Vu Quoc Lam, Fang Chih-Wun, Suhail Muhammad, Wu Pao-Chu
School of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 80708, Taiwan.
Department of Clinical Pharmacy, Thai Nguyen University of Medicine and Pharmacy, 284 Luong Ngoc Quyen Str., Thai Nguyen City 24000, Vietnam.
Pharmaceuticals (Basel). 2021 Nov 27;14(12):1233. doi: 10.3390/ph14121233.
Genistein, the most abundant isoflavone of the soy-derived phytoestrogen compounds, is a potent antioxidant and inhibitor of tyrosine kinase, which can inhibit UVB-induced skin carcinogenesis in hairless mice and UVB-induced erythema on human skin. In current study, genistein-loaded microemulsions were developed by using the various compositions of oil, surfactants, and co-surfactants and used as a drug delivery carrier to improve the solubility, peremability, skin whitening, and bioavailbility of genistein. The mean droplet size and polydispersity index of all formulations was less than 100 nm and 0.26 and demonstrated the formation of microemulsions. Similarly, various studies, such as permeation, drug skin deposition, pharmacokinetics, skin whitening test, skin irritation, and stability, were also conducted. The permeability of genistein was significantly affected by the composition of microemulsion formulation, particular surfactnat, and cosurfactant. In-vitro permeation study revealed that both permeation rate and deposition amount in skin were significantly increased from 0.27 μg/cm·h up to 20.00 μg/cm·h and 4.90 up to 53.52 μg/cm, respectively. In in-vivo whitening test, the change in luminosity index (ΔL*), tended to decrease after topical application of genistein-loaded microemulsion. The bioavailability was increased 10-fold by topical administration of drug-loaded microemulsion. Conclusively, the prepared microemulsion has been enhanced the bioavailability of genistein and could be used for clinical purposes.
染料木黄酮是大豆衍生的植物雌激素化合物中含量最丰富的异黄酮，是一种有效的抗氧化剂和酪氨酸激酶抑制剂，可抑制无毛小鼠中紫外线B诱导的皮肤癌发生以及人类皮肤中紫外线B诱导的红斑。在当前的研究中，通过使用油、表面活性剂和助表面活性剂的各种组合物开发了负载染料木黄酮的微乳剂，并将其用作药物递送载体，以提高染料木黄酮的溶解度、渗透性、皮肤美白效果和生物利用度。所有制剂的平均液滴尺寸和多分散指数均小于100 nm和0.26，表明形成了微乳剂。同样，还进行了各种研究，如渗透、药物皮肤沉积、药代动力学、皮肤美白试验、皮肤刺激性和稳定性研究。染料木黄酮的渗透性受微乳剂配方的组成，特别是表面活性剂和助表面活性剂的显著影响。体外渗透研究表明，渗透速率和皮肤中的沉积量分别从0.27 μg/cm·h显著增加到20.00 μg/cm·h，从4.90 μg/cm显著增加到53.52 μg/cm。在体内美白试验中，局部应用负载染料木黄酮的微乳剂后，亮度指数（ΔL*）的变化趋于降低。通过局部给药负载药物的微乳剂，生物利用度提高了10倍。总之，所制备的微乳剂提高了染料木黄酮的生物利用度，可用于临床目的。
