Al-Rohaimi Abdulmohsen H
College of pharmacy, Al-Dawadmi Campus, Shaqra University.
J Oleo Sci. 2015;64(1):27-40. doi: 10.5650/jos.ess14175. Epub 2014 Dec 16.
The problem of poor bioavailability and clinical efficacy of curcumin can be sorted out after converting crystalline Curcumin (CrysCur) into amorphous NanoCurcumin (NanoCur). Amorphous NanoCur was prepared by converting into nanoemulsion (o/w) using water titration method. The formulation were pre-screen by different physical stress tests, followed by in vitro release study, zeta potential, viscosity, transmittance, globule size distribution and ex vivo studies. The morphology of the NanoCur was determined using transmission electron microscopy (TEM) which revealed fairly spherical shape and good correlation with droplet size distribution study. The NanoCur was converted to gel using Cabopol 934. The composition of optimized NanoCur was curcumin (0.154% w/w), Carbopol 934 (0.702% w/w), ethanolic oil phase [ethanol (0.013% w/w): Capryol 90 (0.015%w/w)], Tween 20 (0.076%w/w) as surfactant, PEG 200 (0.038%w/w) as a co-surfactant and distilled water (q.s) as hydration phase. The steady state flux (Jss), permeability coefficient (Kp) and enhancement ratio (Er) of NanoCur gel was determined and compared with CrysCur gel. Anti-inflammatory effects of the formulations were evaluated in carrageenan-induced paw edema method in rats using Diclofenac as a reference. These ant-inflammatory effects of NanoCur was highly significant (p<0.001) compared to CrysCur and significantly (p<0.05) comparable with standard Diclofenac. The histology of the formulation treated skin showed insignificant changes in the integrity except in the group treated with NanoCur. The slight disruption in the integrity of skin may be because of surfactant present in the nano formulations. Short term storage stability showed insignificant changes in the droplet size and zeta potential, proving its high shelf-life. Finally, it was concluded that NanoCur could be a promising tool in the management of topical inflammation.
将结晶姜黄素(CrysCur)转化为无定形纳米姜黄素(NanoCur)后,姜黄素生物利用度低和临床疗效差的问题便可得到解决。采用水滴定法将其转化为纳米乳剂(水包油型)来制备无定形纳米姜黄素。通过不同的物理应力测试对制剂进行预筛选,随后进行体外释放研究、zeta电位、粘度、透光率、球粒大小分布和离体研究。使用透射电子显微镜(TEM)测定纳米姜黄素的形态,结果显示其形状相当呈球形,且与液滴大小分布研究具有良好的相关性。使用卡波姆934将纳米姜黄素转化为凝胶。优化后的纳米姜黄素组合物包含姜黄素(0.154% w/w)、卡波姆934(0.702% w/w)、乙醇油相[乙醇(0.013% w/w):辛酸癸酸甘油三酯(0.015% w/w)]、吐温20(0.076% w/w)作为表面活性剂、聚乙二醇200(0.038% w/w)作为助表面活性剂以及蒸馏水(适量)作为水合相。测定纳米姜黄素凝胶的稳态通量(Jss)、渗透系数(Kp)和增强比(Er),并与结晶姜黄素凝胶进行比较。以双氯芬酸为参照,采用角叉菜胶诱导大鼠足爪肿胀法评估制剂的抗炎作用。与结晶姜黄素相比,纳米姜黄素的这些抗炎作用非常显著(p<0.001),且与标准双氯芬酸相比具有显著(p<0.05)的可比性。经制剂处理的皮肤组织学检查显示,除纳米姜黄素处理组外,完整性无明显变化。皮肤完整性的轻微破坏可能是由于纳米制剂中存在表面活性剂。短期储存稳定性显示液滴大小和zeta电位无明显变化,证明其保质期长。最后得出结论,纳米姜黄素可能是治疗局部炎症的一种有前景的工具。