Assessment of antimicrobial activity of melittin encapsulated in bicontinuous microemulsions prepared using renewable oils.
Assessment of antimicrobial activity of melittin encapsulated in bicontinuous microemulsions prepared using renewable oils.
复制标题
评估使用可再生油制备的双连续微乳液中封装的蜂毒肽的抗菌活性。
DOI：
10.1002/jsde.12654
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发表时间：
2023
影响因子：
1.6
通讯作者：
Urban,VolkerS
中科院分区：
文献类型：
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作者：
Oehler,MadisonA;Hayes,DouglasG;D'Souza,DorisH;Senanayake,Manjula;Gurumoorthy,Viswanathan;Pingali,SaiVenkatesh;O'Neill,HughM;Bras,Wim;Urban,VolkerS
本研究的目的是证明蜂毒肽（一种经过充分研究的抗菌肽（AMP））可以以活性形式溶解在采用生物相容性油的双连续微乳液（BME）中。所研究的系统包括由水/气溶胶-OT（AOT）/聚山梨酯85/肉豆蔻酸异丙酯组成的Winsor-III和-IV BME相以及使用聚山梨酯80和柠檬烯的Winsor-IV BME。我们发现蜂毒肽存在于富含α-螺旋的构型中，并且对于AOT/聚山梨酯85 Winsor-III系统而言处于非极性环境中，这表明蜂毒肽与表面活性剂单层相互作用并且处于活性构象。在两个Winsor-IV系统中也检测到蜂毒素的非极性环境，但程度低于Winsor-III系统。小角X射线散射分析表明，浓度为1.0 g/L的蜂毒肽对Winsor-IV系统的含水亚相产生了对BME结构的最大影响（例如，准周期性重复距离和相关长度的减小以及界面流动性的诱导）。评价了聚山梨酯80 Winsor-IV系统对慢性伤口和手术部位感染（SSI）中常见的几种细菌的抗菌活性。不含蜂毒肽的BME由于其油柠檬烯而抑制所有测试细菌的生长，而在BME中包含1.0 g/L蜂毒肽增强了对几种细菌的活性。蜂毒素浓度的进一步增加，在BME没有进一步的增强。这些结果证明了BME作为AMP和其他亲水性和亲脂性药物的递送平台的潜在效用，以抑制慢性伤口和SSI中的抗生素耐药性微生物。
The objective of this study is to demonstrate that melittin, a well‐studied antimicrobial peptide (AMP), can be solubilized in an active form in bicontinuous microemulsions (BMEs) that employ biocompatible oils. The systems investigated consisted of Winsor‐III and ‐IV BME phases composed of Water/Aerosol‐OT (AOT)/Polysorbate 85/isopropyl myristate and a Winsor‐IV BME employing Polysorbate 80 and limonene. We found that melittin resided in an α‐helix‐rich configuration and was in an apolar environment for the AOT/Polysorbate 85 Winsor‐III system, suggesting that melittin interacted with the surfactant monolayer and was in an active conformation. An apolar environment was also detected for melittin in the two Winsor‐IV systems, but to a lesser extent than the Winsor‐III system. Small‐angle X‐ray scattering analysis indicated that melittin at a concentration of 1.0 g/Laqin the aqueous subphase of the Winsor‐IV systems led to the greatest impact on the BME structure (e.g., decrease of quasi‐periodic repeat distance and correlation length and induction of interfacial fluidity). The antimicrobial activity of the Polysorbate 80 Winsor‐IV system was evaluated against several bacteria prominent in chronic wounds and surgical site infections (SSIs). Melittin‐free BMEs inhibited the growth of all tested bacteria due to its oil, limonene, while the inclusion of 1.0 g/Laqof melittin in the BMEs enhanced the activity against several bacteria. A further increase of melittin concentration in the BMEs had no further enhancement. These results demonstrate the potential utility of BMEs as a delivery platform for AMPs and other hydrophilic and lipophilic drugs to inhibit antibiotic‐resistant microorganisms in chronic wounds and SSIs.