Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
Department of Pharmaceutics, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
J Cosmet Dermatol. 2024 Jan;23(1):289-295. doi: 10.1111/jocd.15933. Epub 2023 Jul 18.
Acne vulgaris can be treated topically with adapalene, a synthetic derivative of naphthoic acid with retinoid activity. Adapalene has a very low rate of percutaneous absorption and is almost completely insoluble in water. To obviate this problem, microemulsion (ME) carrier is used. The study's goals were to create and characterize adapalene-loaded ME and assess the drug's transfollicular route of penetration to see if hair follicles can serve as a conduit for the drug to enter the skin.
Adapalene microemulsions (MEs) are made by combining the right amounts of the cosurfactant (propylene glycol), surfactant (Tween 80 and Span 20), and oil phase (oleic acid-Transcutol P (10:1)). Physical and chemical characteristics of MEs, including droplet size, stability, viscosity, drug release, and in vitro skin permeability via guinea pigs' hairy and non-hairy skin, were assessed.
The range of 13.86-56.16 nm was found to be the average droplet size of ME formulations. The range of viscosities was 117-240 cps. The drug release profile reveals that 95.374 percent of the drug was released within the experiment's first 24 h. Compared to the adapalene control (aqueous suspension), all MEs enhanced the adapalene flow through both hairy and non-hairy skin. The surfactant/cosurfactant ratio had an impact on the amount of drug that passed through both skins because a larger ratio enhanced the adapalene affinity in the follicular route.
Furthermore, the proportions of the water and oil phases in formulations, as well as the S/C ratio, have a significant impact on the physicochemical characteristics and adapalene permeability across both pathways.
痤疮可以通过阿达帕林进行局部治疗，阿达帕林是一种具有类视黄醇活性的萘甲酸合成衍生物。阿达帕林的经皮吸收率非常低，几乎完全不溶于水。为了解决这个问题，使用了微乳液（ME）载体。该研究的目的是制备和表征载有阿达帕林的 ME，并评估药物的穿毛囊途径渗透，以观察毛囊是否可以作为药物进入皮肤的途径。
通过将适量的助表面活性剂（丙二醇）、表面活性剂（吐温 80 和司盘 20）和油相（油酸-Transcutol P（10:1））组合来制备阿达帕林微乳液（ME）。评估 ME 的物理化学特性，包括粒径、稳定性、粘度、药物释放以及通过豚鼠有毛和无毛皮肤的体外皮肤渗透性。
发现 ME 制剂的平均粒径范围为 13.86-56.16nm。粘度范围为 117-240cps。药物释放曲线表明，实验前 24 小时内释放了 95.374%的药物。与阿达帕林对照（水性混悬液）相比，所有 ME 均增强了阿达帕林在有毛和无毛皮肤中的流量。表面活性剂/助表面活性剂的比例对两种皮肤中药物的透过量有影响，因为较大的比例增强了在毛囊途径中的阿达帕林亲和力。
此外，制剂中水相和油相的比例以及 S/C 比例对理化特性和两种途径的阿达帕林渗透性有显著影响。
