Silva Elton Luiz, Carneiro Guilherme, De Araújo Lidiane Advíncula, Trindade Mariana de Jesus Vaz, Yoshida Maria Irene, Oréfice Rodrigo Lambert, Farias Luis de Macêdo, De Carvalho Maria Auxiliadora Roque, Dos Santos Simone Gonçalves, Goulart Gisele Assis Castro, Alves Ricardo José, Ferreira Lucas Antônio Miranda
J Nanosci Nanotechnol. 2015 Jan;15(1):792-9. doi: 10.1166/jnn.2015.9184.
Topical therapy is the first choice for the treatment of mild to moderate acne and all-trans retinoic acid is one of the most used drugs. The combination of retinoids and antimicrobials is an innovative approach for acne therapy. Recently, lauric acid, a saturated fatty acid, has shown strong antimicrobial activity against Propionibacterium acnes. However, topical application of retinoic acid is followed by high incidence of side-effects, including erythema and irritation. Solid lipid nanoparticles represent an alternative to overcome these side-effects. This work aims to develop solid lipid nanoparticles loaded with retinoic acid and lauric acid and evaluate their antibacterial activity. The influence of lipophilic stearylamine on the characteristics of solid lipid nanoparticles was investigated. Solid lipid nanoparticles were characterized for size, zeta potential, encapsulation efficiency, differential scanning calorimetry and X-ray diffraction. The in vitro inhibitory activity of retinoic acid-lauric acid-loaded solid lipid nanoparticles was evaluated against Propionibacterium acnes, Staphylococcus aureus and Staphylococcus epidermidis. High encapsulation efficiency was obtained at initial time (94 ± 7% and 100 ± 4% for retinoic acid and lauric acid, respectively) and it was demonstrated that lauric acid-loaded-solid lipid nanoparticles provided the incorporation of retinoic acid. However, the presence of stearylamine is necessary to ensure stability of encapsulation. Moreover, retinoic acid-lauric acid-loaded solid lipid nanoparticles showed growth inhibitory activity against Staphylococcus epidermidis, Propionibacterium acnes and Staphylococcus aureus, representing an interesting alternative for the topical therapy of acne vulgaris.
局部治疗是轻至中度痤疮治疗的首选，全反式维甲酸是最常用的药物之一。维甲酸与抗菌剂联合使用是痤疮治疗的一种创新方法。最近，饱和脂肪酸月桂酸对痤疮丙酸杆菌显示出强大的抗菌活性。然而，局部应用维甲酸后副作用发生率较高，包括红斑和刺激。固体脂质纳米粒是克服这些副作用的一种替代方法。这项工作旨在开发负载维甲酸和月桂酸的固体脂质纳米粒，并评估其抗菌活性。研究了亲脂性硬脂胺对固体脂质纳米粒特性的影响。对固体脂质纳米粒的尺寸、zeta电位、包封率、差示扫描量热法和X射线衍射进行了表征。评估了负载维甲酸 - 月桂酸的固体脂质纳米粒对痤疮丙酸杆菌、金黄色葡萄球菌和表皮葡萄球菌的体外抑制活性。在初始时间获得了较高的包封率（维甲酸和月桂酸分别为94±7%和100±4%），并且证明负载月桂酸的固体脂质纳米粒能够包载维甲酸。然而，硬脂胺的存在对于确保包封稳定性是必要的。此外，负载维甲酸 - 月桂酸的固体脂质纳米粒对表皮葡萄球菌、痤疮丙酸杆菌和金黄色葡萄球菌显示出生长抑制活性，是寻常痤疮局部治疗的一种有前景的替代方法。
