Anwar Mohammed, Ahmad Iqbal, Warsi Musarrat H, Mohapatra Sharmistha, Ahmad Niyaz, Akhter Sohail, Ali Asgar, Ahmad Farhan J
Nanoformulation Research Laboratory, Faculty of Pharmacy, Hamdard University, New Delhi, India.
Nanoformulation Research Laboratory, Faculty of Pharmacy, Hamdard University, New Delhi, India.
Eur J Pharm Biopharm. 2015 Oct;96:162-72. doi: 10.1016/j.ejpb.2015.07.021. Epub 2015 Aug 1.
The biomedical applications of curcumin (CUR) are limited due to its poor oral bioavailability. In this work, CUR nanoparticles were successfully prepared by combining the supercritical anti-solvent (SAS) process with Tween 80 as a solubilizing agent and permeation enhancer. Different processing parameters that can govern the mean particle size and size distribution of nanoparticles were well investigated by manipulating the types of solvents, mixing vessel pressure, mixing vessel temperature, CO2 flow rate, solution flow rate and solution concentration. Solid state characterization was done by Fourier Transform infrared spectroscopy, differential scanning calorimetry, dynamic light scattering, scanning electron microscopy, and powder X-ray diffraction study. Solubility and dissolution profile of SAS-processed CUR were found to be significantly increased in comparison with native CUR. Further, a validated ultra-performance liquid chromatographic method with quadrupole-time of flight-mass spectrometry was developed to investigate the pharmacokinetic parameters after a single oral dose (100mg/kg) administration of CUR (before/after SAS-processed) in male Wistar rats. From the plasma concentration vs. time profile graph, oral bioavailability of SAS-processed CUR was found to be increased approximately 11.6-fold (p<0.001) as compared to native CUR.
姜黄素（CUR）的生物医学应用因其口服生物利用度差而受到限制。在本研究中，通过将超临界抗溶剂（SAS）工艺与吐温80作为增溶剂和渗透促进剂相结合，成功制备了CUR纳米颗粒。通过控制溶剂类型、混合容器压力、混合容器温度、CO2流速、溶液流速和溶液浓度，对影响纳米颗粒平均粒径和粒径分布的不同工艺参数进行了深入研究。通过傅里叶变换红外光谱、差示扫描量热法、动态光散射、扫描电子显微镜和粉末X射线衍射研究进行了固态表征。结果发现，与天然CUR相比，经SAS处理的CUR的溶解度和溶出曲线显著增加。此外，还开发了一种经过验证的超高效液相色谱-四极杆飞行时间质谱联用方法，以研究雄性Wistar大鼠单次口服剂量（100mg/kg）的CUR（SAS处理前后）后的药代动力学参数。从血浆浓度-时间曲线图可以看出，与天然CUR相比，经SAS处理的CUR的口服生物利用度提高了约11.6倍（p<0.001）。
