Rehman Khurram, Mohd Amin Mohd Cairul Iqbal, Zulfakar Mohd Hanif
Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia.
J Oleo Sci. 2014;63(10):961-70. doi: 10.5650/jos.ess14101. Epub 2014 Sep 25.
Polymer-Fish oil bigel (hydrogel/oleogel colloidal mixture) was developed by using fish oil and natural (sodium alginate) and synthetic (hydroxypropyl methylcellulose) polymer for pharmaceutical purposes. The bigels were closely monitored and thermal, rheological and mechanical properties were compared with the conventional hydrogels for their potential use as an effective transdermal drug delivery vehicle. Stability of the fish oil fatty acids (especially eicosapentanoic acid, EPA and docosahexanoic acid, DHA) was determined by gas chromatography and the drug content (imiquimod) was assessed with liquid chromatography. Furthermore, in vitro permeation study was conducted to determine the capability of the fish oil-bigels as transdermal drug delivery vehicle. The bigels showed pseudoplastic rheological features, with excellent mechanical properties (adhesiveness, peak stress and hardness), which indicated their excellent spreadability for application on the skin. Bigels prepared with mixture of sodium alginate and fish oil (SB1 and SB2), and the bigels prepared with the mixture of hydroxypropyl methylcellulose and fish oil (HB1-HB3) showed high cumulative permeation and drug flux compared to hydrogels. Addition of fish oil proved to be beneficial in increasing the drug permeation and the results were statistically significant (p < 0.05, one-way Anova, SPSS 20.0). Thus, it can be concluded that bigel formulations could be used as an effective topical and transdermal drug delivery vehicle for pharmaceutical purposes.
聚合物-鱼油双凝胶（水凝胶/油凝胶胶体混合物）是通过使用鱼油以及天然聚合物（海藻酸钠）和合成聚合物（羟丙基甲基纤维素）开发而成，用于制药目的。对双凝胶进行了密切监测，并将其热性能、流变学性能和机械性能与传统水凝胶进行了比较，以评估其作为有效的透皮给药载体的潜力。通过气相色谱法测定鱼油脂肪酸（尤其是二十碳五烯酸，EPA和二十二碳六烯酸，DHA）的稳定性，并用液相色谱法评估药物含量（咪喹莫特）。此外，进行了体外渗透研究，以确定鱼油双凝胶作为透皮给药载体的能力。双凝胶呈现假塑性流变学特征，具有优异的机械性能（粘附性、峰值应力和硬度），这表明它们在皮肤上涂抹时具有出色的铺展性。与水凝胶相比，用海藻酸钠和鱼油混合物制备的双凝胶（SB1和SB2）以及用羟丙基甲基纤维素和鱼油混合物制备的双凝胶（HB1-HB3）显示出较高的累积渗透率和药物通量。事实证明，添加鱼油有助于提高药物渗透率，结果具有统计学意义（p < 0.05，单因素方差分析，SPSS 20.0）。因此，可以得出结论，双凝胶制剂可作为一种有效的局部和透皮给药载体用于制药目的。
