Yang Darren, Pornpattananangkul Dissaya, Nakatsuji Teruaki, Chan Michael, Carson Dennis, Huang Chun-Ming, Zhang Liangfang
Department of Nanoengineering, University of California, San Diego, La Jolla, CA 92093, USA.
Biomaterials. 2009 Oct;30(30):6035-40. doi: 10.1016/j.biomaterials.2009.07.033. Epub 2009 Aug 8.
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 was 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.
本研究评估了月桂酸(LA)及其脂质体衍生物对痤疮丙酸杆菌(P. acnes)的抗菌活性,痤疮丙酸杆菌是引发炎性痤疮的细菌。首先,对三种游离脂肪酸(月桂酸、棕榈酸和油酸)的抗菌研究表明,月桂酸对痤疮丙酸杆菌具有最强的杀菌活性。然而,将月桂酸用作炎性痤疮潜在治疗方法的一个障碍是其水溶性较差。随后,将月桂酸制成脂质体制剂,以帮助其递送至痤疮丙酸杆菌。结果表明,月桂酸的抗菌活性不仅在其脂质体衍生物中得到良好维持,而且在低月桂酸浓度下有所增强。此外,载有月桂酸的脂质体(LipoLA)的抗菌活性主要取决于单个脂质体的月桂酸负载浓度。进一步研究发现,LipoLA可与痤疮丙酸杆菌的细胞膜融合,并将携带的月桂酸直接释放到细菌膜中,从而有效杀灭细菌。由于月桂酸是一种天然化合物,是椰子油中的主要酸,也存在于人乳中,且脂质体已在临床上成功且广泛地用作药物递送载体,因此本研究中开发的LipoLA具有很大潜力成为寻常痤疮和其他与痤疮丙酸杆菌相关疾病的天然、安全且有效的治疗药物。