壳聚糖包被的辅酶 Q10 和姜黄素脂质体共包封（Q10-Cur-Lip-Chi）提高了溶解度和稳定性，具有良好的释放性能和抗氧化活性。
A Co-Encapsulation of Coenzyme Q10 and Curcumin in Liposomes Coated with Chitosan (Q10-Cur-Lip-Chi) with Enhanced Solubility and Stability for Good Release Performance and Antioxidative Activity.
机构信息
Department of Pharmaceutical Engineering, School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, P.R. China.
出版信息
Curr Drug Deliv. 2023;20(9):1391-1403. doi: 10.2174/1567201819666220630122755.
BACKGROUND
Coenzyme Q10 (Q10) is a powerful lipophilic antioxidant with poor solubility in aqueous media. Curcumin (Cur) is a natural polyphenolic phytochemical molecule with poor aqueous solubility. The liposome is an improved administration of drugs because it is biocompatible and permeable for nutraceutical delivery. Chitosan, a hydrophilic polymer, is often used as a polymer coating for its good biocompatible and biodegradable properties, and its relatively low toxicity level.
METHODS
Q10 and Cur co-loaded liposomes coated with chitosan (Q10-Cur-Lip-Chi) were constructed. The co-encapsulation of Q10 and Cur in liposomes coated with chitosan was verified by TEM, DLS, DSC, FT-IR, and XRPD. The release profile and antioxidant activity of Q10-Cur-Lip-Chi were accessed.
RESULTS
The particle size of Q10-Cur-Lip-Chi was about 1440 nm with narrow particle distribution. A satisfactory encapsulation efficiency (EE) of Q10 was about 98%, and 25% for that of Cur. Q10-Cur- Lip-Chi showed higher solubility and better pH resistance with 98.5% of Q10 and Cur retention at pH 7.0 - 9.0. Q10-Cur-Lip also showed great salt stability with a vesicle size change of less than 5%. PSof Q10-Cur-Lip-Chi changed less than 10% at 4°C of storage. Q10-Cur-Lip-Chi also exhibited a good controlled release profile with its accumulative release of less than 34% for Q10 and 30% for curcumin after 24 h. The Q10-Cur-Lip-Chi performed a synergistic effect on antioxidant activity reaching 41.86±1.84%, which was 5.9 times higher than that of Q10, 2.5 times higher than that of Cur, and 1.7 times higher than that of the mixture.
CONCLUSION
The co-encapsulation Q10-Cur-Lip-Chi improves the solubility and stability of Q10 and Cur for good release performance and antioxidative activity.
背景
辅酶 Q10（Q10）是一种具有强大亲脂性的抗氧化剂，在水性介质中的溶解度较差。姜黄素（Cur）是一种天然的多酚类植物化学物质，水溶性差。脂质体是一种改良的药物给药方式，因为它具有生物相容性和对营养输送的通透性。壳聚糖是一种亲水性聚合物，由于其良好的生物相容性和可生物降解性，以及相对较低的毒性水平，常被用作聚合物涂层。
方法
构建了用壳聚糖（Q10-Cur-Lip-Chi）包被的 Q10 和姜黄素共载脂质体。通过 TEM、DLS、DSC、FT-IR 和 XRPD 验证了 Q10 和姜黄素在壳聚糖包被的脂质体中的共包封。研究了 Q10-Cur-Lip-Chi 的释放特性和抗氧化活性。
结果
Q10-Cur-Lip-Chi 的粒径约为 1440nm，粒径分布较窄。Q10 的包封效率（EE）约为 98%，姜黄素的包封效率约为 25%。Q10-Cur-Lip-Chi 具有较高的溶解度和更好的 pH 耐受性，在 pH7.0-9.0 时 Q10 和姜黄素的保留率均为 98.5%。Q10-Cur-Lip 还具有很好的盐稳定性，在 5%的盐浓度下，囊泡粒径变化小于 5%。在 4°C 的储存条件下，Q10-Cur-Lip-Chi 的 PS 变化小于 10%。Q10-Cur-Lip-Chi 也表现出良好的控释特性，24h 时 Q10 的累积释放量小于 34%，姜黄素的累积释放量小于 30%。Q10-Cur-Lip-Chi 对抗氧化活性表现出协同作用，达到 41.86±1.84%，是 Q10 的 5.9 倍，是姜黄素的 2.5 倍，是混合物的 1.7 倍。
结论
共包封 Q10-Cur-Lip-Chi 提高了 Q10 和姜黄素的溶解度和稳定性，具有良好的释放性能和抗氧化活性。
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