背景:腔体液,蚯蚓体内的药理活性化合物,展示了一系列的生物活性,包括抗氧化剂,抗炎,和抗癌。然而,体腔液所发挥的生物活性因其生物利用度和稳定性低而受到抑制。脂质体逐渐被用作生物利用度和稳定性差的天然生物活性化合物的包封系统。这可能适用于体腔液。因此,本研究旨在制造,表征,并评估了作为天然抗氧化剂化合物的脂质体制剂的稳定性。
方法:开发了ACCF-脂质体,随后表征了它们的物理化学属性。物理稳定性,ACCF释放行为,并在体外评价胃肠稳定性。还测定了ACCF及其脂质体制剂的生物活性。
结果:ACCF的脂质体制剂在201nm处具有稳定的特征吸收带和99.20±0.10%的透射率。其平均流体力学粒径为98nm,PDI为0.29±0.04,ζ电位为负(-38.66±0.33mV)。TEM进一步证实了囊泡的形成,单层结构的球形纳米脂质体。此外,观察到ACCF脂质体的显着包封率百分比(77.58±0.82%),渗透率等于3.20±0.31%和高保留率(54.16±2.20%)。傅里叶变换红外光谱(FTIR)结果表明ACCF成功地包埋在脂质体内。ACCF-脂质体在体外表现出缓慢且受控的ACCF释放。关于稳定性研究,脂质体制剂增强了ACCF在储存过程中和在不同pH下的稳定性。此外,ACCF-脂质体在与胃消化相当的肠消化条件下高度稳定。目前的研究表明,脂质体制剂增强了ACCF的生物活性,尤其是抗氧化剂,抗炎,和溶栓活性。
结论:这些有希望的结果为增加ACCF的生物可及性提供了一种新颖的方法,这对于开发药物和富含营养的功能性食品可能至关重要。
Coelomic fluid, a pharmacologically active compound in earthworms, exhibits a range of biological activities, including antioxidant, anti-inflammatory, and anticancer. However, the biological activities exerted by the coelomic fluid can be restrained by its low bioavailability and stability. Liposomes are progressively utilized as an entrapment system for natural bioactive compounds with poor bioavailability and stability, which could be appropriate for coelomic fluid. Thus, the present study was designed to fabricate, characterize, and evaluate the stability of liposomal formulation for Allolobophora caliginosa coelomic fluid (ACCF) as a natural antioxidant compound.
The ACCF-liposomes were developed with a subsequent characterization of their physicochemical attributes. The physical stability, ACCF release behavior, and gastrointestinal stability were evaluated in vitro. The biological activities of ACCF and its liposomal formulation were also determined.
The liposomal formulation of ACCF had a steady characteristic absorption band at 201 nm and a transmittance of 99.20 ± 0.10%. Its average hydrodynamic particle size was 98 nm, with a PDI of 0.29 ± 0.04 and a negative zeta potential (-38.66 ± 0.33mV). TEM further confirmed the formation of vesicular, spherical nano-liposomes with unilamellar configuration. Additionally, a remarkable entrapment efficiency percent (77.58 ± 0.82%) with a permeability rate equal to 3.20 ± 0.31% and a high retention rate (54.16 ± 2.20%) for ACCF-liposomes were observed. The Fourier transform infrared spectroscopy (FTIR) result demonstrated that ACCF successfully entrapped inside liposomes. The ACCF-liposomes exhibited a slow and controlled ACCF release in vitro. Regarding stability studies, the liposomal formulation enhanced the stability of ACCF during storage and at different pH. Furthermore, ACCF-liposomes are highly stable in intestinal digestion conditions comparable to gastric digestion. The current study disclosed that liposomal formulation potentiates the biological activities of ACCF, especially antioxidant, anti-inflammatory, and thrombolytic activities.
These promising results offer a novel approach to increasing the bioaccessibility of ACCF, which may be crucial for the development of pharmaceuticals and nutraceutical-enriched functional foods.