Production of haloperidol loaded PLGA nanoparticles for extended controlled drug release of haloperidol

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controlled release
haloperidol
nanoparticles
PLGA end groups
drug-delivery
Polymer and Organic Materials
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This study developed an emulsion-solvent evaporation method for producing haloperidol-loaded PLGA nanoparticles with up to 2% (wt/wt. of polymer) drug content, in vitro release duration of over 13 days and less than 20% burst release. The free haloperidol is removed from the nanoparticle suspension using a novel solid phase extraction technique. This leads to a more accurate determination of drug incorporation efficiency than the typical washing methods. It was discovered that PLGA end groups have a strong influence on haloperidol incorporation efficiency and its release from PLGA nanoparticles. The hydroxyl-terminated PLGA (uncapped) nanoparticles have a drug incorporation efficiency of more than 30% as compared to only 10% with methyl-terminated PLGA (capped) nanoparticles. The in vitro release profile of nanoparticles with uncapped PLGA has a longer release period and a lower initial burst as compared to capped PLGA. By varying other processing and materials parameters, the size, haloperidol incorporation and haloperidol release of the haloperidol-loaded PLGA nanoparticles were controlled.

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2005-11-01
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Postprint version. Published in Journal of Microencapsulation, Volume 22, Issue 7, November 2005, pages 773-785. Publisher URL: http://dx.doi.org/10.1080/02652040500273753
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