Cargando…

Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers

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 entrap...

Descripción completa

Detalles Bibliográficos
Autores principales: Zhou, Jun, Zhou, Daxin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4583105/
https://www.ncbi.nlm.nih.gov/pubmed/26425076
http://dx.doi.org/10.2147/DDDT.S90016
_version_ 1782391793687461888
author Zhou, Jun
Zhou, Daxin
author_facet Zhou, Jun
Zhou, Daxin
author_sort Zhou, Jun
collection PubMed
description 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.
format Online
Article
Text
id pubmed-4583105
institution National Center for Biotechnology Information
language English
publishDate 2015
publisher Dove Medical Press
record_format MEDLINE/PubMed
spelling pubmed-45831052015-09-30 Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers Zhou, Jun Zhou, Daxin Drug Des Devel Ther Original Research 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. Dove Medical Press 2015-09-18 /pmc/articles/PMC4583105/ /pubmed/26425076 http://dx.doi.org/10.2147/DDDT.S90016 Text en © 2015 Zhou and Zhou. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Zhou, Jun
Zhou, Daxin
Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers
title Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers
title_full Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers
title_fullStr Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers
title_full_unstemmed Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers
title_short Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers
title_sort improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4583105/
https://www.ncbi.nlm.nih.gov/pubmed/26425076
http://dx.doi.org/10.2147/DDDT.S90016
work_keys_str_mv AT zhoujun improvementoforalbioavailabilityoflovastatinbyusingnanostructuredlipidcarriers
AT zhoudaxin improvementoforalbioavailabilityoflovastatinbyusingnanostructuredlipidcarriers