Department of Otolaryngology-Head and Neck Surgery, College of Medicine, Chungnam National University, Daejeon 35015, South Korea.
Polymer Science and Engineering, Chungnam National University, 99 Daehakro, Yuseonggu, Daejeon 34134, South Korea.
Carbohydr Polym. 2022 Feb 15;278:118969. doi: 10.1016/j.carbpol.2021.118969. Epub 2021 Dec 9.
We prepared a new injectable thermogel to enhance the efficiency of inner ear delivery of dexamethasone (DEX). Hexanoyl glycol chitosan (HGC) was synthesized and evaluated as an amphiphilic thermogel (T ~ 32 °C) for use as a solubilizing agent as well as an injectable carrier for intratympanic delivery of the hydrophilic and hydrophobic forms of DEX. Various thermogel formulations with different drug types and concentrations were prepared, and their physicochemical and thermogelling properties were characterized by H NMR, ATR-FTIR, and rheometer. They exhibited versatile release kinetics from several hours to more than 2 weeks, depending on drug type and concentration. Our formulations further showed good residual stability for more than 21 days without any cytotoxicity or inflammation in the middle and inner ear and could deliver a considerably high drug concentration into the inner ear. Therefore, HGC thermogel has great potential as an effective and safe formulation for inner ear drug delivery.
我们制备了一种新的可注射热凝胶，以提高地塞米松（DEX）在内耳传递的效率。己酰化乙二醇壳聚糖（HGC）被合成并评估为一种两亲性热凝胶（T~32°C），可用作增溶剂以及亲水性和疏水性 DEX 经鼓室内给药的可注射载体。用不同的药物类型和浓度制备了各种热凝胶制剂，并通过 H NMR、ATR-FTIR 和流变仪对其理化和热凝胶性质进行了表征。它们表现出多种释放动力学，从数小时到超过 2 周不等，取决于药物类型和浓度。我们的制剂在没有中耳和内耳细胞毒性或炎症的情况下，具有超过 21 天的良好残留稳定性，并且可以将相当高的药物浓度递送到内耳。因此，HGC 热凝胶作为一种有效的内耳药物传递制剂具有很大的潜力。
