Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine
Yan Chen,1 Ling Yuan,2 Lei Zhou,2 Zhen-hai Zhang,1 Wei Cao,2 Qingqing Wu2
1Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People's Republic of China; 2Department of Pharmaceutics, School of Pharmacy, Jiangsu University, Zhenjiang, Jiangsu, People's Republic of China
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.
Keywords: cell-penetrating peptides, nanostructured lipid carriers, tripterine, oral drug delivery, bioavailability
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. Permissions beyond the scope of the License are administered by Dove Medical Press Limited. Information on how to request permission may be found at: http://www.dovepress.com/permissions.php
Readers of this article also read:
Delivery of vincristine sulfate-conjugated gold nanoparticles using liposomes: a light-responsive nanocarrier with enhanced antitumor efficiency
Liu Y, He M, Niu MM, Zhao YQ, Zhu YZ, Li ZH, Feng NP
Published Date: 22 April 2015
Self-assembled micelles of amphiphilic poly(L-phenylalanine)-b-poly(L-serine) polypeptides for tumor-targeted delivery
Zhao ZM, Wang Y, Han J, Wang KL, Yang D, Yang YH, Du Q, Song YJ, Yin XX
Published Date: 12 December 2014
Probing the mechanical properties of TNF-α stimulated endothelial cell with atomic force microscopy [Corrigendum]
Lee SY, Zaske AM, Novellino T, Danila D, Ferrari M, Conyers J, Decuzzi P
Published Date: 23 May 2014
Adjuvanted poly(lactic-co-glycolic) acid nanoparticle-entrapped inactivated porcine reproductive and respiratory syndrome virus vaccine elicits cross-protective immune response in pigs [Corrigendum]
Binjawadagi B, Dwivedi V, Manickam C, Ouyang K, Wu Y, Lee LJ, Torrelles JB, Renukaradhya GJ
Published Date: 12 May 2014
Soosay Raj TA, Smith AM, Moore AS
Published Date: 5 December 2013
Qu X, Yao C, Wang J, Li Z, Zhang Z
Published Date: 26 April 2013
Zhang Y, Chen T
Published Date: 10 October 2012
Published Date: 27 July 2012
Marusza W, Mlynarczyk G, Olszanski R, Netsvyetayeva I, Obrowski M, Iannitti T, Palmieri B
Published Date: 27 July 2012