Formulation of ionic liquid APIs via spray drying processes to enable conversion into single and two-phase solid forms

Tsolaki, Evangelia; Stöcker, Michael; Healy, Anne Marie; Ferguson, Steven

doi:10.1016/j.ijpharm.2021.120669

Cited by 11 publications

(5 citation statements)

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“…Active pharmaceutical ingredient (API)-based ionic liquids (API-ILs) present an exciting new paradigm for the formulation of poorly water-soluble drugs since they can be used to mediate the release of APIs in response to external stimuli, increase bioavailability, and address polymorphism issues, taking advantage of their tunability and well-defined controlled release. − However, the API-IL strategy presents several challenges which demand deep research before it can be a viable approach to formulate APIs with poor aqueous solubility and replace other more mature techniques such as salt formation, solid dispersion, nanosuspensions, and micellar systems . Ionic liquids are generally difficult materials to work with as they generally exist at room temperature and pressure as viscous oils, making handling, processing, and formulation for different solid applications very problematic . To alleviate this, it has been shown that API-ILs can be combined with other materials such as ionogels or mesoporous silica or immobilized via microencapsulation, forming capsules with small size but vast total interfacial area .…”

Section: Introductionmentioning

confidence: 99%

“…11 Ionic liquids are generally difficult materials to work with as they generally exist at room temperature and pressure as viscous oils, making handling, processing, and formulation for different solid applications very problematic. 12 To alleviate this, it has been shown that API-ILs can be combined with other materials such as ionogels or mesoporous silica 9 or immobilized via microencapsulation, forming capsules with small size but vast total interfacial area. 13 Hence, microencapsulation of ionic liquids has been described to be an essential step in the production of, for example, delivery vehicles for chemical compounds 11,12,14,15 and of selflubricating coatings.…”

Section: Introductionmentioning

confidence: 99%

“…12 To alleviate this, it has been shown that API-ILs can be combined with other materials such as ionogels or mesoporous silica 9 or immobilized via microencapsulation, forming capsules with small size but vast total interfacial area. 13 Hence, microencapsulation of ionic liquids has been described to be an essential step in the production of, for example, delivery vehicles for chemical compounds 11,12,14,15 and of selflubricating coatings. 16 Nevertheless, when microencapsulation is not possible, the application of these solvents in processes at industrial scale and in separations involving labile species such as proteins and antioxidants is severely hampered mainly by their high density and significant toxicity.…”

Section: Introductionmentioning

confidence: 99%

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Thermophysical Properties of Mixtures Containing Cholinium l-Alaninate and Water, Ethanol, or Propan-1-ol

Velho,

Estevinho,

Macedo

2023

J. Chem. Eng. Data

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Choline amino acid ionic liquids (CAAILs) provide a greener alternative to classical ionic liquids, such as the ones based on imidazolium cations, since they can be obtained from natural sources with larger biodegradability. Given that most industrial extractions are performed in either aqueous or alcoholic media, the thermophysical characterization of binary mixtures containing these solvents is very important for process design. In this work, the influences of the mole fraction of ionic liquid and of temperature on the thermophysical properties of binary mixtures containing water, ethanol, or propan-1-ol and cholinium L-alaninate ([Ch][Ala]), a well-known CAAIL, were studied. Dynamic viscosity, shear stress, torque (T = 288.15 − 308.15 K), electrical conductivity (T = 298.15 K), and density (T = 293.15, 298.15, 303.15 K) were measured at 0.1 MPa, and the corresponding excess volumes were calculated and fitted to a Redlich−Kister (RK) equation. Moreover, the effect of temperature on density (T = 288.15 − 323.15 K), dynamic viscosity (T = 288.15 − 323.15 K), and refractive index (T = 288.15 − 343.15 K) of the synthesized [Ch][Ala] was also evaluated and compared with literature. Dynamic viscosities of the pure components were determined and fitted using the Vogel− Fulcher−Tammann−Hesse (VFTH) equation.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Thermophysical Properties of Mixtures Containing Cholinium l-Alaninate and Water, Ethanol, or Propan-1-ol

Velho,

Estevinho,

Macedo

2023

J. Chem. Eng. Data

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“…The obtained particles exhibited a mean size of 1.026 µm. Also, Stocker et al [ 36 ] and Tsolaki et al [ 37 ] spray-dried active pharmaceutical ingredient-ionic liquids into EC with a product yield that ranged between 67.9 and 87.8% (only in two cases was the product yield 24.8% and 29.9%), using a mini spray-dryer combined with the B-295 inert loop and two-fluid nozzle (1.5 mm cap and 0.7 mm tip). The EC concentration used was 2.5% ( w / v ).…”

Section: Resultsmentioning

confidence: 99%

Application of Ethyl Cellulose and Ethyl Cellulose + Polyethylene Glycol for the Development of Polymer-Based Formulations using Spray-Drying Technology for Retinoic Acid Encapsulation

Gonçalves

Rocha

Estevinho

2022

Foods

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Ethyl cellulose (EC)-based microparticles, with and without the incorporation of polyethylene glycol (PEG) as a second encapsulating agent, were prepared using the spray-drying process for the encapsulation of retinoic acid (RA). The production of a suitable controlled delivery system for this retinoid will promote its antitumor efficiency against acute promyelocytic leukemia (APL) due to the possibility of increasing the bioavailability of RA. Product yield ranged from 12 to 28% in all the microparticle formulations, including unloaded microparticles and RA-loaded microparticles. Microparticles with a mean diameter between 0.090 ± 0.002 and 0.54 ± 0.02 µm (number size distribution) and with an irregular form and rough surface were obtained. Furthermore, regarding RA-loaded microparticles, both polymer-based formulations exhibited an encapsulation efficiency of around 100%. A rapid and complete RA release was reached in 40 min from EC− and EC + PEG-based microparticles.

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“…Instead, when another material such as ethyl cellulose (EC) was used, the encapsulated API-IL remained in powder form in storage. This is probably due to the water-insolubility and immiscibility of EC with API-IL in contrast with the miscibility of MD with API-IL, which allowed EC to protect the API-IL from moisture more effectively than MD [ 66 ].…”

Section: Formulation Strategies To Reduce or Control Hygroscopicitymentioning

confidence: 99%

Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals

Ling

Hadinoto

2022

Pharmaceutics

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Highly hygroscopic pharmaceutical and nutraceutical solids are prone to significant changes in their physicochemical properties due to chemical degradation and/or solid-state transition, resulting in adverse effects on their therapeutic performances and shelf life. Moisture absorption also leads to excessive wetting of the solids, causing their difficult handling during manufacturing. In this review, four formulation strategies that have been employed to tackle hygroscopicity issues in oral solid dosage forms of pharmaceuticals/nutraceuticals were discussed. The four strategies are (1) film coating, (2) encapsulation by spray drying or coacervation, (3) co-processing with excipients, and (4) crystal engineering by co-crystallization. Film coating and encapsulation work by acting as barriers between the hygroscopic active ingredients in the core and the environment, whereas co-processing with excipients works mainly by adding excipients that deflect moisture away from the active ingredients. Co-crystallization works by altering the crystal packing arrangements by introducing stabilizing co-formers. For hygroscopic pharmaceuticals, coating and co-crystallization are the most commonly employed strategies, whereas coating and encapsulation are popular for hygroscopic nutraceuticals (e.g., medicinal herbs, protein hydrolysates). Encapsulation is rarely applied on hygroscopic pharmaceuticals, just as co-crystallization is rarely used for hygroscopic nutraceuticals. Therefore, there is potential for improved hygroscopicity reduction by exploring beyond the traditionally used strategy.

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Formulation of ionic liquid APIs via spray drying processes to enable conversion into single and two-phase solid forms

Cited by 11 publications

References 64 publications

Thermophysical Properties of Mixtures Containing Cholinium l-Alaninate and Water, Ethanol, or Propan-1-ol

Thermophysical Properties of Mixtures Containing Cholinium l-Alaninate and Water, Ethanol, or Propan-1-ol

Application of Ethyl Cellulose and Ethyl Cellulose + Polyethylene Glycol for the Development of Polymer-Based Formulations using Spray-Drying Technology for Retinoic Acid Encapsulation

Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals

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