Department of Pharmaceutics, I.T.S. Paramedical (Pharmacy) College, Muradnagar, Ghaziabad, Ultra Pradesh 201206, India.
Biomed Res Int. 2013;2013:750690. doi: 10.1155/2013/750690. Epub 2013 Aug 24.
Diclofenac sodium loaded solid lipid nanoparticles (SLNs) were formulated using guggul lipid as major lipid component and analyzed for physical parameters, permeation profile, and anti-inflammatory activity. The SLNs were prepared using melt-emulsion sonication/low temperature-solidification method and characterized for physical parameters, in vitro drug release, and accelerated stability studies, and formulated into gel. Respective gels were compared with a commercial emulgel (CEG) and plain carbopol gel containing drug (CG) for ex vivo and in vivo drug permeation and anti-inflammatory activity. The SLNs were stable with optimum physical parameters. GMS nanoparticle 1 (GMN-1) and stearic acid nanoparticle 1 (SAN-1) gave the highest in vitro drug release. Guggul lipid nanoparticle gel 3 (GLNG-3) showed 104.68 times higher drug content than CEG in receptor fluid. The enhancement ratio of GLNG-3 was 39.43 with respect to CG. GLNG-3 showed almost 8.12 times higher C(max) than CEG at 4 hours. The AUC value of GLNG-3 was 15.28 times higher than the AUC of CEG. GLNG-3 showed edema inhibition up to 69.47% in the first hour. Physicochemical properties of major lipid component govern the properties of SLN. SLN made up of guggul lipid showed good physical properties with acceptable stability. Furthermore, it showed a controlled drug release profile along with a promising permeation profile.
载有双氯芬酸钠的固体脂质纳米粒(SLN)是用古胶脂作为主要脂质成分制成的,并对其物理参数、渗透特性和抗炎活性进行了分析。SLN 是采用熔融乳化超声/低温固化法制备的,并对其物理参数、体外药物释放、加速稳定性研究进行了表征,并将其制成凝胶。将相应的凝胶与市售乳凝胶(CEG)和含有药物的普通卡波姆凝胶(CG)进行了比较,以进行体外和体内药物渗透和抗炎活性的比较。SLN 具有最佳的物理参数,稳定性好。GMS 纳米粒 1(GMN-1)和硬脂酸纳米粒 1(SAN-1)的体外药物释放率最高。古胶脂纳米粒凝胶 3(GLNG-3)在受体液中的药物含量比 CEG 高 104.68 倍。与 CG 相比,GLNG-3 的增强比为 39.43。GLNG-3 在 4 小时时的 C(max)几乎比 CEG 高 8.12 倍。GLNG-3 的 AUC 值比 CEG 高 15.28 倍。GLNG-3 在第 1 小时的抑制水肿作用高达 69.47%。主要脂质成分的物理化学性质决定了 SLN 的性质。由古胶脂制成的 SLN 具有良好的物理性质和可接受的稳定性。此外,它还显示出可控的药物释放特性和有前途的渗透特性。