Back to Browse Journals » International Journal of Nanomedicine » Volume 7

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

Authors Chen Y, Yuan L, Zhou L, Zhang Z, Cao W, Wu Q

Published Date August 2012 Volume 2012:7 Pages 4581—4591


Received 14 June 2012, Accepted 25 July 2012, Published 20 August 2012

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

Download Article [PDF] View Full Text [HTML] 

Creative Commons License 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 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:

Readers of this article also read:

Anti-αvβ3 antibody guided three-step pretargeting approach using magnetoliposomes for molecular magnetic resonance imaging of breast cancer angiogenesis

Yan C, Wu Y, Feng J, Chen W, Liu X, Hao P, Yang R, Zhang J, Lin B, Xu Y, Liu R

International Journal of Nanomedicine 2013, 8:245-255

Published Date: 11 January 2013

Impact of surface coating and particle size on the uptake of small and ultrasmall superparamagnetic iron oxide nanoparticles by macrophages

Saito S, Tsugeno M, Koto D, Mori Y, Yoshioka Y, Nohara S, Murase K

International Journal of Nanomedicine 2012, 7:5415-5421

Published Date: 10 October 2012

Cationic lipid-coated PEI/DNA polyplexes with improved efficiency and reduced cytotoxicity for gene delivery into mesenchymal stem cells

Song HM, Wang G, He B, Li L, Li CX, Lai YS, Xu XH, Gu ZW

International Journal of Nanomedicine 2012, 7:4637-4648

Published Date: 22 August 2012

Studying the effect of particle size and coating type on the blood kinetics of superparamagnetic iron oxide nanoparticles

Roohi F, Lohrke J, Ide A, Schuetz G, Dassler K

International Journal of Nanomedicine 2012, 7:4447-4458

Published Date: 10 August 2012

Lipid-based liquid crystalline nanoparticles as oral drug delivery vehicles for poorly water-soluble drugs: cellular interaction and in vivo absorption

Zeng N, Gao X, Hu Q, Song Q, Xia H, Liu Z, Gu G, Jiang M, Pang Z, Chen H, Chen J, Fang L

International Journal of Nanomedicine 2012, 7:3703-3718

Published Date: 13 July 2012

Evaluation of atherosclerotic lesions using dextran- and mannan–dextran-coated USPIO: MRI analysis and pathological findings

Tsuchiya K, Nitta N, Sonoda A, Nitta-Seko A, Ohta S, Takahashi M, Murata K, Mukaisho K, Shiomi M, Tabata Y, Nohara S

International Journal of Nanomedicine 2012, 7:2271-2280

Published Date: 3 May 2012

Role of aliskiren in cardio-renal protection and use in hypertensives with multiple risk factors

Eduardo Pimenta, Suzanne Oparil

Vascular Health and Risk Management 2009, 5:453-463

Published Date: 19 May 2009