Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, People's Republic of China.
Nanjing Miaobang Meiye Enterprise Management Co, LTD, Nanjing, People's Republic of China.
Int J Nanomedicine. 2024 Jun 4;19:5173-5191. doi: 10.2147/IJN.S459788. eCollection 2024.
Acne vulgaris is a chronic inflammatory skin disorder centered on hair follicles, making hair follicle-targeted delivery of anti-acne drugs a promising option for acne treatment. However, current researches have only focused on the delivering to healthy hair follicles, which are intrinsically different from pathologically clogged hair follicles in acne vulgaris.
Azelaic acid (AZA) micro/nanocrystals with different particle sizes were prepared by wet media milling or high-pressure homogenization. An experiment on AZA micro/nanocrystals delivering to healthy hair follicles was carried out, with and without the use of physical enhancement techniques. More importantly, it innovatively designed an experiment, which could reveal the ability of AZA micro/nanocrystals to penetrate the constructed clogged hair follicles. The anti-inflammatory and antibacterial effects of AZA micro/nanocrystals were evaluated in vitro using a RAW264.7 cell model stimulated by lipopolysaccharide and a Cutibacterium acnes model. Finally, both the anti-acne effects and skin safety of AZA micro/nanocrystals and commercial products were compared in vivo.
In comparison to commercial products, 200 nm and 500 nm AZA micro/nanocrystals exhibited an increased capacity to target hair follicles. In the combination group of AZA micro/nanocrystals and ultrasound, the ability to penetrate hair follicles was further remarkably enhanced ( value up to 9.6). However, toward the clogged hair follicles, AZA micro/nanocrystals cannot easily penetrate into by themselves. Only with the help of 1% salicylic acid, AZA micro/nanocrystals had a great potential to penetrate clogged hair follicle. It was also shown that AZA micro/nanocrystals had anti-inflammatory and antibacterial effects by inhibiting pro-inflammatory factors and Cutibacterium acnes. Compared with commercial products, the combination of AZA micro/nanocrystals and ultrasound exhibited an obvious advantage in both skin safety and in vivo anti-acne therapeutic efficacy.
Hair follicle-targeted delivery of AZA micro/nanocrystals provided a satisfactory alternative in promoting the treatment of acne vulgaris.
寻常痤疮是一种以毛囊为中心的慢性炎症性皮肤病，使针对毛囊的抗痤疮药物递送至毛囊成为治疗痤疮的一种有前途的选择。然而，目前的研究仅集中于向健康的毛囊递药，而健康的毛囊与寻常痤疮中病理性堵塞的毛囊在本质上是不同的。
通过湿介质研磨或高压匀浆法制备不同粒径的壬二酸微/纳米晶体。进行了关于壬二酸微/纳米晶体向健康毛囊递药的实验，包括使用和不使用物理增强技术。更重要的是，设计了一项创新实验，可以揭示壬二酸微/纳米晶体穿透构建的堵塞毛囊的能力。使用脂多糖刺激的 RAW264.7 细胞模型和痤疮丙酸杆菌模型评估了壬二酸微/纳米晶体的抗炎和抗菌作用。最后，在体内比较了壬二酸微/纳米晶体和商业产品的抗痤疮效果和皮肤安全性。
与商业产品相比，200nm 和 500nm 的壬二酸微/纳米晶体具有增加的靶向毛囊的能力。在壬二酸微/纳米晶体和超声的联合组中，穿透毛囊的能力进一步显著增强（ 值高达 9.6）。然而，对于堵塞的毛囊，壬二酸微/纳米晶体本身不容易穿透。只有在 1%水杨酸的帮助下，壬二酸微/纳米晶体才有可能穿透堵塞的毛囊。研究还表明，壬二酸微/纳米晶体通过抑制促炎因子和痤疮丙酸杆菌具有抗炎和抗菌作用。与商业产品相比，壬二酸微/纳米晶体和超声的联合使用在皮肤安全性和体内抗痤疮治疗效果方面都具有明显的优势。
壬二酸微/纳米晶体的毛囊靶向递药为促进寻常痤疮的治疗提供了一种令人满意的替代方法。
