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Impregnation of mesoporous silica with poor aqueous soluble molecule using pressurized carbon dioxide: Is the solubility in the supercritical and subcritical phase a critical parameter?
Eur J Pharm Sci. 2020 Jul 01; 150:105332.EJ

Abstract

Recently, mesoporous silica (MS) has been used as a material able to maintain amorphous state of active compounds and therefore, enhance the oral bioavailability of BCSII drugs. Among impregnation methods of MS, techniques using supercritical carbon dioxide (Sc-CO2) are promising tools. Solubility of compounds in Sc-CO2 is reported as one of the most critical parameters, which usually limits its use in drug formulation. Indeed, most of compounds have poor solubility in Sc-CO2. The aim of this work is to compare different MS and to study alternative processes using pressurized CO2 for insoluble molecule in Sc-CO2. By using high pressure reactor, DSC, HPLC and in vitro dissolution tests, the crystallinity and dissolution profiles of MS with different pore size (6.6 nm, 25.0 nm and 2.5 nm) impregnated with fenofibrate (FF) under Sc-CO2 were compared to select the most appropriate carrier. Then, the selected MS has been impregnated under supercritical, subcritical and atmospheric conditions. We have shown that the MS pore size of 6.6 nm provides the higher amorphous drug loading capacity as well as the faster and higher drug dissolution. In addition, FF-MS formulations produced with pressurized CO2 as fusion medium, both in subcritical and supercritical conditions; give similar crystallinity and dissolution results compared to those produced with supercritical fluids as solvent. Through this study, we show new possibilities of using CO2 for insoluble compounds in this fluid.

Authors+Show Affiliations

University of Liège, Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Avenue Hippocrate B36 (+2), 4000, Liège, Belgium.University of Liège, Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Avenue Hippocrate B36 (+2), 4000, Liège, Belgium.University of Liège, Center for Education and Research on Macromolecules, CERM, Allée du Six Ao슩t B6a (+3) 4000, Liège, Belgium.University of Liège, Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Avenue Hippocrate B36 (+2), 4000, Liège, Belgium.University of Liège, Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Avenue Hippocrate B36 (+2), 4000, Liège, Belgium.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32361178

Citation

Koch, N, et al. "Impregnation of Mesoporous Silica With Poor Aqueous Soluble Molecule Using Pressurized Carbon Dioxide: Is the Solubility in the Supercritical and Subcritical Phase a Critical Parameter?" European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 150, 2020, p. 105332.
Koch N, Jennotte O, Grignard B, et al. Impregnation of mesoporous silica with poor aqueous soluble molecule using pressurized carbon dioxide: Is the solubility in the supercritical and subcritical phase a critical parameter? Eur J Pharm Sci. 2020;150:105332.
Koch, N., Jennotte, O., Grignard, B., Lechanteur, A., & Evrard, B. (2020). Impregnation of mesoporous silica with poor aqueous soluble molecule using pressurized carbon dioxide: Is the solubility in the supercritical and subcritical phase a critical parameter? European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 150, 105332. https://doi.org/10.1016/j.ejps.2020.105332
Koch N, et al. Impregnation of Mesoporous Silica With Poor Aqueous Soluble Molecule Using Pressurized Carbon Dioxide: Is the Solubility in the Supercritical and Subcritical Phase a Critical Parameter. Eur J Pharm Sci. 2020 Jul 1;150:105332. PubMed PMID: 32361178.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Impregnation of mesoporous silica with poor aqueous soluble molecule using pressurized carbon dioxide: Is the solubility in the supercritical and subcritical phase a critical parameter? AU - Koch,N, AU - Jennotte,O, AU - Grignard,B, AU - Lechanteur,A, AU - Evrard,B, Y1 - 2020/05/01/ PY - 2020/02/05/received PY - 2020/03/28/revised PY - 2020/03/30/accepted PY - 2020/5/4/pubmed PY - 2020/5/4/medline PY - 2020/5/4/entrez KW - Amorphous KW - Impregnation KW - Solubility enhancement KW - Subcritical KW - Supercritical SP - 105332 EP - 105332 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 150 N2 - Recently, mesoporous silica (MS) has been used as a material able to maintain amorphous state of active compounds and therefore, enhance the oral bioavailability of BCSII drugs. Among impregnation methods of MS, techniques using supercritical carbon dioxide (Sc-CO2) are promising tools. Solubility of compounds in Sc-CO2 is reported as one of the most critical parameters, which usually limits its use in drug formulation. Indeed, most of compounds have poor solubility in Sc-CO2. The aim of this work is to compare different MS and to study alternative processes using pressurized CO2 for insoluble molecule in Sc-CO2. By using high pressure reactor, DSC, HPLC and in vitro dissolution tests, the crystallinity and dissolution profiles of MS with different pore size (6.6 nm, 25.0 nm and 2.5 nm) impregnated with fenofibrate (FF) under Sc-CO2 were compared to select the most appropriate carrier. Then, the selected MS has been impregnated under supercritical, subcritical and atmospheric conditions. We have shown that the MS pore size of 6.6 nm provides the higher amorphous drug loading capacity as well as the faster and higher drug dissolution. In addition, FF-MS formulations produced with pressurized CO2 as fusion medium, both in subcritical and supercritical conditions; give similar crystallinity and dissolution results compared to those produced with supercritical fluids as solvent. Through this study, we show new possibilities of using CO2 for insoluble compounds in this fluid. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/32361178/Impregnation_of_mesoporous_silica_with_poor_aqueous_soluble_molecule_using_pressurized_carbon_dioxide:_Is_the_solubility_in_the_supercritical_and_subcritical_phase_a_critical_parameter L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(20)30121-4 DB - PRIME DP - Unbound Medicine ER -
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