Drug Delivery

Combinatorial chemistry and high-throughput screening accelerate the research and development of new medicines. Approximately 40% of drug candidates and up to 70% of marketed drugs are poorly water-soluble and, consequently, are plagued with poor bioavailability and delivery problems ^[1]. Strategies such as solid dispersions, nanoemulsions, micelles, cyclodextrin inclusions, and nanoparticles, have been widely adopted to deliver poorly water-soluble drugs and have shown great potential in the enhancement of bioavailability. However, large amount of organic solvents used in manufacturing of these formulations have significant human health and environmental pollution concerns ^[2]. Therefore, green techniques are required for the effective delivery of poorly water-soluble drugs. Ionic liquids are often used as green alternatives to traditional organic solvents due to their environmental friendliness and tunable structure. They can improve drug delivery by enhancing the solubility and permeability of drug substances. Thus, the use of ionic liquids can be used as an effective solution to facilitate drug delivery.

As green and tailorable solvents, ionic liquids are effective in solubilizing poorly water-soluble drugs, even for those poorly soluble in organic solvents. For example, drugs such as amphotericin B, danazol, albendazole, itraconazole, erythromycin, paclitaxel and coumarin are insoluble in water, whereas different ionic liquids can enhance their solubility by hundreds to tens of thousand-fold. Even compared with traditional solvents such as methanol, ethanol, and dimethylsulfoxide, ionic liquids still present excellent solubilizing capacity ^[3].

In addition to solubility, permeability is also a key determinant for the druggability and bioavailability of a drug substance. Once dissolved, drug molecules should be absorbed into the blood circulation to achieve their therapeutical effects, which requires permeation of drug molecules across various biomembranes, such as the cornea for ocular absorption, the epithelium for oral or pulmonary absorption, and the stratum corneum for transdermal absorption. As new permeation enhancers, ionic liquids play a huge role in facilitating transdermal drug delivery. For instance, 1.6-3.4-fold enhancements in permeability coefficient were found in transdermal delivery of diltiazem from a variety of ionic liquids compared to the solution alternative ^[4].

Once a satisfactory drug formulation has been prepared, delivery poses the next challenge. Ionic liquids have environmentally friendly characteristics and can be used as green solvents for drugs with poor solubility in water or even in organic solvents. In addition, they can help permeation of drug molecules incluing small chemical drugs and biomacromolecules across different biomembranes. With in-depth knowledge of drug delivery theory and advanced ionic liquid technology, Alfa chemistry has the ability to provide effective solutions to a variety of problems encountered in the application of ionic liquids in drug delivery, thus contributing to the development of the medical industry and human health.

Why Choose Us

Alfa Chemistry can provide customers with a variety of ionic liquids for drug delivery and customize efficient and high-quality drug delivery solutions for the needs of customers. If you have any questions related to drug delivery, please feel free to contact us.

References

• Shekhawat, P. B.; Pokharkar, V. B. Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles. Acta pharmaceutica sinica B. 2017, 7(3): 260-280.
• Clarke, C. J.; et al. Green and sustainable solvents in chemical processes. Chemical Reviews. 2018, 118(2): 747-800.
• Huang, W.; et al. Ionic liquids: green and tailor-made solvents in drug delivery. Drug Discovery Today. 2020, 25(5): 901-908.
• Monti, D.; et al. Ionic liquids as potential enhancers for transdermal drug delivery. International Journal of Pharmaceutics. 2017, 516(1-2): 45-51.