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Drug Dev Ind Pharm. 2014 Dec;40(12):1607-15. doi: 10.3109/03639045.2013.838581. Epub 2013 Sep 19.

Production of pure indinavir free base nanoparticles by a supercritical anti-solvent (SAS) method.

Author information

1
The Group of Biomaterials and Nanotechnology for Improved Medicines (BIONIMED), Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires , Buenos Aires , Argentina .

Abstract

CONTEXT:

This work investigated the production of pure indinavir free base nanoparticles by a supercritical anti-solvent method to improve the drug dissolution in intestine-like medium.

OBJECTIVE:

To increase the dissolution of the drug by means of a supercritical fluid processing method.

MATERIALS AND METHODS:

Acetone was used as solvent and supercritical CO2 as antisolvent. Products were characterized by dynamic light scattering (size, size distribution), scanning electron microscopy (morphology), differential scanning calorimetry (thermal behaviour) and X-rays diffraction (crystallinity).

RESULTS AND DISCUSSION:

Processed indinavir resulted in particles of significantly smaller size than the original drug. Particles showed at least one dimension at the nanometer scale with needle or rod-like morphology. Results of X-rays powder diffraction suggested the formation of a mixture of polymorphs. Differential scanning calorimetry analysis showed a main melting endotherm at 152 °C. Less prominent transitions due to the presence of small amounts of bound water (in the raw drug) or an unstable polymorph (in processed IDV) were also visible. Finally, drug particle size reduction significantly increased the dissolution rate with respect to the raw drug. Conversely, the slight increase of the intrinsic solubility of the nanoparticles was not significant.

CONCLUSIONS:

A supercritical anti-solvent method enabled the nanonization of indinavir free base in one single step with high yield. The processing led to faster dissolution that would improve the oral bioavailability of the drug.

KEYWORDS:

Drug dissolution; HIV; drug solubility; indinavir free base; pure drug nanoparticles; supercritical anti-solvent method

PMID:
24050705
DOI:
10.3109/03639045.2013.838581
[Indexed for MEDLINE]

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