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Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
| Content Provider | Scilit |
|---|---|
| Author | Yuan, Ling Zhang, Zhen-Hai Wei, Cao Zhou, Lei Wu, Qingqing Chen, Yan |
| Copyright Year | 2012 |
| Description | Journal: International Journal of Nanomedicine 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. |
| Related Links | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3428248/pdf https://www.dovepress.com/getfile.php?fileID=13697 |
| Ending Page | 4591 |
| Page Count | 11 |
| Starting Page | 4581 |
| e-ISSN | 11782013 |
| DOI | 10.2147/IJN.S34991 |
| Journal | International Journal of Nanomedicine |
| Volume Number | 7 |
| Language | English |
| Publisher | Informa UK Limited |
| Publisher Date | 2012-08-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: International Journal of Nanomedicine Pharmacology and Pharmacy Bioavailability Cell-penetrating Peptides Nanostructured Lipid Carriers Oral Drug Delivery |
| Content Type | Text |
