Lu Chuan
Department of Neurosurgery, Wenzhou Central Hospital, 32 Dajian Xiang, Wenzhou, P.R. China.
Curr Drug Deliv. 2016;13(5):682-7. doi: 10.2174/1567201813666151109102532.
Curcumin as an antioxidative agent which has been widely used medicinally in India and China. However, rapid metabolism coupled with the instability of curcumin under physiological conditions has greatly limited its applications in vivo. In the present study, a thermosensitive hydrogel with high payload of curcumin was developed by using a co-precipitation method, and its reversion of oxidative stress in Neuro-2a cells was investigated. With an increase in drug loading capacity, the solgel transition temperature of the thermosensitive hydrogel decreased accordingly. The stability of curcumin in phosphate-buffered saline (PBS; pH=7.4) was greatly improved by encapsulation in the thermosensitive hydrogel, as indicated by an in vitro degradation test. An in vitro release study showed that the encapsulated curcumin was rapidly released from the hydrogel within 6 h. A curcumin/F-127 aqueous solution under the threshold concentration of 4μg/mL was non-toxic against Neuro-2a cells after 24-h incubation. A MitoSOX assay indicated that the developed curcumin formulation could attenuate the oxidative damage induced by H2O2 as compared to that of the H2O2 group. All these results suggested that the developed curcumin/thermosensitive hydrogel might have great potential application in the reversion of oxidative stress after traumatic brain injury.
姜黄素作为一种抗氧化剂，在印度和中国已被广泛用于医学领域。然而，姜黄素在生理条件下代谢迅速且不稳定，这极大地限制了其在体内的应用。在本研究中，采用共沉淀法制备了一种高载药量的热敏水凝胶，并研究了其对Neuro-2a细胞氧化应激的逆转作用。随着载药量的增加，热敏水凝胶的溶胶-凝胶转变温度相应降低。体外降解试验表明，将姜黄素包裹在热敏水凝胶中可大大提高其在磷酸盐缓冲盐水（PBS；pH = 7.4）中的稳定性。体外释放研究表明，包裹的姜黄素在6小时内迅速从水凝胶中释放出来。在4μg/mL阈值浓度以下的姜黄素/F-127水溶液在孵育24小时后对Neuro-2a细胞无毒。MitoSOX分析表明，与H2O2组相比，所制备的姜黄素制剂可减轻H2O2诱导的氧化损伤。所有这些结果表明，所制备的姜黄素/热敏水凝胶在创伤性脑损伤后氧化应激的逆转方面可能具有巨大的潜在应用价值。
