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Ibuprofen-loaded calcium phosphate granules : combination of innovative characterization methods to relate mechanical strength to drug location

Chevalier, Emilie and Viana, Marylène and Cazalbou, Sophie and Makein, Lisa and Dubois, Janie and Chulia, Dominique Ibuprofen-loaded calcium phosphate granules : combination of innovative characterization methods to relate mechanical strength to drug location. (2010) Acta Biomaterialia, 6 (1). 266-274. ISSN 1742-7061

(Document in English)

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Official URL: http://dx.doi.org/10.1016/j.actbio.2009.07.040


This paper studies the impact of the location of a drug substance on the physicochemical and mechanical properties of two types of calcium phosphate granules loaded with seven different contents of ibuprofen, ranging from 1.75% to 46%. These implantable agglomerates were produced by either low or high shear granulation. Unloaded Mi-Pro pellets presented higher sphericity and mechanical properties, but were slightly less porous than Kenwood granules (57.7% vs 61.2%). Nevertheless, the whole expected quantity of ibuprofen could be integrated into both types of granules. A combination of surface analysis, using near-infrared (NIR) spectroscopy coupling chemical imaging, and pellet porosity, by mercury intrusion measurements, allowed ibuprofen to be located. It was shown that, from 0% to 22% drug content, ibuprofen deposited simultaneously on the granule surface, as evidenced by the increase in surface NIR signal, and inside the pores, as highlighted by the decrease in pore volume. From 22%, porosity was almost filled, and additional drug substance coated the granule surfaces, leading to a large increase in the surface NIR signal. This coating was more regular for Mi-Pro pellets owing to their higher sphericity and greater surface deposition of drug substance. Unit crush tests using a microindenter revealed that ibuprofen loading enhanced the mechanical strength of granules, especially above 22% drug content, which was favorable to further application of the granules as a bone defect filler.

Item Type:Article
Additional Information:Thanks to Elsevier editor. The definitive version is available at http://www.sciencedirect.com The original PDF of the article can be found at Acta Biomaterialia website : http://www.sciencedirect.com/science/journal/17427061
Audience (journal):International peer-reviewed journal
Uncontrolled Keywords:
Institution:French research institutions > Centre National de la Recherche Scientifique - CNRS (FRANCE)
Université de Toulouse > Institut National Polytechnique de Toulouse - Toulouse INP (FRANCE)
Other partners > Université de Limoges - UNILIM (FRANCE)
Université de Toulouse > Université Toulouse III - Paul Sabatier - UT3 (FRANCE)
Other partners > Malvern Instruments Ltd (UNITED KINGDOM)
Other partners > Malvern Instruments Inc (USA)
Laboratory name:
Deposited On:22 Feb 2011 12:31

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