Abdelnabi Hiba, Alshaer Walhan, Azzam Hanan, Alqudah Dana, Al-Samydai Ali, Aburjai Talal
School of Pharmacy, The University of Jordan, Amman 11942, Jordan.
Cell Therapy Center, The University of Jordan, Amman 11942, Jordan.
Z Naturforsch C J Biosci. 2021 May 26;76(11-12):503-514. doi: 10.1515/znc-2021-0018. Print 2021 Nov 25.
Capsaicin (CAP) is an active component in L. known to have anti inflammatory and anticancer activity. CAP is highly lipophilic and suffers low bioavailability. Therefore, developing delivery systems that enhance solubility and bioavailability can provide more promising therapeutic applications for CAP. In the current work, CAP was complexed with β-cyclodextrin (βCD) to form capsaicin-in-β-cyclodextrin (CAP-in-βCD) inclusion complexes. Then, the CAP-in-βCD inclusion complexes were characterized and loaded into PEGylated liposomes using the thin-film hydration extrusion method. The size, charge, and polydispersity index (PDI) of the PEGylated liposomes were characterized. The levels of IL-8 production were quantified after treatment using array beads. The results of this work showed that the successful formation of inclusion complexes at 1:5 M ratio of CAP to βCD respectively. PEGylated liposomes loaded with βCD/CAP inclusion complexes (CAP-in-βCD-in-liposomes) have a hydrodynamic diameter of (181 ± 36) nm, zeta potential of (-2.63 ± 4.00) mV, encapsulation efficiency (EE) of (38.65 ± 3.70)%, drug loading (DL) of (1.65 ± 0.16)%, and a stable release profile. Both free CAP and liposomal CAP showed a significant reduction in the IL-8 production by the MDA-MB-231 and A549 cancer cell lines after treatment. In conclusion, a liposomal-based drug delivery system for CAP was achieved.
辣椒素（CAP）是辣椒中的一种活性成分，已知具有抗炎和抗癌活性。CAP具有高度亲脂性，生物利用度低。因此，开发能够提高其溶解度和生物利用度的递送系统可为CAP提供更有前景的治疗应用。在当前工作中，CAP与β-环糊精（βCD）复合形成辣椒素-β-环糊精（CAP-in-βCD）包合物。然后，对CAP-in-βCD包合物进行表征，并使用薄膜水化挤压法将其载入聚乙二醇化脂质体。对聚乙二醇化脂质体的尺寸、电荷和多分散指数（PDI）进行了表征。使用阵列微珠对处理后白细胞介素-8（IL-8）的产生水平进行定量。这项工作的结果表明，分别以1:5的摩尔比成功形成了CAP与βCD的包合物。负载有βCD/CAP包合物的聚乙二醇化脂质体（CAP-in-βCD-in-liposomes）的流体动力学直径为（181±36）nm，ζ电位为（-2.63±4.00）mV，包封率（EE）为（38.65±3.70）%，载药量（DL）为（1.65±0.16）%，且具有稳定的释放曲线。游离CAP和脂质体CAP在处理后均使MDA-MB-231和A549癌细胞系的IL-8产生显著降低。总之，实现了一种基于脂质体的CAP药物递送系统。
