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Understanding the performance of melt-extruded poly(ethylene oxide)-bicalutamide solid dispersions: characterisation of microstructural properties using thermal, spectroscopic and drug release methods.
J Pharm Sci. 2012 Jan; 101(1):200-13.JP

Abstract

In this article, we have prepared hot-melt-extruded solid dispersions of bicalutamide (BL) using poly(ethylene oxide) (PEO) as a matrix platform. Prior to preparation, miscibility of PEO and BL was assessed using differential scanning calorimetry (DSC). The onset of BL melting was significantly depressed in the presence of PEO, and using Flory-Huggins (FH) theory, we identified a negative value of -3.4, confirming miscibility. Additionally, using FH lattice theory, we estimated the Gibbs free energy of mixing which was shown to be negative, passing through a minimum at a polymer fraction of 0.55. Using these data, solid dispersions at drug-to-polymer ratios of 1:10, 2:10 and 3:10 were prepared via hot-melt extrusion. Using a combination of DSC, powder X-ray diffractometry and scanning electron microscopy, amorphous dispersions of BL were confirmed at the lower two drug loadings. At the 3:10 BL to PEO ratio, crystalline BL was detected. The percent crystallinity of PEO was reduced by approximately 10% in all formulations following extrusion. The increased amorphous content within PEO following extrusion accommodated amorphous BL at drug to polymer loadings up to 2:10; however, the increased amorphous domains with PEO following extrusion were not sufficient to fully accommodate BL at drug-to-polymer ratios of 3:10.

Authors+Show Affiliations

The Drug Delivery and Biomaterials Group, School of Pharmacy, Medical Biology Centre, Queen's University, Belfast BT9 7BL, Northern Ireland, UK.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

21905037

Citation

Abu-Diak, Osama A., et al. "Understanding the Performance of Melt-extruded Poly(ethylene Oxide)-bicalutamide Solid Dispersions: Characterisation of Microstructural Properties Using Thermal, Spectroscopic and Drug Release Methods." Journal of Pharmaceutical Sciences, vol. 101, no. 1, 2012, pp. 200-13.
Abu-Diak OA, Jones DS, Andrews GP. Understanding the performance of melt-extruded poly(ethylene oxide)-bicalutamide solid dispersions: characterisation of microstructural properties using thermal, spectroscopic and drug release methods. J Pharm Sci. 2012;101(1):200-13.
Abu-Diak, O. A., Jones, D. S., & Andrews, G. P. (2012). Understanding the performance of melt-extruded poly(ethylene oxide)-bicalutamide solid dispersions: characterisation of microstructural properties using thermal, spectroscopic and drug release methods. Journal of Pharmaceutical Sciences, 101(1), 200-13. https://doi.org/10.1002/jps.22748
Abu-Diak OA, Jones DS, Andrews GP. Understanding the Performance of Melt-extruded Poly(ethylene Oxide)-bicalutamide Solid Dispersions: Characterisation of Microstructural Properties Using Thermal, Spectroscopic and Drug Release Methods. J Pharm Sci. 2012;101(1):200-13. PubMed PMID: 21905037.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Understanding the performance of melt-extruded poly(ethylene oxide)-bicalutamide solid dispersions: characterisation of microstructural properties using thermal, spectroscopic and drug release methods. AU - Abu-Diak,Osama A, AU - Jones,David S, AU - Andrews,Gavin P, Y1 - 2011/09/08/ PY - 2011/05/23/received PY - 2011/07/18/revised PY - 2011/08/12/accepted PY - 2011/9/10/entrez PY - 2011/9/10/pubmed PY - 2012/5/10/medline SP - 200 EP - 13 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 101 IS - 1 N2 - In this article, we have prepared hot-melt-extruded solid dispersions of bicalutamide (BL) using poly(ethylene oxide) (PEO) as a matrix platform. Prior to preparation, miscibility of PEO and BL was assessed using differential scanning calorimetry (DSC). The onset of BL melting was significantly depressed in the presence of PEO, and using Flory-Huggins (FH) theory, we identified a negative value of -3.4, confirming miscibility. Additionally, using FH lattice theory, we estimated the Gibbs free energy of mixing which was shown to be negative, passing through a minimum at a polymer fraction of 0.55. Using these data, solid dispersions at drug-to-polymer ratios of 1:10, 2:10 and 3:10 were prepared via hot-melt extrusion. Using a combination of DSC, powder X-ray diffractometry and scanning electron microscopy, amorphous dispersions of BL were confirmed at the lower two drug loadings. At the 3:10 BL to PEO ratio, crystalline BL was detected. The percent crystallinity of PEO was reduced by approximately 10% in all formulations following extrusion. The increased amorphous content within PEO following extrusion accommodated amorphous BL at drug to polymer loadings up to 2:10; however, the increased amorphous domains with PEO following extrusion were not sufficient to fully accommodate BL at drug-to-polymer ratios of 3:10. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/21905037/Understanding_the_performance_of_melt_extruded_poly_ethylene_oxide__bicalutamide_solid_dispersions:_characterisation_of_microstructural_properties_using_thermal_spectroscopic_and_drug_release_methods_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)31769-X DB - PRIME DP - Unbound Medicine ER -