Propolis-loaded liposomes: characterization and evaluation of the in vitro bioaccessibility of phenolic compounds.

IF 3.4 Q2 CHEMISTRY, MEDICINAL
ADMET and DMPK Pub Date : 2024-02-05 eCollection Date: 2024-01-01 DOI:10.5599/admet.2204
Oznur Saroglu, Ayse Karadag
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引用次数: 0

Abstract

Background and purpose: Propolis has low water solubility, poor stability, and limited bioaccessibility of phenolic constituents when subjected to in vitro digestion. To overcome these drawbacks, the liposomal encapsulation method can be employed.

Experimental approach: Soybean phosphatidylcholine lecithin mixed with Tween 80 (T80) and ammonium phosphatides (AMP) was used to produce propolis extract (PE)-loaded liposomes. The mean particle size, zeta potential, encapsulation efficiency values, and transmission electron microscopy analysis were used to characterize liposomes. Individual phenolics were determined for digested and nondigested propolis-loaded liposomes and propolis extract.

Key results: Tween 80 incorporation reduced the size of unloaded liposomes, whereas AMP inclusion yielded larger liposomes. In both formulations, PE loading significantly increased the size and reduced the zeta potential values and homogeneity of the size distribution. In free PE, the most bioaccessible polyphenols were phenolic acids (3.20 to 5.63 %), and flavonoids such as caffeic acid phenethyl ester, galangin, pinobanksin, and pinocembrin (0.03 to 2.12 %) were the least bioaccessible. Both liposomal propolis provided significantly higher bioaccessibility of phenolic compounds. The liposomes with T80 and AMP in their compositions recovered 52.43 and 185.90 % of the total amount of phenolic compounds in the nondigested samples, respectively. The liposomes containing AMP not only exhibited high solubility for PE but also provided protection to the phenolic compounds during in vitro digestion.

Conclusion: Liposomal encapsulation could be a promising approach to improving the solubility and stability of PE in digestive fluids, making it suitable for the delivery of propolis in oral formulations.

蜂胶脂质体:酚类化合物体外生物可及性的表征和评估。
背景和目的:蜂胶的水溶性低、稳定性差,体外消化时酚类成分的生物可利用性有限。为了克服这些缺点,可以采用脂质体封装法:实验方法:用大豆磷脂酰胆碱卵磷脂与吐温80(T80)和磷酸铵(AMP)混合,制备蜂胶提取物(PE)负载脂质体。利用平均粒径、ZETA电位、封装效率值和透射电子显微镜分析来表征脂质体。对消化和未消化的蜂胶负载脂质体和蜂胶提取物进行了单个酚类物质的测定:主要结果:加入吐温 80 会减小未负载脂质体的大小,而加入 AMP 则会产生更大的脂质体。在这两种配方中,PE负载都会显著增加脂质体的大小,降低zeta电位值和大小分布的均匀性。在游离 PE 中,生物可利用度最高的多酚类物质是酚酸(3.20% 至 5.63%),而生物可利用度最低的是黄酮类物质,如咖啡酸苯乙酯、高良姜素、松果菊素和松果菊素(0.03% 至 2.12%)。两种脂质体蜂胶对酚类化合物的生物利用率都明显较高。含有 T80 和 AMP 的脂质体分别回收了未消化样品中酚类化合物总量的 52.43% 和 185.90%。含有 AMP 的脂质体不仅对 PE 有很高的溶解度,还能在体外消化过程中保护酚类化合物:结论:脂质体封装是一种很有前景的方法,可提高聚乙烯在消化液中的溶解度和稳定性,使其适用于蜂胶口服制剂的给药。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
ADMET and DMPK
ADMET and DMPK Multiple-
CiteScore
4.40
自引率
0.00%
发文量
22
审稿时长
4 weeks
期刊介绍: ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study
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