Kojic Acid and Kojic Acid Ester: Review on Nanotechnology-based Approach for Enhancing the Delivery Efficacy.

Nur Yasmin Diana Lokman Hakim, Hardeep Kaur A/P Joginder Singh, How Kang Nien, Mah Siau Hui, Lai Zee Wei
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Abstract

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.

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曲酸和曲酸酯:纳米技术提高给药效能的研究进展。
曲酸(KA)是一种真菌次生代谢物,在化妆品行业中通常用作皮肤增白剂,因为它能够抑制酪氨酸酶,酪氨酸酶是一种参与黑色素生成的酶。然而,KA的脱色效果较差,长期储存后变得不稳定。由于其亲水性,它在化妆品中的使用也受到限制。为了克服这些限制,可以改变KA的结构,形成KA衍生物,如KA酯(KAE),具有更好的化学和生物性能。例如,多项研究表明,KAE比KA更有效地抑制酪氨酸酶,毒性更小,稳定性更强,因此更有益。除了结构修饰外,纳米技术的应用,如纳米乳等,已经显示出通过增加皮肤渗透性和以更好的控制释放率更精确地将药物输送到目标部位来增强KA和KAE疗效的能力。因此,本文的目的是讨论修饰KA的化学结构的重要性,以及纳米乳、固体脂质纳米颗粒(SLN)、纳米结构脂质载体(NLC)、脂质体和脂质体在改善KA和KAE在化妆品和制药应用中的局部递送中的作用。
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