Liu Xin, Chen Teng, Liu Xuesong, Chen Yong, Wang Longhu
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
J Oleo Sci. 2013;62(9):657-64. doi: 10.5650/jos.62.657.
The present study investigated the feasibility of ostrich oil utilizing as a promising vehicle for improved skin permeation of sinomenine with reference to vaseline matrix containing different content of chemical enhancers. The fatty acid composition of ostrich oil was analyzed by GC-MS. Penetration enhancing potential of ostrich oil on permeation of sinomenine across rat abdominal skin in vitro was studied using an automatic diffusion cell apparatus. The content of sinomenine percutaneous absorbed was determined by HPLC. Various parameters viz. steady-state skin flux (J(ss)), permeability coefficient (kP), cumulative amount of sinomenine (Q) and enhancement ratios (ER) were calculated from the permeation data. Fick's law of diffusion and Scheuplein kinetic were used to evaluate the transdermal absorbent enhancement of ostrich oil to sinomenine. Ostrich oil showed significant penetration effect on sinomenine compared with vaseline matrix containing different content of chemical enhancers, the density sequence as follow: 2% Azone > ostrich oil > 1% Azone plus 1% propylene glycol > 1% Azone > 3% Azone > 1% propylene glycol. The percutaneous endosmic rate constant (J(ss)) and permeability coefficient (k(P)) of sinomenine in ostrich oil through rat skin were 10.01 μg/cm²/h and 0.087, respectively. Ostrich oil produced stronger enhancement (ER = 24.31) with greater cumulative amount of drug permeated (255.53 μg/cm²) up to 24 h and caused no skin irritation. The drug release of sinomenine was coincided with Fick's equation. In summary, ostrich oil containing fatty acids is proposed as a promising adjuvant for use in cosmetics and pharmaceuticals for improved permeation of drug.
本研究考察了鸵鸟油作为一种有前景的载体，用于改善青藤碱经皮渗透的可行性，并以含有不同化学促渗剂含量的凡士林基质作为参照。采用气相色谱 - 质谱联用仪（GC - MS）分析鸵鸟油的脂肪酸组成。使用自动扩散池装置研究鸵鸟油对青藤碱体外透过大鼠腹部皮肤的促渗潜力。采用高效液相色谱法（HPLC）测定青藤碱经皮吸收的含量。根据渗透数据计算各种参数，即稳态皮肤通量（J(ss)）、渗透系数（kP）、青藤碱的累积量（Q）和增强倍数（ER）。利用菲克扩散定律和舍普林动力学来评估鸵鸟油对青藤碱的透皮吸收增强作用。与含有不同化学促渗剂含量的凡士林基质相比，鸵鸟油对青藤碱显示出显著的渗透效果，密度顺序如下：2%氮酮＞鸵鸟油＞1%氮酮加1%丙二醇＞1%氮酮＞3%氮酮＞1%丙二醇。青藤碱在鸵鸟油中透过大鼠皮肤的经皮渗透速率常数（J(ss)）和渗透系数（k(P)）分别为10.01 μg/cm²/h和0.087。鸵鸟油在2至4小时内产生更强的增强作用（ER = 24.31），药物透过的累积量更大（255.53 μg/cm²），且未引起皮肤刺激。青藤碱的药物释放符合菲克方程。总之，含有脂肪酸的鸵鸟油被认为是一种有前景的佐剂，可用于化妆品和药物中以改善药物的渗透。
