Ahmad Niyaz, Ahmad Rizwan, Al-Qudaihi Ali, Alaseel Salman Edrees, Fita Ibrahim Zuhair, Khalid Mohammed Saifuddin, Pottoo Faheem Hyder, Bolla Srinivasa Rao
1Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Kingdom of Saudi Arabia.
2Department of Pharmaceutical Chemistry, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Kingdom of Saudi Arabia.
3 Biotech. 2019 Oct;9(10):360. doi: 10.1007/s13205-019-1885-3. Epub 2019 Sep 9.
The main objective of this study was to develop and evaluate self-nanoemulsifying drug delivery system (SNEDDS) of curcumin (Cur) to enhance their solubility as well as improve skin permeation; and evaluate wound healing potential of Cur via SNEDDS in comparison with standards pure eucalyptus oil-SNEDDS (Euc-SNEDDS), pure curcumin suspension (Cur-S), and standard fusidic acid followed by their anti-inflammatory action. Curcumin-loaded different SNEDDS formulations were formulated through aqueous phase titration method and the zones of SNEDDS were recognized by the construction of phase diagrams. Eucalyptus oil, Tween 80 (surfactant), and Transcutol HP (co-surfactant) were selected on the basis of their solubility and highest nanoemulsion region. Characterization of thermodynamic stability for Cur-loaded SNEDDS was evaluated by its globule size, zeta potential, polydispersity index, viscosity, % transmittance, refractive index, and surface morphology. Cur-SNEDDS (Cur-SN4) was optimized and selected on the basis of their excellent physicochemical parameters for in vivo activity. The particle size (59.56 ± 0.94 nm), % transmittance (99.08 ± 0.07%), and PDI (0.207 ± 0.011 were observed for optimized Cur-SNEDDS. TEM and SEM showed their smooth and spherical shape of the morphological characterization with zeta potential (- 21.41 ± 0.89), refractive index (1.341 ± 0.06), and viscosity (11.64 ± 1.26 cp) for optimized Cur-SNEDDS. Finally, optimized Cur-SNEDDS was used to enhance skin permeation with improvement in the solubility of Cur. However, optimized Cur-SNEDDS showed significant wound healing activity as compared with pure eucalyptus oil and Cur-S on topical application. Optimized Cur-SNEDDS showed healing of wound as compared to standard fusidic acid. Optimized Cur-SNEDDS exhibited no signs of inflammatory cells on the histopathological studies of treated rats which were recommended the safety and non-toxicity of Cur-SNEDDS. Newly developed Cur-SNEDDS could be successfully used to enhance Cur-solubility and skin permeation, as well as suggested a potential role of Cur-SNEDDS for better improvement of wound healing activity followed by anti-inflammatory action of Cur via topical application.
本研究的主要目的是开发并评估姜黄素（Cur）的自纳米乳化药物递送系统（SNEDDS），以提高其溶解度并改善皮肤渗透性；并与标准纯桉叶油-SNEDDS（Euc-SNEDDS）、纯姜黄素混悬液（Cur-S）和标准夫西地酸相比，评估通过SNEDDS递送的姜黄素的伤口愈合潜力及其抗炎作用。通过水相滴定法制备了载姜黄素的不同SNEDDS制剂，并通过构建相图识别SNEDDS区域。根据桉叶油、吐温80（表面活性剂）和二乙二醇单乙基醚（助表面活性剂）的溶解度和最大纳米乳液区域进行选择。通过球粒大小、zeta电位、多分散指数、粘度、透光率%、折射率和表面形态对载姜黄素SNEDDS的热力学稳定性进行表征。基于其优异的体内活性理化参数，对Cur-SNEDDS（Cur-SN4）进行了优化和选择。优化后的Cur-SNEDDS的粒径为（59.56±0.94）nm，透光率%为（99.08±0.07）%，多分散指数为（0.207±0.011）。透射电子显微镜（TEM）和扫描电子显微镜（SEM）显示其形态特征为光滑球形，优化后的Cur-SNEDDS的zeta电位为（-21.41±0.89），折射率为（1.341±0.06），粘度为（11.64±1.26）cp。最后，优化后的Cur-SNEDDS用于提高姜黄素的溶解度并改善皮肤渗透性。然而，与纯桉叶油和Cur-S局部应用相比，优化后的Cur-SNEDDS显示出显著的伤口愈合活性。与标准夫西地酸相比，优化后的Cur-SNEDDS显示出伤口愈合效果。在对治疗大鼠的组织病理学研究中，优化后的Cur-SNEDDS未显示炎症细胞迹象，这表明Cur-SNEDDS具有安全性和无毒性。新开发的Cur-SNEDDS可成功用于提高姜黄素的溶解度和皮肤渗透性，并表明Cur-SNEDDS在通过局部应用更好地改善伤口愈合活性以及姜黄素的抗炎作用方面具有潜在作用。
