The molecular mechanism behind the stabilization of insulin by choline and geranate (CAGE) ionic liquids – computational insights into oral insulin drug formulation

Palanisamy, Kandhan; Prakash, M.

doi:10.1039/d1cp03349b

Cited by 17 publications

(6 citation statements)

References 54 publications

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“…[131,141] Fortunately, choline and geranate (CAGE)-based IL formulations offer a new strategy. [55,[142][143][144] CAGE enables high-efficiency oral delivery of insulin by preventing its degradation by gastric acid and digestive enzymes, promoting paracellular transport, and increasing insulin absorption. Buccal administration of insulin-CAGE is another promising route of administration.…”

Section: Ionic Liquid-peptides and Ionic Liquid-proteinsmentioning

confidence: 99%

Ionic Liquids: Momentous Tools in Transdermal Delivery of Biomacromolecules

Tai

et al. 2023

Advanced Therapeutics

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Transdermal drug delivery is a promising strategy characterized by minor fluctuations in blood concentrations, few adverse effects, convenience, and excellent patient compliance, especially for biomacromolecules. Conversely, traditional delivery methods are limited by their poor penetration abilities and complex preparation and application techniques. However, some inherent properties of biomacromolecules, such as large sizes, complex structure, and poor stability, can affect their ability to overcome skin barriers and reach deeper layers. Ionic liquids (ILs) are organic salts composed of asymmetric cations and anions in liquid form below 100 °C. ILs provide excellent protection for biomacromolecules and can facilitate their passage through the stratum corneum to cells for therapeutic effects. Therefore, they represent one of the most promising approaches to promoting transdermal penetration. Here, the barriers to effective transdermal delivery, including skin properties and the stability and biocompatibility of IL‐based biomacromolecule formulations, are highlighted and the current status of IL‐based biomacromolecule formulations are focused on, the tremendous advantages of using ILs based on current challenges in transdermal drug delivery are discussed, and light is shed on several ILs frequently used in the delivery of biomacromolecules.

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Section: Ionic Liquid-peptides and Ionic Liquid-proteinsmentioning

confidence: 99%

Ionic Liquids: Momentous Tools in Transdermal Delivery of Biomacromolecules

Tai

et al. 2023

Advanced Therapeutics

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“…For example, the addition of a buffered choline–dihydrogen phosphate IL could substantially prolong the shelf-life of siRNA up to three months [ 73 ]. As another example, molecular simulation results indicated that CAGE could stabilize insulin by occupying the solvation shell of insulin, concomitantly exiling water molecules from the insulin surface [ 74 ]. Furthermore, an IL mixture of CAGE and choline–phenylpropanoic acid (CAPA) was designed to topically deliver siRNA for psoriasis treatment [ 10 ].…”

Section: Novel Pharmaceutical Strategies For Skin Penetrationmentioning

confidence: 99%

Novel Pharmaceutical Strategies for Enhancing Skin Penetration of Biomacromolecules

et al. 2022

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Skin delivery of biomacromolecules holds great advantages in the systemic and local treatment of multiple diseases. However, the densely packed stratum corneum and the tight junctions between keratinocytes stand as formidable skin barriers against the penetration of most drug molecules. The large molecular weight, high hydrophilicity, and lability nature of biomacromolecules pose further challenges to their skin penetration. Recently, novel penetration enhancers, nano vesicles, and microneedles have emerged as efficient strategies to deliver biomacromolecules deep into the skin to exert their therapeutic action. This paper reviews the potential application and mechanisms of novel skin delivery strategies with emphasis on the pharmaceutical formulations.

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“…47 Using an insulin dimer, Prakash and co-workers investigated a range of CAGE IL concentrations (0.05-1.00 mole fractions). 48 Their calculations reveal that, in the presence of water, choline and geranate ions easily occupy the first solvation shell of insulin. Moreover, for the 0.30-0.50 mole fraction of CAGE IL, intermolecular hydrogen bonding (H-bonding) interactions with insulin were eliminated due to the strong interactions between the geranate ions and water molecules.…”

Section: Introductionmentioning

confidence: 99%

Effect of mixtures of ionic liquids and water on the structure and stability of the insulin dimer: a combined DFT and MD simulation study

Lakshman,

Rubavathy,

Priyankha

et al. 2023

New J. Chem.

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The molecular mechanism behind the stabilization of insulin by choline and geranate (CAGE) ionic liquids – computational insights into oral insulin drug formulation

Abstract: Insulin is a principle hormone that is involved in the regulation of glucose levels in the blood. Oral insulin formulation is a recent development in drug delivery systems. Biocompatible choline-based...

Cited by 17 publications

References 54 publications

Ionic Liquids: Momentous Tools in Transdermal Delivery of Biomacromolecules

Ionic Liquids: Momentous Tools in Transdermal Delivery of Biomacromolecules

Novel Pharmaceutical Strategies for Enhancing Skin Penetration of Biomacromolecules

Effect of mixtures of ionic liquids and water on the structure and stability of the insulin dimer: a combined DFT and MD simulation study

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