Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Student Research Committee, Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Artif Cells Nanomed Biotechnol. 2020 Dec;48(1):841-853. doi: 10.1080/21691401.2020.1770271.
Kojic acid (KA) as tyrosinase inhibitor shows insufficient skin penetration and several adverse events due topical administration. KA solid lipid nanoparticles (KA-SLNs) were prepared using high speed homogenisation followed by ultra-probe sonication method for improve its effectiveness.KA-SLNs was optimised by Glyceryl mono-stearate (GMS) and Cholesterol (Chol) as lipid excipients and span 60 (SP 60) and Tween 20 (Tw 20) as co-emulsifiers (particle size 156.97 ± 7.15 nm, encapsulation efficiency 59.02 ± 0.74%, drug loading 14.755 ± 1.63%, polydispersity index (PDI) of 0.388 ± 0.004 and zeta potential (ZP) of -27.67 ± 1.89 mV). Optimum formulation (KA-SLN dispersion) was stable at 4 and 25 °C for 3 months. Also, TEM image confirmed these results. The results of XRD, DSC and ATR-FTIR analysis indicated that KA was well encapsulated within the SLNs either in molecularly dispersed state and stabilised in amorphous form and there was no chemical interaction between drug and other ingredients. Controlled release was achieved with this formulation. KA-SLN dispersion have more tyrosinase inhibition potency in comparison with pure KA. Also, the results of the and percutaneous absorption show that KA-SLN dispersion improved percutaneous delivery of KA as a promising and potential novel topical preparation and might open new avenues for treatment of hyperpigmentation disorders.
曲酸（KA）作为酪氨酸酶抑制剂，由于经皮给药，其皮肤穿透性不足，且存在多种不良反应。采用高速匀化法，随后进行超音波探针处理，制备 KA 固体脂质纳米粒（KA-SLNs），以提高其功效。以单硬脂酸甘油酯（GMS）和胆固醇（Chol）作为脂质赋形剂，Span 60（SP 60）和 Tween 20（Tw 20）作为复合乳化剂，对 KA-SLNs 进行优化（粒径为 156.97±7.15nm，包封率为 59.02±0.74%，载药量为 14.755±1.63%，多分散指数（PDI）为 0.388±0.004，Zeta 电位（ZP）为-27.67±1.89mV）。最佳配方（KA-SLN 分散体）在 4℃和 25℃下可稳定 3 个月。此外，TEM 图像也证实了这一结果。XRD、DSC 和 ATR-FTIR 分析结果表明，KA 以分子分散状态良好地包封于 SLNs 中，处于无定形状态，且药物与其他成分之间无化学相互作用。该制剂实现了控释。与纯 KA 相比，KA-SLN 分散体具有更强的酪氨酸酶抑制作用。此外，经皮渗透吸收的结果表明，KA-SLN 分散体提高了 KA 的经皮递送，是一种有前途的新型局部制剂，可能为治疗色素沉着障碍开辟新的途径。
