PDF(Pubmed)
Abstract：
UNASSIGNED: 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.
UNASSIGNED: 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.
UNASSIGNED: 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 (ER 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.
UNASSIGNED: Hair follicle-targeted delivery of AZA micro/nanocrystals provided a satisfactory alternative in promoting the treatment of acne vulgaris.
UNASSIGNED: 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.
UNASSIGNED: 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 (ER 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.
UNASSIGNED: Hair follicle-targeted delivery of AZA micro/nanocrystals provided a satisfactory alternative in promoting the treatment of acne vulgaris.
摘要：
■寻常痤疮是一种以毛囊为中心的慢性炎症性皮肤病，使毛囊靶向递送抗痤疮药物成为痤疮治疗的有希望的选择。然而,目前的研究只集中在传递到健康的毛囊，这与寻常痤疮中病理堵塞的毛囊本质上是不同的。
■通过湿介质研磨或高压均质化制备了具有不同粒径的壬二酸（AZA）微/纳米晶体。进行了AZA微/纳米晶体向健康毛囊递送的实验，使用和不使用物理增强技术。更重要的是,它创新地设计了一个实验，这可以揭示AZA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细胞模型和粉刺杆菌模型在体外评估AZA微/纳米晶体的抗炎和抗菌作用。最后,在体内比较了AZA微/纳米晶体和商业产品的抗痤疮作用和皮肤安全性。
■与商业产品相比，200nm和500nm的AZA微/纳米晶体表现出增加的靶向毛囊的能力。在AZA微/纳米晶体和超声的组合组中，穿透毛囊的能力进一步显着增强（ER值高达9.6）。然而,朝向堵塞的毛囊，AZA微/纳米晶体不能轻易地通过自身渗入。仅在1％水杨酸的帮助下，AZA微/纳米晶体具有很好的穿透堵塞的毛囊的潜力。还表明AZA微/纳米晶体通过抑制促炎因子和痤疮杆菌而具有抗炎和抗菌作用。与商业产品相比，AZA微/纳米晶体和超声的组合在皮肤安全性和体内抗痤疮治疗效果上都表现出明显的优势。
■毛囊靶向递送AZA微/纳米晶体在促进寻常痤疮治疗方面提供了令人满意的替代方案。
■通过湿介质研磨或高压均质化制备了具有不同粒径的壬二酸（AZA）微/纳米晶体。进行了AZA微/纳米晶体向健康毛囊递送的实验，使用和不使用物理增强技术。更重要的是,它创新地设计了一个实验，这可以揭示AZA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细胞模型和粉刺杆菌模型在体外评估AZA微/纳米晶体的抗炎和抗菌作用。最后,在体内比较了AZA微/纳米晶体和商业产品的抗痤疮作用和皮肤安全性。
■与商业产品相比，200nm和500nm的AZA微/纳米晶体表现出增加的靶向毛囊的能力。在AZA微/纳米晶体和超声的组合组中，穿透毛囊的能力进一步显着增强（ER值高达9.6）。然而,朝向堵塞的毛囊，AZA微/纳米晶体不能轻易地通过自身渗入。仅在1％水杨酸的帮助下，AZA微/纳米晶体具有很好的穿透堵塞的毛囊的潜力。还表明AZA微/纳米晶体通过抑制促炎因子和痤疮杆菌而具有抗炎和抗菌作用。与商业产品相比，AZA微/纳米晶体和超声的组合在皮肤安全性和体内抗痤疮治疗效果上都表现出明显的优势。
■毛囊靶向递送AZA微/纳米晶体在促进寻常痤疮治疗方面提供了令人满意的替代方案。
