Tran Thi-Quynh-Mai, Hsieh Ming-Fa, Chang Keng-Lun, Pho Quoc-Hue, Nguyen Van-Cuong, Cheng Ching-Yi, Huang Chun-Ming
International Master Program of Biomedical Material and Technology, Chung Yuan Christian University, 200 Chung-Pei Road, Chung Li District, Taoyuan City 32023, Taiwan.
Department of Biomedical Engineering, Chung Yuan Christian University, 200 Chung-Pei Road, Chung Li District, Taoyuan City 32023, Taiwan.
Polymers (Basel). 2016 Aug 27;8(9):321. doi: 10.3390/polym8090321.
Acne is the over growth of the commensal bacteria () on human skin. Lauric acid (LA) has been investigated as an effective candidate to suppress the activity of . Although LA is nearly insoluble in water, dimethyl sulfoxide (DMSO) has been reported to effectively solubilize LA. However, the toxicity of DMSO can limit the use of LA on the skin. In this study, LA-loaded poly(ɛ-caprolactone)-poly(ethylene glycol)-poly(ɛ-caprolactone) micelles (PCL-PEG-PCL) were developed to improve the bactericidal effect of free LA on . The block copolymers mPEG-PCL and PCL-PEG-PCL with different molecular weights were synthesized and characterized using ¹H Nuclear Magnetic Resonance spectroscopy (¹H NMR), Fourier-transform infrared spectroscopy (FT-IR), Gel Permeation Chromatography (GPC), and Differential Scanning Calorimetry (DSC). In the presence of LA, mPEG-PCL diblock copolymers did not self-assemble into nano-sized micelles. On the contrary, the average particle sizes of the PCL-PEG-PCL micelles ranged from 50⁻198 nm for blank micelles and 27⁻89 nm for LA-loaded micelles. The drug loading content increased as the molecular weight of PCL-PEG-PCL polymer increased. Additionally, the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) of free LA were 20 and 80 μg/mL, respectively. The MICs and MBCs of the micelles decreased to 10 and 40 μg/mL, respectively. This study demonstrated that the LA-loaded micelles are a potential treatment for acne.
痤疮是人体皮肤上共生细菌（）过度生长所致。月桂酸（LA）已被研究作为一种抑制该细菌活性的有效候选物。尽管LA几乎不溶于水，但据报道二甲基亚砜（DMSO）能有效溶解LA。然而，DMSO的毒性会限制LA在皮肤上的使用。在本研究中，开发了负载LA的聚（ε-己内酯）-聚（乙二醇）-聚（ε-己内酯）胶束（PCL-PEG-PCL），以提高游离LA对该细菌的杀菌效果。合成了不同分子量的嵌段共聚物mPEG-PCL和PCL-PEG-PCL，并使用¹H核磁共振光谱（¹H NMR）、傅里叶变换红外光谱（FT-IR）、凝胶渗透色谱（GPC）和差示扫描量热法（DSC）对其进行了表征。在有LA存在的情况下，mPEG-PCL二嵌段共聚物不会自组装成纳米尺寸的胶束。相反，PCL-PEG-PCL胶束的平均粒径对于空白胶束范围为50⁻198 nm，对于负载LA的胶束为27⁻89 nm。载药量随着PCL-PEG-PCL聚合物分子量的增加而增加。此外，游离LA的最低抑菌浓度（MIC）和最低杀菌浓度（MBC）分别为20和80 μg/mL。胶束的MIC和MBC分别降至10和40 μg/mL。本研究表明，负载LA的胶束是一种治疗痤疮的潜在方法。
