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.

译文

:固体脂质纳米颗粒(SLN)是用于局部递送抗炎药和抗关节炎药的非常潜在的制剂。脂质颗粒的固态能够实现有效的药物包封和受控的药物释放。在本研究中,研究了基于脂质和辅助表面活性剂浓度变化对不同配方参数的评估。将分散体的SLN凝胶制剂与SLN分散体以及醋氯芬酸的市售凝胶进行比较。 SLN通过高速均质和超声法制备,固定量的醋氯芬酸(10%)和普朗尼克F68(1.5%)。发现随着脂质浓度从7.5%增加到40%,所开发制剂的粒度,ζ电势和跨度分别在123nm至323nm,-12.4至-18.5和0.42至0.86的范围内。发现具有30%脂质浓度和0.85%磷脂90G的制剂的最高包封率是75%。通过切下的猪皮24小时研究了载有黄原胶的SLN凝胶制剂和SLN分散体的渗透速率和控释性能。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,对于SLN分散液和凝胶制剂,醋氯芬酸的作用增强。结果表明基于SLN的制剂对醋氯芬酸的局部递送具有优越性。

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