Teeranachaideekul Veerawat, Boribalnukul Putita, Morakul Boontida, Junyaprasert Varaporn Buraphacheep
Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.
Pharmaceutics. 2022 Oct 11;14(10):2160. doi: 10.3390/pharmaceutics14102160.
Nanostructured lipid carriers (NLC) were prepared from solid lipid (glyceryl monostearate, GMS) and vegetable oils, including palm oil (PO), rice bran oil (RBO) or virgin coconut oil (VCO), at different ratios (95:5, 90:10 and 80:20), while nanoemulsions (NE) were prepared with sole vegetable oils. After production, the particle size of the lutein-free NLC and NE was found to be between 100 and 150 nm and increased after loading with lutein. An increase in oil loading in NLC reduced the particle size and resulted in a less ordered lipid matrix and an increase in % entrapment efficiency. From the stability study, it was observed that the types of oils and oil content in the lipid matrix had an impact on the chemical stability of lutein. Regarding the release study, lutein-loaded NE showed higher release than lutein-loaded NLC. Both NLC and NE prepared from VCO exhibited higher release than those prepared from PO and RBO, respectively (p < 0.05). In contrast, among the formulations of NLC and NE, both lutein-loaded NLC and NE prepared from RBO showed the highest permeation through the human epidermis due to the skin enhancement effect of RBO. Based on all the results, the lipid nanocarriers composed of RBO could effectively enhance the chemical stability of lutein and promote drug penetration into the skin.
纳米结构脂质载体(NLC)由固体脂质(单硬脂酸甘油酯,GMS)和植物油(包括棕榈油(PO)、米糠油(RBO)或初榨椰子油(VCO))按不同比例(95:5、90:10和80:20)制备,而纳米乳液(NE)则仅用植物油制备。制备后,发现不含叶黄素的NLC和NE的粒径在100至150纳米之间,加载叶黄素后粒径增大。NLC中油含量的增加会降低粒径,并导致脂质基质的有序度降低以及包封效率百分比增加。从稳定性研究中观察到,脂质基质中的油类型和油含量对叶黄素的化学稳定性有影响。关于释放研究,加载叶黄素的NE显示出比加载叶黄素的NLC更高的释放率。由VCO制备的NLC和NE分别比由PO和RBO制备的表现出更高的释放率(p < 0.05)。相反,在NLC和NE的制剂中,由RBO制备的加载叶黄素的NLC和NE由于RBO的皮肤增强作用而显示出通过人表皮的最高渗透率。基于所有结果,由RBO组成的脂质纳米载体可以有效地提高叶黄素的化学稳定性并促进药物渗透到皮肤中。