Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam, 786004, India.
Curr Drug Deliv. 2013 Dec;10(6):656-66. doi: 10.2174/156720181006131125150023.
Solid lipid nanoparticles (SLN) are very potential formulations for topical delivery of anti-inflammatory and anti-arthritic drugs. The solid state of the lipid particles enable efficient drug encapsulation and controlled drug release. In the present study, the evaluation of different formulation parameters based on variation of concentration of lipid and cosurfactant was studied. The SLN gel formulations of the dispersions were compared to the SLN dispersions and with the marketed gel of aceclofenac. The SLNs were prepared by high speed homogenization and ultra-sonication method with fixed amount of aceclofenac (10%) and pluronic F68 (1.5%). The particle size, zeta potential and span of developed formulations was found to be within the range of 123 nm to 323 nm, -12.4 to -18.5 and 0.42 to 0.86 respectively as the lipid concentration was increased from 7.5% to 40%. The highest entrapment efficiency was found to be 75% with the formulation having lipid concentration of 30% and 0.85% of phospholipon 90G. Permeation rate and controlled release property of xanthan gum loaded SLN gel formulations and SLN dispersion was studied through excised pig skin for 24hr. The drug release of SLN gel formulations was better controlled as compare to SLN dispersions. In vivo anti-inflammatory study showed that action of aceclofenac was enhanced for SLN dispersion and gel formulations. The results indicated the superiority of SLN based formulations for topical delivery of aceclofenac.
固体脂质纳米粒(SLN)是一种很有前途的用于局部递药的制剂,可递运抗炎和抗关节炎药物。由于脂质颗粒的固态特性,它能够实现高效的药物包封和药物控制释放。在本研究中,我们基于脂质和助表面活性剂浓度的变化,对不同制剂参数进行了评估。将分散体的 SLN 凝胶制剂与 SLN 分散体和市售的双氯芬酸钠凝胶进行了比较。采用高速匀化和超声法,以固定量的双氯芬酸钠(10%)和泊洛沙姆 F68(1.5%)制备 SLN。随着脂质浓度从 7.5%增加到 40%,所开发制剂的粒径、Zeta 电位和跨度分别为 123nm 至 323nm、-12.4 至-18.5 和 0.42 至 0.86。当脂质浓度为 30%且磷脂酰胆碱 90G 的浓度为 0.85%时,包封效率最高,达到 75%。通过 24 小时猪皮进行了 Xanthan 胶载 SLN 凝胶制剂和 SLN 分散体的渗透速率和控制释放研究。与 SLN 分散体相比,SLN 凝胶制剂的药物释放得到了更好的控制。体内抗炎研究表明,双氯芬酸钠 SLN 分散体和凝胶制剂的作用得到了增强。结果表明,基于 SLN 的制剂在双氯芬酸钠的局部递药方面具有优越性。