Bendas Ehab R, Tadros Mina I
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Kasr Elainy St, Cairo, Egypt.
AAPS PharmSciTech. 2007 Dec 14;8(4):E107. doi: 10.1208/pt0804107.
The main objective of the present work was to compare the transdermal delivery of salbutamol sulfate (SS), a hydrophilic drug used as a bronchodilator, from ethosomes and classic liposomes containing different cholesterol and dicetylphosphate concentrations. All the systems were characterized for shape, particle size, and entrapment efficiency percentage, by image analysis optical microscopy or transmission electron microscopy, laser diffraction, and ultracentrifugation, respectively. In vitro drug permeation via a synthetic semipermeable membrane or skin from newborn mice was studied in Franz diffusion cells. The selected systems were incorporated into Pluronic F 127 gels and evaluated for both drug permeation and mice skin deposition. In all systems, the presence of spherical-shaped vesicles was predominant. The vesicle size was significantly decreased (P < .05) by decreasing cholesterol concentration and increasing dicetylphosphate and ethanol concentrations. The entrapment efficiency percentage was significantly increased (P < .05) by increasing cholesterol, dicetylphosphate, and ethanol concentrations. In vitro permeation studies of the prepared gels containing the selected vesicles showed that ethosomal systems were much more efficient at delivering SS into mice skin (in terms of quantity and depth) than were liposomes or aqueous or hydroalcoholic solutions.
本研究的主要目的是比较硫酸沙丁胺醇（SS）（一种用作支气管扩张剂的亲水性药物）从含有不同胆固醇和磷酸二鲸蜡酯浓度的乙醇脂质体和经典脂质体中的透皮递送情况。所有体系分别通过图像分析光学显微镜或透射电子显微镜、激光衍射和超速离心法对形状、粒径和包封率进行了表征。在Franz扩散池中研究了通过合成半透膜或新生小鼠皮肤的体外药物渗透。将选定的体系掺入泊洛沙姆F 127凝胶中，并对药物渗透和小鼠皮肤沉积进行评估。在所有体系中，球形囊泡占主导地位。通过降低胆固醇浓度、增加磷酸二鲸蜡酯和乙醇浓度，囊泡尺寸显著减小（P < 0.05）。通过增加胆固醇、磷酸二鲸蜡酯和乙醇浓度，包封率显著提高（P < 0.05）。对含有选定囊泡的制备凝胶进行的体外渗透研究表明，乙醇脂质体体系在将SS递送至小鼠皮肤（在数量和深度方面）方面比脂质体或水性或水醇溶液更有效。
