一种纳米脂质体制剂增强了宽体金线蛭体腔液的抗氧化、抗炎和纤溶活性：制剂和特性。

A nano-Liposomal formulation potentiates antioxidant, anti-inflammatory, and fibrinolytic activities of Allolobophora caliginosa coelomic fluid: formulation and characterization.

机构信息

Department of Zoology, Faculty of Science, Cairo University, Giza, 12613, Egypt.

出版信息

BMC Biotechnol. 2023 Aug 3;23(1):28. doi: 10.1186/s12896-023-00795-5.

DOI:10.1186/s12896-023-00795-5

PMID:37537554

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10401763/

Abstract

BACKGROUND

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.

METHODS

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.

RESULTS

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.

CONCLUSION

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.

摘要

背景

蚯蚓的体腔液是一种具有多种生物活性的药理学活性化合物，具有抗氧化、抗炎和抗癌作用。然而，体腔液的生物活性会因其低生物利用度和稳定性而受到限制。脂质体作为一种包封生物活性化合物的方法，逐渐被应用于那些生物利用度和稳定性较差的天然化合物，这对于体腔液来说可能是合适的。因此，本研究旨在制备、表征和评估作为天然抗氧化剂化合物的 Allolobophora caliginosa 体腔液（ACCF）的脂质体制剂的稳定性。

方法

用 ACCF 制备脂质体，并对其理化性质进行了后续表征。体外评价了脂质体的物理稳定性、ACCF 释放行为和胃肠道稳定性。还测定了 ACCF 及其脂质体制剂的生物活性。

结果

ACCF 脂质体的特征吸收带在 201nm 处稳定，透光率为 99.20±0.10%。其平均水动力粒径为 98nm，PDI 为 0.29±0.04，zeta 电位为负-38.66±0.33mV。TEM 进一步证实了形成了具有单室结构的囊泡状、球形纳米脂质体。此外，观察到 ACCF-脂质体的包封效率百分比（77.58±0.82%）显著，渗透率等于 3.20±0.31%，保留率（54.16±2.20%）高。傅里叶变换红外光谱（FTIR）结果表明，ACCF 成功地包封在脂质体中。ACCF-脂质体在体外具有缓慢和控制的 ACCF 释放。关于稳定性研究，脂质体制剂在储存和不同 pH 值下增强了 ACCF 的稳定性。此外，ACCF-脂质体在肠内消化条件下比胃内消化条件下更稳定。本研究表明，脂质体制剂增强了 ACCF 的生物活性，特别是抗氧化、抗炎和溶栓活性。