The antimicrobial activity of liposomal lauric acids against Propionibacterium acnes.
The antimicrobial activity of liposomal lauric acids against Propionibacterium acnes.
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DOI：
10.1016/j.biomaterials.2009.07.033
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发表时间：
2009-10
期刊：
影响因子：
14
通讯作者：
Zhang, Liangfang
中科院分区：
文献类型：
--
作者：
Yang, Darren;Pornpattananangkul, Dissaya;Nakatsuji, Teruaki;Chan, Michael;Carson, Dennis;Huang, Chun-Ming;Zhang, Liangfang
本研究评价了月桂酸（LA）及其脂质体衍生物对痤疮丙酸杆菌（P. acnes）的抗微生物活性，痤疮丙酸杆菌是一种促进炎症性痤疮的细菌。首先，三种游离脂肪酸（月桂酸、棕榈酸和油酸）的抗菌研究表明，LA对痤疮丙酸杆菌具有最强的杀菌活性。然而，使用LA作为炎性痤疮的潜在治疗的挫折是其水溶性差。然后将LA掺入脂质体制剂中以帮助其递送至痤疮丙酸杆菌。结果表明，LA不仅在其脂质体衍生物中保持了良好的抗菌活性，而且在低浓度下增强了抗菌活性。此外，载LA脂质体（LipoLA）的抗菌活性主要取决于单个脂质体的LA负载浓度。进一步的研究发现，LipoLA可以与痤疮丙酸杆菌的细胞膜融合，并将所携带的LA直接释放到细菌细胞膜中，从而有效地杀灭细菌。由于LA是一种天然化合物，是椰子油中的主要酸，也存在于人类母乳中，并且脂质体已成功并广泛应用于临床作为药物递送载体，因此本工作中开发的LipoLA具有成为寻常痤疮和其他痤疮丙酸杆菌相关疾病的天然，安全和有效的治疗药物的巨大潜力。
This study evaluated the antimicrobial activity of lauric acid (LA) and its liposomal derivatives against Propionibacterium acnes (P. acnes), the bacterium that promotes inflammatory acne. First, the antimicrobial study of three free fatty acids (lauric acid, palmitic acid and oleic acid) demonstrated that LA gives the strongest bactericidal activity against P. acnes. However, a setback of using LA as a potential treatment for inflammatory acne is its poor water solubility. Then the LA was incorporated into a liposome formulation to aid its delivery to P. acnes. It's demonstrated that the antimicrobial activity of LA was not only well maintained in its liposomal derivatives but also enhanced at low LA concentration. In addition, the antimicrobial activity of LA-loaded liposomes (LipoLA) mainly depended on the LA loading concentration per single liposomes. Further study found that the LipoLA could fuse with the membranes of P. acnes and release the carried LA directly into the bacterial membranes, thereby killing the bacteria effectively. Since LA is a natural compound that is the main acid in coconut oil and also resides in human breast milk and liposomes have been successfully and widely applied as a drug delivery vehicle in the clinic, the LipoLA developed in this work holds great potential of becoming an innate, safe and effective therapeutic medication for acne vulgaris and other P. acnes associated diseases.
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