Formulation, characterization, and evaluation of curcumin-loaded ginger-derived nanovesicles for anti-colitis activity.

Journal of pharmaceutical analysis Pub Date : 2024-12-01 Epub Date: 2024-05-30 DOI:10.1016/j.jpha.2024.101014
Shengjie Huang, Min Zhang, Xiaoge Li, Jierong Pei, Zhirong Zhou, Peng Lei, Meng Wang, Peng Zhang, Heshui Yu, Guanwei Fan, Lifeng Han, Haiyang Yu, Yuefei Wang, Miaomiao Jiang
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Abstract

Plant-derived nanovesicles have gained attention given their similarity to mammalian exosomes and advantages such as low cost, sustainability, and tissue targeting. Thus, they hold promise for disease treatment and drug delivery. In this study, we proposed a time-efficient method, PEG 8000 combined with sucrose density gradient centrifugation to prepare ginger-derived nanovesicles (GDNVs). Subsequently, curcumin (CUR) was loaded onto GDNV by ultrasonic incubation. The optimum conditions for ginger-derived nanovesicles loaded with curcumin (CG) were ultrasound time of 3 min, a carrier-to-drug ratio (GDNV:CUR) of 1:1. The study achieved a high loading capacity (94.027% ± 0.094%) and encapsulation efficiency (89.300% ± 0.344%). Finally, the drugs' in vivo distribution and anti-colitis activity were investigated in mice. CG was primarily distributed in the colon after oral administration. Compared to CUR and GDNV, CG was superior in improving disease activity, colon length, liver and spleen coefficients, myeloperoxidase activity, and biochemical factor levels in ulcerative colitis (UC) mice. In addition, CG plays a protective role against UC by modulating serum metabolite levels and gut flora. In summary, our study demonstrated that GDNV can be used for CUR delivery with enhanced therapeutic potential.

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姜黄素负载姜源纳米囊泡抗结肠炎活性的配方、表征和评价。
植物源性纳米囊泡因其与哺乳动物外泌体的相似性以及低成本、可持续性和组织靶向性等优势而受到关注。因此,它们有望用于疾病治疗和药物输送。在本研究中,我们提出了一种时间效率高的方法,PEG 8000结合蔗糖密度梯度离心制备姜源性纳米囊泡(GDNVs)。随后,超声孵育将姜黄素(curcumin, CUR)加载到GDNV上。姜黄素纳米囊泡制备的最佳工艺条件为超声时间3 min,载药比(GDNV:CUR) 1:1。本研究获得了较高的负载能力(94.027%±0.094%)和封装效率(89.300%±0.344%)。最后观察药物在小鼠体内分布及抗结肠炎活性。口服给药后,CG主要分布于结肠。与CUR和GDNV相比,CG在改善溃疡性结肠炎(UC)小鼠的疾病活动性、结肠长度、肝脏和脾脏系数、髓过氧化物酶活性和生化因子水平方面优于CUR和GDNV。此外,CG通过调节血清代谢物水平和肠道菌群对UC具有保护作用。总之,我们的研究表明,GDNV可以用于CUR的递送,具有增强的治疗潜力。
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