Ionic liquids as ingredients in topical drug delivery systems

Dobler, Dorota; Schmidts, Thomas; Klingenhöfer, Ines; Runkel, Frank

doi:10.1016/j.ijpharm.2012.10.035

Cited by 160 publications

(105 citation statements)

References 48 publications

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“…Taken together, both ILs and DESs have gained acceptance for their beneficial antimicrobial and antifungal properties as demonstrated in several reports over the last decade (19)(20)(21)(22). More recently, both ILs and DESs were found to increase drug solubility and serve as a carrier for topical drug delivery (23)(24)(25)(26). Our comprehensive approach is unique in that we examine a panel of in-house synthesized ILs and DESs (henceforth referred to as ILs for simplicity) for all of the following applications: (i) antimicrobial properties on two biofilm forming Gram-negative pathogenic bacteria, Pseudomonas aeruginosa ATCC15692 and Salmonella enterica serovar Typhimurium LT2; (ii) cytotoxicity effects on mammalian cell lines; (iii) skin irritation potential; (iv) transdermal drug delivery properties; and (v) treatment of biofilm on a skin-wound model.…”

Section: Significancementioning

confidence: 99%

Ionic liquids as a class of materials for transdermal delivery and pathogen neutralization

Zakrewsky

Lovejoy

Kern

et al. 2014

Proc. Natl. Acad. Sci. U.S.A.

269

270

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Biofilm-protected microbial infections in skin are a serious health risk that remains to be adequately addressed. The lack of progress in developing effective treatment strategies is largely due to the transport barriers posed by the stratum corneum of the skin and the biofilm. In this work, we report on the use of Ionic Liquids (ILs) for biofilm disruption and enhanced antibiotic delivery across skin layers. We outline the syntheses of ILs, analysis of relevant physicochemical properties, and subsequent neutralization effects on two biofilm-forming pathogens: Pseudomonas aeruginosa and Salmonella enterica. Further, the ILs were also examined for cytotoxicity, skin irritation, delivery of antibiotics through the skin, and treatment of biofilms in a wound model. Of the materials examined, choline-geranate emerged as a multipurpose IL with excellent antimicrobial activity, minimal toxicity to epithelial cells as well as skin, and effective permeation enhancement for drug delivery. Specifically, choline-geranate was comparable with, or more effective than, bleach treatment against established biofilms of S. enterica and P. aeruginosa, respectively. In addition, cholinegeranate increased delivery of cefadroxil, an antibiotic, by >16-fold into the deep tissue layers of the skin without inducing skin irritation. The in vivo efficacy of choline-geranate was validated using a biofilm-infected wound model (>95% bacterial death after 2-h treatment). This work establishes the use of ILs for simultaneous enhancement of topical drug delivery and antibiotic activity.antibacterial | antimicrobial agents | antibiotic resistance | ion-pairing | formulation

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Section: Significancementioning

confidence: 99%

Ionic liquids as a class of materials for transdermal delivery and pathogen neutralization

Zakrewsky

Lovejoy

Kern

et al. 2014

Proc. Natl. Acad. Sci. U.S.A.

269

270

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“…Neste âmbito, os líquidos iónicos (LI) têm sido estudados como promotores de solubilidade e permeação e têm sido desenvolvidos alguns estudos que utilizam estes materiais com esta finalidade [3,7,8]. Os LI são sais orgânicos [9,10], constituídos por iões, um catião orgânico e um anião orgânico ou inorgânico [9,11], que podem ser líquidos a temperaturas inferiores a 100 ºC [12,13] ou, em alguns casos, líquidos à temperatura ambiente [3,11]. Estes compostos têm diversas propriedades valiosas, sendo a suscetibilidade a modificações a mais relevante.…”

Section: Materials and Reagentsunclassified

“…Estes compostos têm diversas propriedades valiosas, sendo a suscetibilidade a modificações a mais relevante. Assim, é possível alterar deliberadamente os iões que os constituem e sintetizar LI com propriedades físicas e químicas específicas [3,9]. Atualmente, são diversos os estudos, que envolvem a incorporação de LI em formulações tópicas, demonstrando que existe um impacto destes sais na solubilidade e permeação de compostos ativos pouco solú-veis [3,7,8,14,15].…”

Section: Materials and Reagentsunclassified

“…In this context, ionic liquids (ILs) have been studied as promoters of solubility and permeation and some studies have shown the use of these materials for this purpose [3,7,8,14,15]. Ionic liquids are organic salts [7,8], constituted by ions, an organic cation and an organic or inorganic anion [7,9], which are liquid at temperatures below 100 ºC [10,11] or, in some cases, liquids at room temperature [3,9]. These compounds have several valuable properties, the ease of modification being the most relevant.…”

Section: Introductionmentioning

confidence: 99%

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Permeation of Ionic Liquids through the skin

Júlio¹,

Caparica²,

Mota³

et al. 2017

BBR

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233 Biomedical and Biopharmaceutical Research J o r n a l d e I n v e s t i g a ç ã o B i o m é d i c a e B i o f a r m a c ê u t i c a Permeation of Ionic Liquids through the skin Permeação de Líquidos Iónicos através da pele AbstractAlternative forms of drug delivery such as delivery through the skin, have been developed to explore other routes. However, the incorporation of poorly soluble or partially insoluble drugs into these delivery systems represents a major problem. Ionic liquids (ILs) may be incorporated in aqueous, oily or hydroalcoholic solutions and thus, may be used as excipients in drug delivery systems to increase/improve the topical and transdermal drug delivery. However, it is fundamental to consider the cytotoxicity of these salts and it is also crucial to evaluate if these compounds permeate through the skin.

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“…Multiple emulsions containing ILs as a hydrophobic phase have also been reported (18). While hydrophilic ILs can be used to proportionally replace the water phase, hydrophobic ILs prefer to form an independent phase within the emulsion (19).…”

Section: Introductionmentioning

confidence: 99%

Hydrophilic Ionic Liquids as Ingredients of Gel-Based Dermal Formulations

et al. 2015

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Abstract. Ionic liquids (ILs) have several properties that offer many advantages in dermal drug delivery systems. Depending on the chemical structure, ILs can be used for protection against microorganisms, to enhance skin penetration, and as a solvent. In the present work, SEPINEO™ P 600 formulations and hydroxyethylcellulose gels containing the hydrophilic ILs hexylpyridinium chloride, choline dihydrogen phosphate, and 1-ethyl-3-methylimidazolium ethyl sulfate were prepared, and the influence of the ILs on the formulation properties was evaluated. ILs were successfully incorporated into the emulsion structure, resulting in stable formulations. The antimicrobial activity of the ILs was estimated. The minimal inhibitory concentration values for hexylpyridinium chloride are about 2.5 mg/mL. The other two ILs have no antimicrobial activity. Skin penetration enhancement of caffeine, a hydrophilic model substance, was observed in the presence of hexylpyridinium chloride.

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Ionic liquids as ingredients in topical drug delivery systems

Cited by 160 publications

References 48 publications

Ionic liquids as a class of materials for transdermal delivery and pathogen neutralization

Ionic liquids as a class of materials for transdermal delivery and pathogen neutralization

Permeation of Ionic Liquids through the skin

Hydrophilic Ionic Liquids as Ingredients of Gel-Based Dermal Formulations

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