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已发表论文

通过使用纳米结构脂质载体提高洛伐他汀 (Lovastatin) 的口服生物利用度

 

Authors Zhou J, Zhou DX
Received 6 June 2015
Accepted for publication 10 July 2015
Published 18 September 2015 Volume 2015:9 Pages 5269—5275
DOI http://dx.doi.org/10.2147/DDDT.S90016
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Rekha Dhanwani
Peer reviewer comments 2
Editor who approved publication: Professor Wei Duan

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, pharmacodynamics


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