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Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers

Authors Zhou J, Zhou D

Received 6 June 2015

Accepted for publication 10 July 2015

Published 18 September 2015 Volume 2015:9 Pages 5269—5275

DOI https://doi.org/10.2147/DDDT.S90016

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Prof. Dr. Wei Duan


Jun Zhou,1,2 Daxin Zhou3

1Department of Medicine, Clinical Medical College of Soochow University, 2Department of Medicine, Tongren Hospital, Shanghai Jiaotong University School of Medicine, 3Department of Cardiovascular Medicine, Zhongshan Hospital, Fudan University, Shanghai, People’s Republic of China

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.

Keywords: nanostructured lipid carriers, lovastatin, in vitro release, pharmacokinetic, pharmacodynamic

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