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Oral delivery of capsaicin using MPEG-PCL nanoparticles.
- Source :
- Acta Pharmacologica Sinica; Jan2015, Vol. 36 Issue 1, p139-148, 10p
- Publication Year :
- 2015
-
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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 16714083
- Volume :
- 36
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Acta Pharmacologica Sinica
- Publication Type :
- Academic Journal
- Accession number :
- 100237305
- Full Text :
- https://doi.org/10.1038/aps.2014.113