Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, University under Section 3 of UGC Act-1956, Elite Status & Centre of Excellence-Govt. of Maharashtra, TEQIP Phase II Funded, Matunga, Mumbai, 400019, India.
AAPS PharmSciTech. 2013 Sep;14(3):1072-82. doi: 10.1208/s12249-013-9986-5. Epub 2013 Jul 2.
Lornoxicam is a potent oxicam class of non steroidal anti-inflammatory agent, prescribed for mild to moderate pain and inflammation. Niosomal gel of lornoxicam was developed for topical application. Lornoxicam niosomes (Lor-Nio) were fabricated by thin film hydration technique. Bilayer composition of niosomal vesicles was optimized. Lor-Nio dispersion was characterized by DSC, XRD, and FT-IR. Morphological evaluation was performed by scanning electron microscopy (SEM). Lor-Nio dispersion was incorporated into a gel using 2% w/w Carbopol 980 NF. Rheological and texture properties of Lor-Nio gel formulation showed suitability of the gel for topical application. The developed formulation was evaluated for in vitro skin permeation and skin deposition studies, occlusivity test and skin irritation studies. Pharmacodynamic activity of the Lor-Nio gel was performed by carragenan-induced rat paw model. Optimized Lor-Nio comprised of Span 60 and cholesterol in a molar ratio of 3:1 with 30 μM dicetyl palmitate as a stabilizer. It had particle size of 1.125 ± 0.212 μm (d 90), with entrapment efficiency of 52.38 ± 2.1%. DSC, XRD, and IR studies showed inclusion of Lor into niosomal vesicles. SEM studies showed spherical closed vesicular structure with particles in nanometer range. The in vitro skin permeation studies showed significant improvement in skin permeation and skin deposition for Lor-Nio gel (31.41 ± 2.24 μg/cm(2), 30.079 ± 1.2 μg/cm(2)) over plain lornoxicam gel (7.37 ± 1.27 μg/cm(2), 6.6 ± 2.52 μg/cm(2)). The Lor-Nio gel formulation showed enhanced anti-inflammatory activity by exhibiting mean edema inhibition (87.69 ± 1.43%) which was significantly more than the plain lornoxicam gel (53.84 ± 2.21%).
氯诺昔康是一种强效昔康类非甾体抗炎药，用于治疗轻度至中度疼痛和炎症。氯诺昔康的脂质体凝胶被开发用于局部应用。氯诺昔康脂质体（Lor-Nio）通过薄膜水化技术制备。优化了脂质体囊泡的双层组成。通过差示扫描量热法（DSC）、X 射线衍射（XRD）和傅里叶变换红外光谱（FT-IR）对 Lor-Nio 分散体进行了表征。通过扫描电子显微镜（SEM）进行了形态评价。将 Lor-Nio 分散体掺入含有 2%w/w Carbopol 980 NF 的凝胶中。Lor-Nio 凝胶制剂的流变学和质地特性表明该凝胶适合于局部应用。对所开发的制剂进行了体外皮肤渗透和皮肤沉积研究、封闭性试验和皮肤刺激性研究。通过角叉菜胶诱导的大鼠足模型进行了 Lor-Nio 凝胶的药效学活性研究。优化的 Lor-Nio 由摩尔比为 3:1 的 Span 60 和胆固醇组成，并用 30 μM 二硬脂酸甘油酯作为稳定剂。它的粒径为 1.125 ± 0.212 μm（d90），包封效率为 52.38 ± 2.1%。DSC、XRD 和 IR 研究表明 Lor 被包含在脂质体囊泡中。SEM 研究表明，具有纳米级粒子的球形封闭囊泡结构。体外皮肤渗透研究表明，Lor-Nio 凝胶（31.41 ± 2.24 μg/cm2，30.079 ± 1.2 μg/cm2）比普通氯诺昔康凝胶（7.37 ± 1.27 μg/cm2，6.6 ± 2.52 μg/cm2）显著提高了皮肤渗透和皮肤沉积。Lor-Nio 凝胶制剂通过表现出平均水肿抑制（87.69 ± 1.43%）显示出增强的抗炎活性，这显著高于普通氯诺昔康凝胶（53.84 ± 2.21%）。
