Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Thailand.
AAPS PharmSciTech. 2012 Mar;13(1):323-35. doi: 10.1208/s12249-012-9751-1. Epub 2012 Jan 19.
Niosomes composed of Tween 61 and cholesterol at 1:1 molar ratio were entrapped with the mixture of the three semi-purified rice (Oryza sativa L., Family Gramineae) bran bioactive compounds [ferulic acid (F), γ-oryzanol (O), and phytic acid (P)] at 0.5%, 1.5%, and 1.5%, respectively, by the supercritical CO(2) technique. The transdermal absorption by vertical Franz diffusion cells of the compounds entrapped in niosomes (Nio FOP), the unentrapped compounds (Mixed FOP), the compounds incorporated in gel and cream (Gel FOP and Cream FOP), and the compounds entrapped in niosomes and incorporated in gel and cream (Gel nio and Cream nio) was investigated. At 6 h, F and P from Nio FOP gave lower cumulative amount in viable epidermis and dermis (VED) than from Mixed FOP of 1.1 and 1.6 times, respectively, while O from Nio FOP exhibited higher cumulative amount in VED than from Mixed FOP of 2.4 times. The highest cumulative amount in VED of F, O, and P were from Gel nio, Cream nio, and Mixed FOP at 1.564 ± 0.052, 15.972 ± 0.273, and 25.857 ± 0.025 ng/cm(2), respectively. Niosomes enhanced the transdermal absorption of the hydrophobic compound O, while retarded the hydrophilic compounds F and P indicating the less systemic risk of F and P than O when entrapped in niosomes. Thus, transdermal absorption of F, O, and P appeared to depend on niosomal size, lipophilicity of the bioactive compounds, and types of formulations. These preclinical results can be applied for the design of the clinical study of the developed rice bran niosomal topical products.
由 Tween 61 和胆固醇以 1:1 摩尔比组成的尼奥斯omes 用 0.5%、1.5%和 1.5%的三种半纯化稻（稻属禾本科）麸皮生物活性化合物[阿魏酸（F）、γ-谷维素（O）和植酸（P）]混合物包封，用超临界 CO2 技术。通过垂直 Franz 扩散细胞研究了包封在尼奥斯omes 中的化合物（Nio FOP）、未包封的化合物（混合 FOP）、掺入凝胶和乳膏中的化合物（Gel FOP 和 Cream FOP）以及包封在尼奥斯omes 中并掺入凝胶和乳膏中的化合物（Gel nio 和 Cream nio）的透皮吸收。在 6 小时时，与混合 FOP 相比，Nio FOP 中的 F 和 P 在活表皮和真皮（VED）中的累积量分别低 1.1 倍和 1.6 倍，而 Nio FOP 中的 O 在 VED 中的累积量比混合 FOP 高 2.4 倍。VED 中 F、O 和 P 的累积量最高的是凝胶 nio、奶油 nio 和混合 FOP，分别为 1.564 ± 0.052、15.972 ± 0.273 和 25.857 ± 0.025ng/cm2。尼奥斯omes 增强了疏水化合物 O 的透皮吸收，同时延迟了亲水性化合物 F 和 P 的吸收，这表明当 F 和 P 包封在尼奥斯omes 中时，比 O 具有更低的全身风险。因此，F、O 和 P 的透皮吸收似乎取决于尼奥斯omes 的大小、生物活性化合物的亲脂性以及制剂的类型。这些临床前结果可应用于开发的米糠尼奥斯omal 局部产品的临床研究设计。
