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Physico-chemical characterization and in vivo evaluation of indomethacin ethyl ester-loaded nanocapsules by PCS, TEM, SAXS, interfacial alkaline hydrolysis and antiedematogenic activity.
- Source :
-
Journal of nanoscience and nanotechnology [J Nanosci Nanotechnol] 2006 Sep-Oct; Vol. 6 (9-10), pp. 3154-62. - Publication Year :
- 2006
-
Abstract
- Nanocapsules are vesicular drug carriers constituted of an oil core, a polymeric wall, and surfactants. A general understanding about the influence of the polymeric wall of nanocapsules on the release profiles of drugs is not known. So, this work was devoted to characterize formulations prepared without polymer or containing it at different concentrations. The indomethacin ethyl ester was used as model and the strategy was based on its interfacial alkaline hydrolysis simulating a sink condition for the release. The antiedematogenic activity in rats for ester-loaded-nanocarriers was also evaluated. The nanocapsules (NC) and nanoemulsion (NE) presented particle sizes below 300 nm, polydispersity lower than 1.2 and pH around 5. SAXS analyses showed that the sorbitan monostearate is dissolved in the oil and the polymer presents regions of crystallinity independently on the PCL concentration. TEM analyses showed droplets (NE) and spherical particles (NC). The time for the total disappearance of the ester varied from 12 h to 24 h depending on the polymer concentration. The biexponential model showed that the indomethacin ester was essentially entrapped within the nanocarriers in an extension of 85 to 95%. The half-lives varied from 147 to 289 min for the sustained phases and from 3 to 6 min for the burst phases. The ester-loaded-NC showed significant antiedematogenic activity, while the ester-loaded-NE did not inhibit the carrageenin-induced paw edema. The nanocapsules promoted the absorption of the indomethacin ethyl ester and the presence of the polymer is important to achieve the pharmacological effect.
- Subjects :
- Alkalies chemistry
Animals
Anti-Inflammatory Agents, Non-Steroidal administration & dosage
Anti-Inflammatory Agents, Non-Steroidal chemistry
Edema pathology
Hydrolysis
Indomethacin administration & dosage
Indomethacin chemistry
Male
Microscopy, Electron, Transmission
Molecular Conformation
Particle Size
Rats
Rats, Wistar
Treatment Outcome
X-Ray Diffraction
Capsules chemistry
Edema drug therapy
Indomethacin analogs & derivatives
Nanostructures chemistry
Nanostructures ultrastructure
Subjects
Details
- Language :
- English
- ISSN :
- 1533-4880
- Volume :
- 6
- Issue :
- 9-10
- Database :
- MEDLINE
- Journal :
- Journal of nanoscience and nanotechnology
- Publication Type :
- Academic Journal
- Accession number :
- 17048531
- Full Text :
- https://doi.org/10.1166/jnn.2006.417