Tags

Type your tag names separated by a space and hit enter

Formulation of ionic liquid APIs via spray drying processes to enable conversion into single and two-phase solid forms.
Int J Pharm. 2021 Jun 15; 603:120669.IJ

Abstract

Ionic liquid (IL) forms of drugs are increasingly being explored to address problems presented by poorly water-soluble drugs and solid-state stability. However, before ILs of active pharmaceutical ingredients (APIs) can be routinely incorporated into oral solid dosage forms (OSDs), challenges surrounding their ease of handling and manufacture must be addressed. To this end a framework for transforming API-ILs into solid forms at high loadings based on spray encapsulation using an immiscible polymer has recently been demonstrated. The current work demonstrates that this framework can be applied to a broad range of newly synthesized low glass transition temperature (Tg) API-ILs. Furthermore, the work explores a second novel approach to solidification of API-ILs based on polymer-API-IL miscibility that, to the best of our knowledge, has not been previously demonstrated. Modulated differential scanning calorimetry (mDSC) and attenuated total reflectance Fourier transform infrared spectroscopy showed that it was possible to produce spray dried solid materials, at acceptable loadings and yields for OSD applications in the form of both two-phase phase encapsulated systems and single phase amorphous solid dispersions (ASDs). This was achieved by the appropriate selection of an API-IL insoluble polymer (ethyl cellulose) for phase separated systems, or a miscible polymer with an exceptionally high Tg (the polysaccharide, maltodextrin) for the ASDs. Both approaches successfully overcame the Tg suppression associated with room temperature ILs. This work represents the first step to understanding the fundamental critical physical attributes of these systems to facilitate a more mechanistic methodology for their design.

Authors+Show Affiliations

School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland; SSPC, The SFI Research Centre for Pharmaceuticals, School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland; EPSRC-SFI Centre for Doctoral Training in Transformative Pharmaceutical Technologies, Ireland. Electronic address: evangelia.tsolaki@ucdconnect.ie.School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland. Electronic address: michael.stocker@ucdconnect.ie.SSPC, The SFI Research Centre for Pharmaceuticals, School of Pharmacy and Pharmaceutical Sciences, Panoz Institute, Trinity College Dublin, Dublin 2, Ireland. Electronic address: healyam@tcd.ie.School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland; SSPC, The SFI Research Centre for Pharmaceuticals, School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland; I-Form, The SFI Research Centre for Advanced Manufacturing, School of Chemical and Bioprocess Engineering, University College Dublin, Dublin 4, Ireland; National Institute for Bioprocess Research and Training, 24 Foster's Ave, Belfield, Blackrock, Co. Dublin A94 X099, Ireland. Electronic address: steven.ferguson@ucd.ie.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

33989753

Citation

Tsolaki, Evangelia, et al. "Formulation of Ionic Liquid APIs Via Spray Drying Processes to Enable Conversion Into Single and Two-phase Solid Forms." International Journal of Pharmaceutics, vol. 603, 2021, p. 120669.
Tsolaki E, Stocker MW, Healy AM, et al. Formulation of ionic liquid APIs via spray drying processes to enable conversion into single and two-phase solid forms. Int J Pharm. 2021;603:120669.
Tsolaki, E., Stocker, M. W., Healy, A. M., & Ferguson, S. (2021). Formulation of ionic liquid APIs via spray drying processes to enable conversion into single and two-phase solid forms. International Journal of Pharmaceutics, 603, 120669. https://doi.org/10.1016/j.ijpharm.2021.120669
Tsolaki E, et al. Formulation of Ionic Liquid APIs Via Spray Drying Processes to Enable Conversion Into Single and Two-phase Solid Forms. Int J Pharm. 2021 Jun 15;603:120669. PubMed PMID: 33989753.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation of ionic liquid APIs via spray drying processes to enable conversion into single and two-phase solid forms. AU - Tsolaki,Evangelia, AU - Stocker,Michael W, AU - Healy,Anne Marie, AU - Ferguson,Steven, Y1 - 2021/05/12/ PY - 2021/02/12/received PY - 2021/04/07/revised PY - 2021/04/30/accepted PY - 2021/5/15/pubmed PY - 2021/5/15/medline PY - 2021/5/14/entrez KW - Co-processed APIs KW - Ionic liquid APIs KW - Solid dispersions KW - Spray drying KW - Spray encapsulation SP - 120669 EP - 120669 JF - International journal of pharmaceutics JO - Int J Pharm VL - 603 N2 - Ionic liquid (IL) forms of drugs are increasingly being explored to address problems presented by poorly water-soluble drugs and solid-state stability. However, before ILs of active pharmaceutical ingredients (APIs) can be routinely incorporated into oral solid dosage forms (OSDs), challenges surrounding their ease of handling and manufacture must be addressed. To this end a framework for transforming API-ILs into solid forms at high loadings based on spray encapsulation using an immiscible polymer has recently been demonstrated. The current work demonstrates that this framework can be applied to a broad range of newly synthesized low glass transition temperature (Tg) API-ILs. Furthermore, the work explores a second novel approach to solidification of API-ILs based on polymer-API-IL miscibility that, to the best of our knowledge, has not been previously demonstrated. Modulated differential scanning calorimetry (mDSC) and attenuated total reflectance Fourier transform infrared spectroscopy showed that it was possible to produce spray dried solid materials, at acceptable loadings and yields for OSD applications in the form of both two-phase phase encapsulated systems and single phase amorphous solid dispersions (ASDs). This was achieved by the appropriate selection of an API-IL insoluble polymer (ethyl cellulose) for phase separated systems, or a miscible polymer with an exceptionally high Tg (the polysaccharide, maltodextrin) for the ASDs. Both approaches successfully overcame the Tg suppression associated with room temperature ILs. This work represents the first step to understanding the fundamental critical physical attributes of these systems to facilitate a more mechanistic methodology for their design. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/33989753/Formulation_of_ionic_liquid_APIs_via_spray_drying_processes_to_enable_conversion_into_single_and_two_phase_solid_forms_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(21)00474-9 DB - PRIME DP - Unbound Medicine ER -