Dept. of Pharmaceutics, School of Pharmacy, Shahid Beheshti Univ. of Medical Sciences, Tehran, Iran.
Pharmaceutical Sciences Research Center, Shahid Beheshti Univ. of Medical Sciences, Tehran, Iran.
J Food Sci. 2019 Sep;84(9):2572-2583. doi: 10.1111/1750-3841.14763. Epub 2019 Aug 22.
This study was aimed to develop a novel nanocarrier for coenzyme Q10 (CoQ10) by a green process that prevented the use of surfactants and organic solvents. Triglyceride/phospholipid-based nanocarriers were developed through high-pressure homogenization (an industrial feasible process), and a 2 fractional factorial design was adopted to assess the influences of formulation variables on the considered responses, including vesicle size, entrapment efficiency, loading capacity, and solubility of the vehicles in simulated gastrointestinal fluids. The optimized formulation was further in-depth characterized in terms of morphology, release behavior, biocompatibility (Caco-2 cell cytotoxicity and histological examination), thermal behavior, and Fourier transform infrared analysis. Optimal nanocarriers were found to have mean particle size of 75 nm, narrow particle distribution, and CoQ10 entrapment of 95%. The optimized formulation was stable upon incubation in simulated gastrointestinal fluids without considerable leakage of cargo, which was in agreement with their sustained release behavior. Microscopic observations also confirmed nanosized nature of the vesicles and revealed their spherical shape. Moreover, toxicity evaluations at the cellular and tissue levels revealed their nontoxic nature. In conclusion, triglyceride/phospholipid-based nanocarriers proved to be a green safe vehicle for delivery of CoQ10 with industrial-scale production capability and could provide a new horizon for delivery of hydrophobic nutraceuticals. PRACTICAL APPLICATION: Green nanostructure formulation approaches have recently gained tremendous attraction for their safe profile especially when it comes to supplements, which are generally recommended for daily use. However, their sufficient association with cargoes and industrial-scale production have remained considerable challenges. This study focuses on the development of lipid-based nanocarriers for CoQ10 by an industrial feasible process that prevents the use of any surfactants or organic solvents.
本研究旨在开发一种新型的辅酶 Q10（CoQ10）纳米载体，采用绿色工艺，避免使用表面活性剂和有机溶剂。通过高压匀质（一种工业可行的工艺）制备了基于甘油三酯/磷脂的纳米载体，并采用 2 阶分数因子设计评估了制剂变量对所考虑的响应的影响，包括囊泡大小、包封效率、载药量和载体在模拟胃肠液中的溶解度。优化的配方进一步从形态、释放行为、生物相容性（Caco-2 细胞细胞毒性和组织学检查）、热行为和傅里叶变换红外分析等方面进行了深入表征。优化的纳米载体具有平均粒径为 75nm、窄粒径分布和 95%的 CoQ10 包封率。优化的配方在模拟胃肠液中孵育时稳定，没有货物的大量泄漏，这与其持续释放行为一致。显微镜观察也证实了囊泡的纳米尺寸，并显示出它们的球形。此外，细胞和组织水平的毒性评估表明它们具有非毒性。总之，甘油三酯/磷脂基纳米载体被证明是一种用于传递 CoQ10 的绿色安全载体，具有工业规模生产能力，可以为传递疏水性营养保健品提供新的前景。 实用程序：绿色纳米结构制剂方法因其安全特性而最近引起了极大的关注，特别是当涉及到通常建议每天使用的补充剂时。然而，它们与货物的充分结合和工业规模生产仍然是相当大的挑战。本研究侧重于通过工业可行的工艺开发 CoQ10 的脂质基纳米载体，该工艺可避免使用任何表面活性剂或有机溶剂。
