Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, PR China.
Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Melbourne, Australia.
J Microencapsul. 2021 Aug;38(5):314-323. doi: 10.1080/02652048.2021.1915398. Epub 2021 May 19.
Current study aimed to improve the solubility and release profile of the celecoxib for cancer application. However, the low water solubility of celecoxib limited its application for cancer chemotherapy. Hence, new drug delivery-based approaches are compulsory for the efficient delivery of hydrophobic celecoxib for chemotherapy.
The celecoxib-loaded nanocrystals were prepared by anti-solvent precipitation-ultrasonication technique, and the formulation was optimised through various process parameters.
The optimised formulation had an average particle diameter of 171.09 ± 6.23 nm, with a PDI of 0.123 ± 0.009 and high ZP -27.3 ± 0.2 mV. The optimised formulation was stable, had higher entrapment efficiency 97.26 ± 1.12%. The conformational changes in the denatured protein solution were detected through fluorescence spectroscopy. The transmission electron microscopy investigation showed rod-shaped nanocrystals morphology, and no chemical interactions were observed in optimised formulation through FTIR. The DSC and PXRD analysis exhibited an amorphous state of the freeze-dried formulation drug. Also, optimised nanocrystals enhance drug solubility around 26.01-fold, 15.51-fold and 19.08-fold in purified water, pH 6.8 and pH 7.4, and accomplish sustained drug delivery, respectively.
It can be concluded that biopolymer-coated celecoxib nanocrystals might be potential drug delivery of hydrophobic molecules for cancer therapy.
本研究旨在提高塞来昔布的水溶性和释放特性，以将其应用于癌症治疗。然而，塞来昔布的水溶性较低，限制了其在癌症化疗中的应用。因此，需要新的药物递送方法来有效递送疏水性的塞来昔布用于化疗。
采用抗溶剂沉淀-超声技术制备塞来昔布载纳米晶，并通过各种工艺参数对制剂进行优化。
优化后的制剂平均粒径为 171.09±6.23nm，PDI 为 0.123±0.009，Zeta 电位为-27.3±0.2mV。优化后的制剂稳定，包封效率高达 97.26±1.12%。通过荧光光谱检测到变性蛋白溶液中的构象变化。透射电子显微镜研究显示出棒状纳米晶体形态，傅里叶变换红外光谱未观察到优化制剂中存在化学相互作用。差示扫描量热法和粉末 X 射线衍射分析表明，冻干制剂药物呈无定形态。此外，优化后的纳米晶可使药物在纯水中的溶解度提高约 26.01 倍，在 pH 6.8 和 pH 7.4 中的溶解度分别提高 15.51 倍和 19.08 倍，并实现药物的持续释放。
综上所述，生物聚合物包被的塞来昔布纳米晶可能是用于癌症治疗的疏水分子的潜在药物递送系统。
