Lokman Hakim Nur Yasmin Diana, A/P Joginder Singh Hardeep Kaur, Kang Nien How, Siau Hui Mah, Zee Wei Lai
Faculty of Medical and Health Sciences, School of Biosciences, Taylor's University, Subang Jaya, Malaysia.
Dermatology Unit, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia.
Recent Adv Drug Deliv Formul. 2023 Apr 6. doi: 10.2174/2667387817666230406091232.
Kojic acid (KA), a fungal secondary metabolite, is commonly used in the cosmetic industry as a skin-whitening agent because of its ability to inhibit tyrosinase, the enzyme involved in melanin production. However, KA has shown poor depigmenting effects and becomes unstable after prolonged storage. Its use in cosmetics products has also been restricted due to its hydrophilic nature. To overcome these limitations, the structure of KA can be altered to form KA derivatives, such as KA ester (KAE), with improved chemical and biological properties. For instance, multiple studies have shown that KAE is more effective at inhibiting tyrosinase, is less toxic and more stable than KA, thus making it more beneficial. Aside from structural modification, nanotechnology applications such as nanoemulsion, and others have shown the ability to strengthen the efficacy of both KA and KAE by increasing skin permeability and delivering the drug more precisely to the targeted site with better controlled release rate. Therefore, the aim of this review article is to discuss the importance of modifying KA's chemical structure as well as the role of nanoemulsion, solid lipid nanoparticles (SLN), nanostructured lipid carrier (NLC), liposomes and ethosomes in improving topical delivery of KA and KAE for cosmetic and pharmaceutical applications.
曲酸(KA)是一种真菌次生代谢产物,因其能够抑制酪氨酸酶(参与黑色素生成的酶),在化妆品行业中常用作皮肤美白剂。然而,曲酸的色素脱除效果不佳,且长时间储存后会变得不稳定。由于其亲水性,它在化妆品中的使用也受到了限制。为克服这些局限性,可以改变曲酸的结构以形成曲酸衍生物,如曲酸酯(KAE),其化学和生物学性质均得到改善。例如,多项研究表明,曲酸酯在抑制酪氨酸酶方面比曲酸更有效,毒性更小且更稳定,因此更具优势。除了结构修饰外,纳米技术应用如纳米乳剂等已显示出通过增加皮肤渗透性以及以更好的控释速率将药物更精确地递送至靶向部位,从而增强曲酸和曲酸酯功效的能力。因此,本文综述的目的是讨论修饰曲酸化学结构的重要性以及纳米乳剂、固体脂质纳米粒(SLN)、纳米结构脂质载体(NLC)、脂质体和醇质体在改善曲酸和曲酸酯用于化妆品和制药应用的局部递送方面的作用。