用于芦丁皮肤给药的热敏凝胶系统。
Thermosensitive Gelling System for Dermal Drug Delivery of Rutin.
作者信息
Gözcü Sefa, Polat Kerem Heybet
机构信息
Erzincan Binali Yıldırım University, Faculty of Pharmacy, Department of Pharmacognosy, Erzincan, Türkiye.
Erzincan Binali Yıldırım University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Erzincan, Türkiye.
出版信息
Turk J Pharm Sci. 2023 May 9;20(2):78-83. doi: 10.4274/tjps.galenos.2022.00334.
OBJECTIVES
Rutin has been broadly applied for treating several diseases due to its pharmacological activities. However, its low aqueous solubility limits its absorption and bioavailability. This research aims to increase the solubility of rutin using cyclodextrin and to develop a temperature-triggered gelling system for dermal application.
MATERIALS AND METHODS
The solubility of rutin was increased with sulfobutyl ether-β-cyclodextrin (SBE-β-CD). Rutin- SBE-β-CD inclusion complex was prepared by kneading and freeze dying method. Structural characterization was carried out using differential scanning calorimetry and fourier transform infrared spectroscopy. gel formulations were prepared with pluronic F127 (PF127), a thermosensitive polymer, and chitosan (CH), a natural, biodegradable, and mucoadhesive hydrophilic polymer. gel characteristics such as pH, clarity, gelation temperature, and viscosity were determined.
RESULTS
When the solubility diagrams were examined, it was concluded that SBE-β-CD showed a linear increase, therefore, AL-type diagram was selected. The formulations were produced using different amounts of PF127 and a fixed ratio of CH. Three gels were evaluated for their pH, gelling temperature, and the rheological behaviors, and one formulation was selected. It was observed that the formulations had a pH between 6-6.1, and their gelation temperature decreased with increasing PF127 that was between 20°C to 34°C. For the selected formulation (formulation E3), 0.5% rutin and rutin/SBE-β-CD were transferred to the gelling system. Because of release studies, it was observed that the release of the rutin/SBE-β-CD inclusion complex containing NZ formulation showed a higher burst effect than the others and the release continued for 6 hours.
CONCLUSION
The results indicated that the combination of PF127 and CH can be a hopeful gelling vehicle for dermal delivery of rutin and rutin/SBE-β-CD.
目的
芦丁因其药理活性已被广泛应用于多种疾病的治疗。然而，其低水溶性限制了其吸收和生物利用度。本研究旨在利用环糊精提高芦丁的溶解度，并开发一种用于皮肤给药的温度触发凝胶系统。
材料与方法
用磺丁基醚-β-环糊精（SBE-β-CD）提高芦丁的溶解度。采用捏合法和冷冻干燥法制备芦丁-SBE-β-CD包合物。使用差示扫描量热法和傅里叶变换红外光谱进行结构表征。用热敏聚合物泊洛沙姆F127（PF127）和天然、可生物降解且具有粘膜粘附性的亲水性聚合物壳聚糖（CH）制备凝胶制剂。测定凝胶的pH值、澄清度、凝胶化温度和粘度等特性。
结果
检查溶解度图时得出结论，SBE-β-CD呈线性增加，因此选择AL型图。使用不同量的PF127和固定比例的CH制备制剂。对三种凝胶的pH值、凝胶化温度和流变行为进行了评估，并选择了一种制剂。观察到制剂的pH值在6-6.1之间，其凝胶化温度随着PF127含量的增加而降低，范围在20°C至34°C之间。对于所选制剂（制剂E3），将0.5%的芦丁和芦丁/SBE-β-CD转移到凝胶系统中。通过释放研究观察到，含NZ制剂的芦丁/SBE-β-CD包合物的释放显示出比其他制剂更高的突释效应，且释放持续6小时。
结论
结果表明，PF127和CH的组合可能是一种有前景的用于芦丁和芦丁/SBE-β-CD皮肤给药的凝胶载体。
Zotero 插件