相互作用的盐。研究了不同的盐和聚合物浓度,以获得具有以下特征的制剂:(i)室温下低粘度,便于给药,(ii)37°C 时具有明显的弹性特性,对受损组织具有保护作用,和(iii)粘膜粘附特性。具有不同 κ-CG、HPC 和 CaCl₂浓度的原型进行了彻底的流变特性和体外粘膜粘附性和可洗性测试。总的结果表明,所开发的制剂能够产生一种能够与唾液离子相互作用并粘附于生物基质的凝胶。