Polycaprolactone Based Nanoparticles Loaded with Indomethacin for Anti-Inflammatory Therapy: From Preparation to Ex Vivo Study
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This work focused on the preparation of polycaprolactone based nanoparticles containing indomethacin to provide topical analgesic and anti-inflammatory effect for symptomatic treatment of inflammatory diseases. Indomethacin loaded nanoparticles are prepared for topical application to decrease indomethacin side effects and administration frequency. Oppositely to already reported works, in this research non-invasive method has been used for the enhancement of indomethacin dermal drug penetration. Ex-vivo skin penetration study was carried out on fresh human skin.
Nanoprecipitation was used to prepare nanoparticles. Nanoparticles were characterized using numerous techniques; dynamic light scattering, SEM, TEM, DSC and FTIR. Regarding ex-vivo skin penetration of nanoparticles, confocal laser scanning microscopy has been used.
The results showed that NPs hydrodynamic size was between 220 to 245 nm and the zeta potential value ranges from −19 to −13 mV at pH 5 and 1 mM NaCl. The encapsulation efficiency was around 70% and the drug loading was about 14 to 17%. SEM and TEM images confirmed that the obtained nanoparticles were spherical with smooth surface. The prepared nanoparticles dispersions were stable for a period of 30 days under three temperatures of 4°C, 25°C and 40°C. In addition, CLSM images proved that obtained NPs can penetrate the skin as well.
The prepared nanoparticles are submicron in nature, with good colloidal stability and penetrate the stratum corneum layer of the skin. This formulation potentiates IND skin penetration and as a promising strategy would be able to decline the side effects of IND.
KEY WORDSanti-inflammatory indomethacin nanoparticles polycaprolactone skin penetration
- COX enzyme
Confocal laser scanning microscopy
Differential scanning calorimeter
Fourier transform infrared spectroscopy
Non-Steroidal Anti-inflammatory Drugs
Room temperature (25°C)
Scanning Electron Microscopy
Transmission Electron Microscopy
Acknowledgments and Disclosures
Waisudin Badri gratefully acknowledges French foreign affairs ministry and Afghanistan higher education ministry for providing the PhD scholarship.
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