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Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine

PURPOSE: To develop nanostructured-lipid carriers (NLCs) coated with cell-penetrating peptides (CPP) for improving the oral bioavailability of tripterine. METHODS: We prepared CPP-coated tripterine-loaded NLCs (CT-NLCs) by using a solvent evaporation method, and determined their physical properties....

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Autores principales: Chen, Yan, Yuan, Ling, Zhou, Lei, Zhang, Zhen-hai, Cao, Wei, Wu, Qingqing
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3428248/
https://www.ncbi.nlm.nih.gov/pubmed/22942642
http://dx.doi.org/10.2147/IJN.S34991
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author Chen, Yan
Yuan, Ling
Zhou, Lei
Zhang, Zhen-hai
Cao, Wei
Wu, Qingqing
author_facet Chen, Yan
Yuan, Ling
Zhou, Lei
Zhang, Zhen-hai
Cao, Wei
Wu, Qingqing
author_sort Chen, Yan
collection PubMed
description PURPOSE: To develop nanostructured-lipid carriers (NLCs) coated with cell-penetrating peptides (CPP) for improving the oral bioavailability of tripterine. METHODS: We prepared CPP-coated tripterine-loaded NLCs (CT-NLCs) by using a solvent evaporation method, and determined their physical properties. In vitro drug release was determined by using a dialysis bag diffusion technique, and intestinal toxicity was evaluated by performing MTT assay using Caco-2 cells. In vivo absorption was studied in an in situ rat intestinal perfusion model, and oral bioavailability was examined in beagles. RESULTS: The average particle size, zeta potential, and encapsulation efficiency of the optimized CT-NLCs were 126.7 ± 9.2 nm, 28.7 ± 3.4 mV, and 72.64% ± 1.37%, respectively. The CT-NLCs showed a controlled release profile in vitro and had significantly lower intestinal cytotoxicity than the tripterine solution (P < 0.05). The absorption levels of tripterine from the CT-NLCs in the rat duodenum and jejunum were markedly higher than with tripterine-loaded NLCs without the CPP coating (T-NLCs), and with tripterine solution. Pharmacokinetic study showed that the maximum concentration of the CT-NLCs was greater than that of the T-NLCs and tripterine suspension, and that the time to maximum concentration of the CT-NLCs as well as the T-NLCs, was longer than that of the tripterine suspension. The relative oral bioavailability of the CT-NLCs compared to that of tripterine suspension and T-NLCs were 484.75% and 149.91% respectively. CONCLUSION: The oral bioavailability of tripterine is dramatically increased by CT-NLCs. Therefore, CT-NLCs seem to be a promising carrier for oral delivery of tripterine.
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spelling pubmed-34282482012-08-31 Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine Chen, Yan Yuan, Ling Zhou, Lei Zhang, Zhen-hai Cao, Wei Wu, Qingqing Int J Nanomedicine Original Research PURPOSE: To develop nanostructured-lipid carriers (NLCs) coated with cell-penetrating peptides (CPP) for improving the oral bioavailability of tripterine. METHODS: We prepared CPP-coated tripterine-loaded NLCs (CT-NLCs) by using a solvent evaporation method, and determined their physical properties. In vitro drug release was determined by using a dialysis bag diffusion technique, and intestinal toxicity was evaluated by performing MTT assay using Caco-2 cells. In vivo absorption was studied in an in situ rat intestinal perfusion model, and oral bioavailability was examined in beagles. RESULTS: The average particle size, zeta potential, and encapsulation efficiency of the optimized CT-NLCs were 126.7 ± 9.2 nm, 28.7 ± 3.4 mV, and 72.64% ± 1.37%, respectively. The CT-NLCs showed a controlled release profile in vitro and had significantly lower intestinal cytotoxicity than the tripterine solution (P < 0.05). The absorption levels of tripterine from the CT-NLCs in the rat duodenum and jejunum were markedly higher than with tripterine-loaded NLCs without the CPP coating (T-NLCs), and with tripterine solution. Pharmacokinetic study showed that the maximum concentration of the CT-NLCs was greater than that of the T-NLCs and tripterine suspension, and that the time to maximum concentration of the CT-NLCs as well as the T-NLCs, was longer than that of the tripterine suspension. The relative oral bioavailability of the CT-NLCs compared to that of tripterine suspension and T-NLCs were 484.75% and 149.91% respectively. CONCLUSION: The oral bioavailability of tripterine is dramatically increased by CT-NLCs. Therefore, CT-NLCs seem to be a promising carrier for oral delivery of tripterine. Dove Medical Press 2012 2012-08-20 /pmc/articles/PMC3428248/ /pubmed/22942642 http://dx.doi.org/10.2147/IJN.S34991 Text en © 2012 Chen et al, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.
spellingShingle Original Research
Chen, Yan
Yuan, Ling
Zhou, Lei
Zhang, Zhen-hai
Cao, Wei
Wu, Qingqing
Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
title Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
title_full Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
title_fullStr Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
title_full_unstemmed Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
title_short Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
title_sort effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3428248/
https://www.ncbi.nlm.nih.gov/pubmed/22942642
http://dx.doi.org/10.2147/IJN.S34991
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