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古胶脂质固体脂质纳米粒作为透皮给药的药物载体。

Solid lipid nanoparticles of guggul lipid as drug carrier for transdermal drug delivery.

机构信息

Department of Pharmaceutics, I.T.S. Paramedical (Pharmacy) College, Muradnagar, Ghaziabad, Ultra Pradesh 201206, India.

出版信息

Biomed Res Int. 2013;2013:750690. doi: 10.1155/2013/750690. Epub 2013 Aug 24.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0883/3766613/c62825d2b6ff/BMRI2013-750690.001.jpg

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