School of Pharmacy, University of Oslo, Oslo, Norway.
J Pharm Sci. 2010 Aug;99(8):3499-513. doi: 10.1002/jps.22119.
The aim of the present study was to incorporate a model water-insoluble photosensitizer, curcumin, in novel alginate foams, further to evaluate the suitability of the curcumin loaded foams in antimicrobial photodynamic therapy of infected wounds. Six foam formulations were prepared and characterized with respect to physical characteristics, in vitro release and storage- and photo-stability of curcumin. One formulation was sterilized (gamma-sterilization). The foams contained hydroxypropyl-beta-cyclodextrins or hydroxypropyl-gamma-cyclodextrins as solubilizers of curcumin. A reference foam without cyclodextrins was prepared with PEG 400 as the solubilizer. At a curcumin load of 0.153% (w/w), the water insoluble photosensitizer was uniformly distributed in the hydrophilic foams matrix. All foams were easy to handle, flexible and hydrated rapidly in a model physiological fluid. Release of curcumin in its monomeric form was demonstrated in vitro and found to be dependent on the type and amount of cyclodextrins in the formulation. Curcumin was stable during storage, but susceptible to photodegradation in the foams, especially when the formulations contain PEG 400 or hydroxypropyl-gamma-cyclodextrins. Curcumin did not degrade after gamma-sterilization, however a decrease in the in vitro release rate of curcumin and changes in the foams physical characteristics were detected.
本研究的目的是将模型疏水性光敏剂姜黄素包封于新型海藻酸钠泡沫中，进一步评估载姜黄素泡沫在感染性伤口抗菌光动力疗法中的适用性。制备了六种泡沫制剂，并就其物理特性、体外释放以及姜黄素的储存稳定性和光稳定性进行了评价。一种制剂经过了灭菌（γ 射线灭菌）。这些泡沫制剂中含有羟丙基-β-环糊精或羟丙基-γ-环糊精作为姜黄素的增溶剂。制备了一种不含环糊精的对照泡沫制剂，其中聚乙二醇 400 作为增溶剂。当姜黄素的载药量为 0.153%（w/w）时，这种疏水性的光敏剂均匀地分布在亲水性泡沫基质中。所有泡沫制剂均易于处理，具有柔韧性，并且在模型生理液中能迅速水合。体外实验表明，姜黄素以单体形式释放，这取决于制剂中环糊精的类型和用量。姜黄素在储存过程中稳定，但在泡沫制剂中易光降解，尤其是当制剂中含有聚乙二醇 400 或羟丙基-γ-环糊精时。然而，经过 γ 射线灭菌后，姜黄素并未降解，但检测到体外释放姜黄素的速率降低以及泡沫制剂物理特性的变化。
