Journal
FITOTERAPIA
Volume 84, Issue -, Pages 64-71Publisher
ELSEVIER
DOI: 10.1016/j.fitote.2012.09.013
Keywords
20(S)-protopanaxadiol; Cubosome; Caco-2 cell monolayer; Rat intestinal perfusion model; Bioavailability
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Funding
- National Natural Science Foundation of China [81274068]
- Administration of Traditional Chinese Medicine of Jiangsu Province [LZ11066]
- open fund from the Key Laboratory of New Drug Delivery System of Chinese Materia Medica in Jiangsu Province Academy of Traditional Chinese Medicine [2011NDDCM02003]
- Foundation for High-level Talent on six areas of the Jiangsu province
- Suzhou City Science and Technology Development Plan [ZXY2012009]
- Key Laboratory of Traditional Chinese Medicine Oral Preparation of Chinese Traditional Medicine Release System [2011NDDCM01001]
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As with many other anti-cancer agents, 20(S)-protopanaxadiol (PPD) has a low oral absorption. In this study, in order to improve the oral bioavailability of PPD, the cubic nanoparticles that it contains were used to enhance absorption. Therefore, the cubic nanoparticle loaded PPD were prepared through the fragmentation of the glyceryl monoolein (GMO)/poloxamer 407 bulk cubic gel and were verified by transmission electron microscope, small angle X-ray scattering and differential scanning calorimetry. The in vitro release of 20(S)-protopanaxadiol from these nanoparticles was less than 5% at 12 h. And then Caco-2 cell monolayer model was used to evaluate the absorption of PPD in vitro. Meanwhile the rat intestinal perfusion model and bioavailability were also estimated in vivo. The results showed that, in the Caco-2 cell model, the PPD-cubosome could increase the permeability values from the apical (AP) to the basolateral (BL) of PPD at 53%. The result showed that the four-site rat intestinal perfusion model was consistent with the Caco-2 cell model. And the result of a pharmacokinetic study in rats showed that the relative bioavailability of the PPD-cubosome (AUC(0-infinity)) compared with the raw PPD (AUC(0-infinity)) was 169%. All the results showed that the PPD-cubosome enhanced bioavailability was likely due to the increased absorption by the cubic nanoparticles rather than by the improved release. Hence, the cubic nanoparticles may be a promising oral carrier for the drugs that have a poor oral absorption. (c) 2012 Elsevier B.V. All rights reserved.
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