title: Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers.
abstract: Nanostructured lipid carriers (NLCs) have been one of the systems of choice for improving the oral bioavailability of drugs with poor water solubility. In the present study, lovastatin (LVT)-loaded NLCs (LVT-NLCs) were successfully prepared by hot high-pressure homogenization method with high entrapment efficiency, drug loading, and satisfactory particle size distribution. The particles had almost spherical and uniform shapes and were well dispersed with a particle size of <50 nm (23.5 ± 1.6 nm) and a low polydispersity index (0.17 ± 0.05 mV). The result of stability showed that the LVT-NLCs dispersion maintained excellent stability without exhibiting any aggregation, precipitation, or phase separation at 4 °C for 6 months of storage. The LVT release data from all developed solid lipid nanoparticles (SLNs) and NLCs were best fitted to a Ritger-Peppas kinetic model (0.9832 and 0.9783 for NLCs and SLNs, respectively). This indicated that the release of LVT from the SLNs and NLCs was due to a combination of drug diffusion and erosion from the lipid matrix. The pharmacokinetic and pharmacodynamic results show that LVT-NLCs were better compared to free drug, which could be attributed to an increase in bioavailability.
authors.affiliation: Department of Medicine, Clinical Medical College of Soochow University, Shanghai, People's Republic of China ; Department of Medicine, Tongren Hospital, Shanghai Jiaotong University School of Medicine, Shanghai, People's Republic of China.
authors.forename: Jun
authors.initials: J
authors.lastname: Zhou
authors.affiliation: Department of Cardiovascular Medicine, Zhongshan Hospital, Fudan University, Shanghai, People's Republic of China.
authors.forename: Daxin
authors.initials: D
authors.lastname: Zhou
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D015415:Biomarkers / Q000097:blood; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol / Q000097:blood; D008076:Cholesterol, HDL / Q000097:blood; D004195:Disease Models, Animal; D004337:Drug Carriers; D004355:Drug Stability; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D006949:Hyperlipidemias / Q000097:blood / Q000175:diagnosis / Q000188:drug therapy*; D008148:Lovastatin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D008956:Models, Chemical; D053758:Nanoparticles; D017208:Rats, Wistar; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D015415:Biomarkers; D008076:Cholesterol, HDL; D004337:Drug Carriers; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D002784:Cholesterol; D008148:Lovastatin
keywords: in vitro release; lovastatin; nanostructured lipid carriers; pharmacodynamic; pharmacokinetic