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Cationic Dextran Stearate (Dex-St-GTMAC): Synthesis and Evaluation as Polymeric Micelles for Indomethacin Corneal Penetration
ACS Omega ( IF 3.7 ) Pub Date : 2023-10-02 , DOI: 10.1021/acsomega.3c04187
Farzin Firozian 1 , Zahra Arabkhani 2 , Mohammad Mehdi Mahboobian 1 , Mojdeh Mohammadi 3 , Gholamabbas Chehardoli 2
ACS Omega ( IF 3.7 ) Pub Date : 2023-10-02 , DOI: 10.1021/acsomega.3c04187
Farzin Firozian 1 , Zahra Arabkhani 2 , Mohammad Mehdi Mahboobian 1 , Mojdeh Mohammadi 3 , Gholamabbas Chehardoli 2
Affiliation
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Background Indomethacin as a non-steroidal anti-inflammatory drug (NSAID) is commonly used to treat some ocular inflammatory disorders. Unfortunately, indomethacin is a drug that is poorly soluble in water; therefore, it has low efficacy. An attractive approach is the targeted delivery of indomethacin to the cornea using cationic dextran stearate as a polymeric micelle drug carrier. Methods A dextran stearate-glycidyl trimethylammonium chloride (Dex-St-GTMAC) copolymer was prepared through the reaction of GTMAC, stearoyl chloride, and dextran. Then, Dex-St-GTMAC was characterized by Fourier transform infrared (FT-IR) spectroscopy and 1H NMR spectroscopy. Dex-St-GTMAC forms micelles in the presence of indomethacin. The prepared polymeric micelles were characterized for size, ζ-potential, drug loading, particle morphology, critical micelle concentration, and encapsulation efficiency. To study the irritation potential of the indomethacin-loaded Dex-St-GTMAC, Het-Cam and Draize tests have been performed. Prepared cationic micelles were subjected to the in vitro drug release and ex vivo trans-corneal permeation test. Results The dialysis method was used for the preparation of indomethacin-loaded micelles (10, 20, and 30%). Measurement of the particle size showed a mean diameter of 122.1 and 150.9 nm for the drug-loaded micelles. Scanning electron microscopy (SEM) images showed that the morphology of the particles is spherical. 10% formulation was chosen as the best formulation due to more surface charge and reasonable drug loading. ζ-potential measurement for the 10% drug-containing micelles showed a value of +39.1 mV. Drug loading efficiency and the encapsulation efficiency for 10% drug-containing micelles were 6.36 and 63.61%, respectively. The results of the Het-Cam and Draize tests indicated that the indomethacin-loaded Dex-St-GTMAC formulation had no toxicity to eye tissues. Based on our results, the prepared micelles (indomethacin-loaded Dex-St-GTMAC) exhibited a sustained drug release pattern compared to the control group. Indomethacin penetration from the micelles to the excised bovine cornea was 1.75-fold greater than the control (indomethacin 0.1% in phosphate-buffered saline (PBS)). Conclusions Data from the ζ-potential, SEM, drug loading capacity, and in vitro drug release studies indicated that cationic dextran stearate polymeric micelles are an appropriate carrier for the efficient penetration of indomethacin into cornea tissues.
中文翻译：
阳离子右旋糖酐硬脂酸酯 (Dex-St-GTMAC)：吲哚美辛角膜渗透聚合物胶束的合成和评价
背景吲哚美辛作为一种非甾体类抗炎药 (NSAID)，通常用于治疗一些眼部炎症性疾病。不幸的是，吲哚美辛是一种难溶于水的药物。因此，其功效较低。一种有吸引力的方法是使用阳离子右旋糖酐硬脂酸酯作为聚合物胶束药物载体将吲哚美辛靶向递送至角膜。方法以GTMAC、硬脂酰氯和葡聚糖反应制备葡聚糖硬脂酸酯-缩水甘油基三甲基氯化铵(Dex-St-GTMAC)共聚物。然后，通过傅里叶变换红外（FT-IR）光谱和1 H NMR 光谱对 Dex-St-GTMAC 进行了表征。Dex-St-GTMAC 在吲哚美辛存在下形成胶束。对制备的聚合物胶束的尺寸、ze电位、载药量、颗粒形态、临界胶束浓度和包封效率进行了表征。为了研究载有吲哚美辛的 Dex-St-GTMAC、Het-Cam 和 Draize 测试的刺激潜力。制备的阳离子胶束进行体外药物释放和离体 角膜渗透测试。结果采用透析法制备吲哚美辛胶束（10%、20%、30%）。粒径测量显示载药胶束的平均直径为 122.1 和 150.9 nm。扫描电子显微镜（SEM）图像显示颗粒的形态为球形。由于表面电荷较多且载药量合理，选择10%制剂为最佳制剂。含 10% 药物的胶束的 ζ 电位测量结果显示值为 +39.1 mV。10%含药胶束的载药率和包封率分别为6.36%和63.61%。Het-Cam 和 Draize 测试的结果表明，载有吲哚美辛的 Dex-St-GTMAC 制剂对眼组织没有毒性。根据我们的结果，与对照组相比，制备的胶束（负载吲哚美辛的 Dex-St-GTMAC）表现出持续的药物释放模式。吲哚美辛从胶束到离体牛角膜的渗透比对照（磷酸盐缓冲盐水 (PBS) 中的 0.1% 吲哚美辛）高 1.75 倍。结论ζ电位、SEM、载药量和体外药物释放研究的数据表明，阳离子右旋糖酐硬脂酸酯聚合物胶束是吲哚美辛有效渗透到角膜组织的合适载体。
更新日期：2023-10-02
中文翻译：
阳离子右旋糖酐硬脂酸酯 (Dex-St-GTMAC)：吲哚美辛角膜渗透聚合物胶束的合成和评价
背景吲哚美辛作为一种非甾体类抗炎药 (NSAID)，通常用于治疗一些眼部炎症性疾病。不幸的是，吲哚美辛是一种难溶于水的药物。因此，其功效较低。一种有吸引力的方法是使用阳离子右旋糖酐硬脂酸酯作为聚合物胶束药物载体将吲哚美辛靶向递送至角膜。方法以GTMAC、硬脂酰氯和葡聚糖反应制备葡聚糖硬脂酸酯-缩水甘油基三甲基氯化铵(Dex-St-GTMAC)共聚物。然后，通过傅里叶变换红外（FT-IR）光谱和1 H NMR 光谱对 Dex-St-GTMAC 进行了表征。Dex-St-GTMAC 在吲哚美辛存在下形成胶束。对制备的聚合物胶束的尺寸、ze电位、载药量、颗粒形态、临界胶束浓度和包封效率进行了表征。为了研究载有吲哚美辛的 Dex-St-GTMAC、Het-Cam 和 Draize 测试的刺激潜力。制备的阳离子胶束进行体外药物释放和离体 角膜渗透测试。结果采用透析法制备吲哚美辛胶束（10%、20%、30%）。粒径测量显示载药胶束的平均直径为 122.1 和 150.9 nm。扫描电子显微镜（SEM）图像显示颗粒的形态为球形。由于表面电荷较多且载药量合理，选择10%制剂为最佳制剂。含 10% 药物的胶束的 ζ 电位测量结果显示值为 +39.1 mV。10%含药胶束的载药率和包封率分别为6.36%和63.61%。Het-Cam 和 Draize 测试的结果表明，载有吲哚美辛的 Dex-St-GTMAC 制剂对眼组织没有毒性。根据我们的结果，与对照组相比，制备的胶束（负载吲哚美辛的 Dex-St-GTMAC）表现出持续的药物释放模式。吲哚美辛从胶束到离体牛角膜的渗透比对照（磷酸盐缓冲盐水 (PBS) 中的 0.1% 吲哚美辛）高 1.75 倍。结论ζ电位、SEM、载药量和体外药物释放研究的数据表明，阳离子右旋糖酐硬脂酸酯聚合物胶束是吲哚美辛有效渗透到角膜组织的合适载体。
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