PMID:18054182
| Citation |
Ye, J, Wang, Q, Zhou, X and Zhang, N (2008) Injectable actarit-loaded solid lipid nanoparticles as passive targeting therapeutic agents for rheumatoid arthritis. Int J Pharm 352:273-9 |
|---|---|
| Abstract |
This work systematically studied the intravenous injection formulation of solid lipid nanoparticles (SLNs) loaded with actarit, a poor water soluble anti-rheumatic drug. The goal of this study was to design passive targeting nanoparticles which could improve therapeutic efficacy and reduce side-effects such as nephrotoxicity and gastrointestinal disorders commonly associated with oral formulations of actarit. Based on the optimized results of single-factor and orthogonal design, actarit-loaded SLNs were prepared by a modified solvent diffusion-evaporation method. The formulated SLNs were found to be relatively uniform in size (241+/-23 nm) with a negative zeta potential (-17.14+/-1.6 mV). The average drug entrapment efficiency and loading were (50.87+/-0.25)% and (8.48+/-0.14)%, respectively. The actarit-loaded SLNs exhibited a longer mean retention time in vivo (t(1/2(beta)), 9.373 h; MRT, 13.53 h) compared with the actarit 50% propylene glycol solution (t(1/2(ke)), 0.917 h; MRT, 1.323 h) after intravenous injection to New Zealand rabbits. The area under curve of plasma concentration-time (AUC) of actarit-loaded SLNs was 1.88 times greater than that of the actarit in 50% propylene glycol solution. The overall targeting efficiency (TE(C)) of the actarit-loaded SLNs was enhanced from 6.31% to 16.29% in spleen while the renal distribution of actarit was significantly reduced as compared to that of the actarit solution after intravenous administration to mice. These results indicated that injectable actarit-loaded solid lipid nanoparticles were promising passive targeting therapeutic agents for rheumatoid arthritis. |
| Links |
PubMed Online version:10.1016/j.ijpharm.2007.10.014 |
| Keywords |
Animals; Antirheumatic Agents/administration & dosage; Antirheumatic Agents/chemistry; Antirheumatic Agents/pharmacokinetics; Antirheumatic Agents/toxicity; Area Under Curve; Biological Availability; Chemistry, Pharmaceutical; Delayed-Action Preparations; Drug Carriers; Drug Compounding; Female; Injections, Intravenous; Kidney/metabolism; Lipids/chemistry; Male; Mice; Nanoparticles; Particle Size; Phenylacetates/administration & dosage; Phenylacetates/chemistry; Phenylacetates/pharmacokinetics; Phenylacetates/toxicity; Rabbits; Solubility; Spleen/metabolism; Technology, Pharmaceutical/methods; Tissue Distribution |
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