Lung-targeting delivery of dexamethasone acetate loaded solid lipid nanoparticles
- 420 Downloads
The objective of the present study was to develop a novel solid lipid nanoparticle (SLN) for the lung-targeting delivery of dexamethasone acetate (DXM) by intravenous administration. DXM loaded SLN colloidal suspensions were prepared by the high pressure homogenization method. The mean particle size, drug loading capacity and drug entrapment efficiency (EE %) of SLNs were investigated. In vitro drug release was also determined. The biodistribution and lung-targeting efficiency of DXM-SLNs and DXM-solutions (DXM-sol) in mice after intravenous administration were studied using reversed-phase high-performance liquid chromatography (HPLC). The results (expressed as mean ± SD) showed that the DXM-SLNs had an average diameter of 552 ± 6.5 nm with a drug loading capacity of 8.79 ± 0.04% and an entrapment efficiency of 92.1 ± 0.41%. The in vitro drug release profile showed that the initial burst release of DXM from DXM-SLNs was about 68% during the first 2 h, and then the remaining drug was released gradually over the following 48 hours. The biodistribution of DXM-SLNs in mice was significantly different from that of DXM-sol. The concentration of DXM in the lung reached a maximum level at 0.5 h post DXM-SLNs injection. A 17.8-fold larger area under the curve of DXM-SLNs was achieved compared to that of DXM-sol. These results indicate that SLN may be promising lung-targeting drug carrier for lipophilic drugs such as DXM.
Key wordsDexamethasone acetate Solid lipid nanoparticles Lung-targeting
Unable to display preview. Download preview PDF.
- Chinese Pharmacopoeia, pp. 184 (2005).Google Scholar
- Huo, D. J., Deng, S. H., Li, L. B., and Ji, J., Studies on the poly(lactic-co-glycolic) acid microspheres of cisplatin for lungtargeting. Inf.J. Pharm., 289, 63–67 (2005).Google Scholar
- Lukowski, G. and Pflegel, P., Electron diffraction of solid lipid nanoparticles loaded with aciclovir.Pharmazie, 52, 642–643 (1997).Google Scholar
- Mühlen, zur A. and Mehnert, W., Drug release and release mechanism of prednisolone loaded solid lipid nanoparticles.Pharmazie, 53, 552 (1998).Google Scholar
- Serpe, L., Catalano, M. G., Cavalli, R., Ugazio, E., Bosco, O., Canaparoa, R., Muntoni, E., Frairia, R., Gasco, M. R., Eandi, M., and Zara, G. P., Cytotoxicity of anticancer drugs incorporated in solid lipid nanoparticles on HT-29 colorectal cancer cell line.Eur. J. Pharm. Biopharm., 58, 673–680 (2004).PubMedCrossRefGoogle Scholar
- Siekmann, B. and Westesen, K., Melt-homogenized solid lipid nanoparticles stabilized by the nonionic surfactant tyloxapol. I. Preparation and particle size determination.Pharm. Pharmacol. Lett., 3, 194–197 (1994).Google Scholar
- Speiser, P., Lipidnanopellets als Tragersystem fur Arzneimittel zur peroralen Anwendung. European Patent EP0167825 (1990).Google Scholar
- Tao, Z. W., Xu, Q. Y., Ye, Y. Q., Peng, P., and Wang, Z. R., Preparation andin vitro characterization of microspheres containing dexamethasone sodium phosphate.Chin. Hosp. Pharm. J., 26, 515–517 (2006).Google Scholar
- Wang, J. S., Zhu, J. B., Lu, R. Q., and Shen, W., Preparation of lung targeting azithromycin liposomes and its tissue distribution in mice.Acta Pharm. Sin., 40, 274–278 (2005).Google Scholar