a Laboratory for Biophysics of Lipid Aggregates, Faculty of Fundamental Problems of Technology, Wroclaw University of Science and Technology , Wroclaw , Poland.
b Lipid Systems sp z o.o , Wroclaw , Poland , and.
J Liposome Res. 2018 Jun;28(2):106-111. doi: 10.1080/08982104.2016.1275678. Epub 2017 Jan 18.
Octenidine dihydrochloride is an effective antiseptic compound which mode of action is based on destabilization plasma membrane of microorganisms. This ensures that microorganisms cannot develop the drug resistance in a straightforward way, as the entire cellular structure, rather than specific molecular target is affected. Since the octenidine is a hydrophobic compound, it requires organic solvent such as phenoxyethanol in order to be effectively administered. However, the presence of phenoxyethanol has strong irritating effect, particularly when applied on open wounds and mucous membranes. Phospholipids are known as neutral excipients free of side effects and in their aggregated form may serve as solvent for octenidine. In this article, we propose a new antiseptic formulation composed of equimolar ratio of lipids and octenidine. The resulting particles are ∼4 nm in diameter showing that their topology is different from that known for liposomes. The new formulation has proven to be equally effective as octenidine dihydrochloride formulation marketed under the name of Octenisept®. The main advantage of the new formulation is that it does not contain phenoxyethanol, which opens new possibilities for broader application spectrum of octenidine, including treatments of mucous membranes and open wounds.
双氯苯双胍己烷是一种有效的防腐剂，其作用模式基于破坏微生物的细胞膜。这确保了微生物不能以简单直接的方式产生耐药性，因为受影响的是整个细胞结构，而不是特定的分子靶点。由于双氯苯胍是一种疏水性化合物，它需要有机溶剂，如苯氧乙醇，才能有效地使用。然而，苯氧乙醇的存在具有强烈的刺激性，特别是在应用于开放性伤口和粘膜时。磷脂被认为是无副作用的中性赋形剂，在聚集状态下可作为双氯苯胍的溶剂。在本文中，我们提出了一种由等摩尔比的脂质和双氯苯胍组成的新型防腐剂配方。所得颗粒的直径约为 4nm，表明其拓扑结构与已知的脂质体不同。新配方与以 Octenisept®为名销售的盐酸双氯苯胍配方同样有效。新配方的主要优点是它不含有苯氧乙醇，这为双氯苯胍更广泛的应用范围开辟了新的可能性，包括治疗粘膜和开放性伤口。
