School of Pharmacy, University of Oslo, Oslo 0316, Norway.
J Pharm Sci. 2012 Apr;101(4):1524-37. doi: 10.1002/jps.23046. Epub 2012 Jan 6.
Curcumin has been investigated as a potential photosensitizer (PS) in antimicrobial photodynamic therapy (aPDT). The phototoxic effect of curcumin is dependent on proper formulations of the compound because of the lipophilic nature of the molecule and the extremely low water solubility at physiological conditions. In the present study, the combination of curcumin with either a methylated β-cyclodextrin (CD) or polyethylene glycol-based β-CD or γ-CD polymers was investigated in aPDT using Escherichia coli (E. coli) and Enterococcus faecalis as model bacteria. Solutions with various supersaturation ratios of curcumin were prepared with the selected CD or CD polymers. The concept of supersaturation was then investigated as a mean to enhance the phototoxic effect of curcumin, especially toward the gram-negative bacteria E. coli. A high supersaturation ratio corresponded with high phototoxicity of E. coli. Depending on the curcumin preparation, the bacterial survival ranged from 0.01% to no significant effect after irradiation with blue light (29 J/cm(2) ). Temporal stabilization of the supersaturated state is necessary in order to retain high and predictable photoreactivity of the PS. Further studies will be needed in order to formulate curcumin preparations with acceptable hydrolytic and photolytic stability and a temporal stabilization of a supersaturated state.
姜黄素已被研究作为一种潜在的光敏剂(PS),用于抗菌光动力疗法(aPDT)。由于分子的亲脂性和在生理条件下极低的水溶性,姜黄素的光毒性效应取决于该化合物的适当制剂。在本研究中,用大肠杆菌(E. coli)和粪肠球菌作为模型细菌,研究了姜黄素与甲基-β-环糊精(CD)或基于聚乙二醇的β-CD 或 γ-CD 聚合物的组合在 aPDT 中的应用。用选定的 CD 或 CD 聚合物制备了具有不同过饱和度比的姜黄素溶液。然后,将过饱和度的概念作为一种提高姜黄素光毒性效应的手段进行了研究,特别是针对革兰氏阴性细菌大肠杆菌。高过饱和度比与大肠杆菌的高光毒性相对应。根据姜黄素的制备方法,细菌的存活率从 0.01%到用蓝光(29 J/cm²)照射后没有显著影响不等。为了保持 PS 的高且可预测的光反应性,需要对过饱和状态进行时间稳定。需要进一步的研究来制定具有可接受的水解和光解稳定性以及过饱和状态的时间稳定性的姜黄素制剂。