Preparation and characterization of a solid dispersion formulation of coenzyme Q10 loaded with protamine: an efficient and novel strategy to enhance bioavailability and stability

Yingying Liao, Li Sun, Wenhao Xu, Pei Qiao, Duncong Fan
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Abstract

Coenzyme Q10 (CoQ10) is an endogenous, lipophilic quinone compound that functions as an electron carrier in the mitochondrial respiratory chain and plays a pivotal role in cell metabolism. Despite its numerous important physiological functions, the practical application of CoQ10 is limited due to its high molecular weight, poor water solubility, photolability, chemical instability, and low bioavailability. To overcome these challenges, we developed a solid dispersion formulation of protamine loaded CoQ10 (CoQ10/Pr) using an efficient mechanochemical technology without solvents. Protamine was used as carrier and poloxamer 188 as solubilizer, while butylated hydroxytoluene (BHT) and micro powder silica gel were utilized as stabilizers and lubricants. The optimal ball milling condition to prepare CoQ10/Pr was at 100 r/min for 4 hours. The treated CoQ10/Pr has exhibited rapid-release properties, with significantly enhanced water solubility by 392,000 times, and bioavailability by 0.68 times. Furthermore, the treated CoQ10/Pr became resistant to moisture, high temperature and strong light, which makes it suitable for long-term storage. The molecular docking suggested that the solubilization mechanism of CoQ10 was closely associated with the encapsulation and complexation of protamine, as well as the formation of an intermolecular complex through hydrogen bond between CoQ10 and arginine residues on protamine. In summary, the CoQ10 solid dispersion formulation enjoys advantages such as excellent water solubility, stability, bioavailability, and low cost. This formulation also meets the stringent quality requirements of products in the food, cosmetic, and health industries. It offers dual benefits in both theoretical research and industrial development.
添加原胺的辅酶 Q10 固体分散制剂的制备和表征:提高生物利用率和稳定性的高效新策略
辅酶 Q10(CoQ10)是一种内源性亲脂性醌化合物,在线粒体呼吸链中充当电子载体,在细胞新陈代谢中发挥着关键作用。尽管 CoQ10 具有众多重要的生理功能,但由于其分子量高、水溶性差、光溶性强、化学性质不稳定以及生物利用率低等原因,其实际应用受到了限制。为了克服这些挑战,我们采用高效的机械化学技术,在不使用溶剂的情况下,开发出了一种负载 CoQ10 的原胺固体分散制剂(CoQ10/Pr)。原胺用作载体,聚氧乙烯醚 188 用作增溶剂,丁基羟基甲苯(BHT)和微粉硅胶用作稳定剂和润滑剂。制备 CoQ10/Pr 的最佳球磨条件为 100 转/分钟,持续 4 小时。处理后的 CoQ10/Pr 具有快速释放的特性,水溶性显著提高了 392,000 倍,生物利用度提高了 0.68 倍。此外,经过处理的 CoQ10/Pr 还具有防潮、耐高温和耐强光的特性,适合长期保存。分子对接表明,CoQ10的增溶机理与原胺的包裹和络合密切相关,CoQ10与原胺上的精氨酸残基通过氢键形成分子间络合物。总之,CoQ10 固体分散制剂具有优异的水溶性、稳定性、生物利用度和低成本等优点。该配方还能满足食品、化妆品和保健品行业对产品质量的严格要求。它在理论研究和工业开发方面具有双重优势。
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