Abstract
Aim:
To prepare a biodegradable polymeric carrier for oral delivery of a water-insoluble drug capsaicin (CAP) and evaluate its quality.
Methods:
CAP-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) nanoparticles (CAP/NPs) were prepared using a modified emulsification solvent diffusion technique. The quality of CAP/NPs were evaluated using transmission electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared techniques. A dialysis method was used to analyze the in vitro release profile of CAP from the CAP/NPs. Adult male rats were orally administered CAP/NPs (35 mg/kg), and the plasma concentrations of CAP were measured with a validated HPLC method. The morphology of rat gastric mucosa was studied with HE staining.
Results:
CAP/NPs had an average diameter of 82.54±0.51 nm, high drug-loading capacity of 14.0%±0.13% and high stability. CAP/NPs showed a biphasic release profile in vitro: the burst release was less than 25% of the loaded drug within 12 h followed by a more sustained release for 60 h. The pharmacokinetics study showed that the mean maximum plasma concentration was observed 4 h after oral administered of CAP/NPs, and approximately 90 ng/mL of CAP was detected in serum after 36 h. The area under the curve for the CAP/NPs group was approximately 6-fold higher than that for raw CAP suspension. Histological studies showed that CAP/NPs markedly reduced CAP-caused gastric mucosa irritation.
Conclusion:
CAP/NPs significantly enhance the bioavailability of CAP and markedly reduce gastric mucosa irritation in rats.
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Acknowledgements
This work was supported by the National Natural Science Foundation of China (30973677), National “Twelfth Five-Year” Plan for Science & Technology Support (2012BAD36B01), the Doctoral Fund of Ministry of Education of China (20113227110012), Special Funds for 333 (BRA2013198) and 331 Projects and Industry-University-Research Institution Cooperation (JHB2012-37, GY2012049, and GY2011028) in Jiangsu Province and Zhenjiang City. The authors also thank the Jiangsu University Ethics Committee for their guidance in the animal experiments.
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Peng, W., Jiang, Xy., Zhu, Y. et al. Oral delivery of capsaicin using MPEG-PCL nanoparticles. Acta Pharmacol Sin 36, 139–148 (2015). https://doi.org/10.1038/aps.2014.113
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DOI: https://doi.org/10.1038/aps.2014.113
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