The Journal of Membrane Biology ( IF 2.3 ) Pub Date : 2021-05-03 , DOI: 10.1007/s00232-021-00180-3 Ghenwa Nasr 1, 2 , Hélène Greige-Gerges 1 , Abdelhamid Elaissari 2 , Nathalie Khreich 1
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Encapsulation in liposomes has been an efficient strategy to improve the stability of sensitive bioactive compounds such as essential oils (EOs). However, the stability of liposomal formulations remains a key parameter controlling the delivery of encapsulated ingredients. Cholesterol (Chol) modulates the membrane properties conferring stability to the lipid bilayer. Thus, the Chol content in the liposome formulations encapsulating EO components should be carefully chosen. In this work, various liposome formulations differing by Chol content (DPPC:Chol 100:10; 100:25; 100:50; 100:75; 100:100) were exposed to a series of 22 EO components at DPPC/EO 100/25. The formulations were characterized for their final composition and their permeability to the hydrophilic fluorophore, sulforhodamine B (SRB), was monitored. Results showed that the Chol content experimentally determined for the various formulations (above 10% Chol) was below the theoretical weighed Chol. Among the tested components, 13 molecules displayed a significant permeabilizing effect on 10% Chol membranes. Most of these possess a hydroxyl group. The EO induced permeability was dependent on the Chol content which affects the membrane phase: their effect was reduced upon increasing Chol content keeping five EOs components effective at 40% Chol. The EO’s effect was also linked to the hydrophobicity of the molecule. Hence, the DPPC:Chol ratio of the formulation is chosen considering the structure of the compound, its hydrophobicity and its effect on the permeability at different Chol content: a formulation comprising 40% Chol is suggested for highly hydrophobic molecules whereas a formulation with higher Chol content could be selected for less hydrophobic compounds.
Graphic Abstract
中文翻译：
脂质体对精油成分的渗透性：关注胆固醇含量
脂质体中的包裹一直是提高敏感生物活性化合物（如精油（EO））稳定性的有效策略。然而，脂质体制剂的稳定性仍然是控制封装成分递送的关键参数。胆固醇 (Chol) 调节膜特性，赋予脂质双层稳定性。因此，应仔细选择封装 EO 成分的脂质体制剂中的 Chol 含量。在这项工作中，各种脂质体配方因 Chol 含量而异（DPPC:Chol 100:10；100:25；100:50；100:75；100:100）在 DPPC/EO 100/ 下暴露于一系列 22 种 EO 组分25. 对制剂的最终组成进行了表征，并监测了它们对亲水性荧光团磺基罗丹明 B (SRB) 的渗透性。结果表明，通过实验确定的各种制剂的 Chol 含量（高于 10% Chol）低于理论称重的 Chol。在测试的组分中，13 个分子对 10% Chol 膜表现出显着的通透作用。其中大多数具有羟基。EO 诱导的渗透性取决于影响膜相的 Chol 含量：它们的影响随着 Chol 含量的增加而降低，保持五种 EOs 组分在 40% Chol 下有效。EO 的作用也与分子的疏水性有关。因此，配方的 DPPC:Chol 比率的选择要考虑到化合物的结构、疏水性及其在不同 Chol 含量下对渗透性的影响：
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