Jhawat Vikas, Gupta Sumeet, Saini Vipin
a Department of Pharmacology , M. M. College of Pharmacy, M. M. University, Mullana , Ambala , Haryana, India.
Drug Deliv. 2016 Nov;23(9):3573-3581. doi: 10.1080/10717544.2016.1212439. Epub 2016 Aug 5.
In the present study, pluronic lecithin based organogels (PLO gels) were formulated as topical carrier for controlled delivery of mefenamic acid. Ten organogel formulations were prepared by a method employing lecithin as lipophilic phase and pluronic F-127 as hydrophilic phase in varying concentrations to study various parameters using in vitro diffusion study and in vivo studies. All formulations were found to be off-white, homogenous, and reluctant to be washed easily and have pH value within the range of 5.56-5.80 which is nonirritant. Polymer concentration increased in formulations of F1 to F5 (lecithin) and F6 to F10 (pluronic) resulted in decrease of the gelation temperature, increase of viscosity and reduction of spreadability of gels having polymer tendency to form rigid 3D network. Organogels with higher viscosity were found to be more stable and retard the drug release from the gel. The formulations of F2 and F3 were selected for kinetic studies and stability studies, as they found to have all physical parameters within acceptable limits, highest percent drug content and exhibited highest drug release in eight hours. The order of drug release from various formulations was found to be F2 > F3 > F10 > F4 > F1 > F9 > F8 > F5 > F7 > F6. The optimized formulation F2 was found to follow zero order rate kinetics showing controlled release of the drug from the formulations. In vivo anti-inflammatory activity of optimized mefenamic acid organogel (F2) against a standard marketed preparation (Volini gel) was found satisfactory and significant.
在本研究中,基于普朗尼克卵磷脂的有机凝胶(PLO凝胶)被制备为甲芬那酸控释的局部给药载体。通过采用卵磷脂作为亲脂相和不同浓度的普朗尼克F - 127作为亲水相的方法制备了十种有机凝胶制剂,以利用体外扩散研究和体内研究来考察各种参数。所有制剂均呈灰白色、均匀,不易被轻易洗去,pH值在5.56 - 5.80范围内,无刺激性。F1至F5(卵磷脂)和F6至F10(普朗尼克)制剂中聚合物浓度的增加导致凝胶化温度降低、粘度增加以及具有形成刚性三维网络聚合物倾向的凝胶的铺展性降低。发现粘度较高的有机凝胶更稳定,并能延缓药物从凝胶中的释放。选择F2和F3制剂进行动力学研究和稳定性研究,因为它们的所有物理参数均在可接受范围内,药物含量百分比最高,且在八小时内表现出最高的药物释放。发现各种制剂的药物释放顺序为F2>F3>F10>F4>F1>F9>F8>F5>F7>F6。发现优化后的制剂F2遵循零级速率动力学,表明药物从制剂中得到控释。优化后的甲芬那酸有机凝胶(F2)对市售标准制剂(沃利尼凝胶)的体内抗炎活性令人满意且具有显著性。