Ionic conjugates of lidocaine and sweeteners as better tasting local anesthetics for dentistry

Iryna O. Lebedyeva; Alexander A. Oliferenko; Polina V. Oliferenko; Robert A. Hromas; John K. Neubert; Robert M. Caudle; Jay Wickersham; William L. Castleman; Gary I. Altschuler; David A. Ostrov; C. Dennis Hall; Alan R. Katritzky

doi:10.1039/c5tb00674k

Ionic conjugates of lidocaine and sweeteners as better tasting local anesthetics for dentistry

Iryna O. Lebedyeva, Alexander A. Oliferenko, Polina V. Oliferenko, Robert A. Hromas, John K. Neubert, Robert M. Caudle, Jay Wickersham, William L. Castleman, Gary I. Altschuler, David A. Ostrov, C. Dennis Hall, Alan R. Katritzky

Chemistry and Physics

Research output: Contribution to journal › Article › peer-review

5 Scopus citations

Abstract

Lidocaine is the most widely utilized intraoral injected dental anesthetic, used for more than 500 million dental injections per year. Local anesthesia is essential for pain-free dentistry, yet intraoral injections are often considered painful and a source of anxiety for many patients. Any new anesthetics that will reduce the stress and anxiety of dental injection are expected to be beneficial. A novel chemical approach to taste modulation is proposed, in which the lidocaine cation is coupled with anionic sweeteners such as saccarinate and acesulfamate. The ionic conjugates synthesized using anion exchange techniques, were much less bitter, demonstrated a high local anesthetic potential in animal studies, and were as safe as the original hydrochloride. Based on the currently robust market for lidocaine it is expected that the resulting anesthetics will be in high demand in clinical practices worldwide.

Original language	English (US)
Pages (from-to)	8492-8498
Number of pages	7
Journal	Journal of Materials Chemistry B
Volume	3
Issue number	43
DOIs	https://doi.org/10.1039/c5tb00674k
State	Published - Sep 23 2015

ASJC Scopus subject areas

Chemistry(all)
Biomedical Engineering
Materials Science(all)

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Lebedyeva, I. O., Oliferenko, A. A., Oliferenko, P. V., Hromas, R. A., Neubert, J. K., Caudle, R. M., Wickersham, J., Castleman, W. L., Altschuler, G. I., Ostrov, D. A., Hall, C. D., & Katritzky, A. R. (2015). Ionic conjugates of lidocaine and sweeteners as better tasting local anesthetics for dentistry. Journal of Materials Chemistry B, 3(43), 8492-8498. https://doi.org/10.1039/c5tb00674k

Lebedyeva, IO, Oliferenko, AA, Oliferenko, PV, Hromas, RA, Neubert, JK, Caudle, RM, Wickersham, J, Castleman, WL, Altschuler, GI, Ostrov, DA, Hall, CD & Katritzky, AR 2015, 'Ionic conjugates of lidocaine and sweeteners as better tasting local anesthetics for dentistry', Journal of Materials Chemistry B, vol. 3, no. 43, pp. 8492-8498. https://doi.org/10.1039/c5tb00674k

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abstract = "Lidocaine is the most widely utilized intraoral injected dental anesthetic, used for more than 500 million dental injections per year. Local anesthesia is essential for pain-free dentistry, yet intraoral injections are often considered painful and a source of anxiety for many patients. Any new anesthetics that will reduce the stress and anxiety of dental injection are expected to be beneficial. A novel chemical approach to taste modulation is proposed, in which the lidocaine cation is coupled with anionic sweeteners such as saccarinate and acesulfamate. The ionic conjugates synthesized using anion exchange techniques, were much less bitter, demonstrated a high local anesthetic potential in animal studies, and were as safe as the original hydrochloride. Based on the currently robust market for lidocaine it is expected that the resulting anesthetics will be in high demand in clinical practices worldwide.",

author = "Lebedyeva, {Iryna O.} and Oliferenko, {Alexander A.} and Oliferenko, {Polina V.} and Hromas, {Robert A.} and Neubert, {John K.} and Caudle, {Robert M.} and Jay Wickersham and Castleman, {William L.} and Altschuler, {Gary I.} and Ostrov, {David A.} and Hall, {C. Dennis} and Katritzky, {Alan R.}",

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AU - Lebedyeva, Iryna O.

AU - Oliferenko, Alexander A.

AU - Oliferenko, Polina V.

AU - Hromas, Robert A.

AU - Neubert, John K.

AU - Caudle, Robert M.

AU - Wickersham, Jay

AU - Castleman, William L.

AU - Altschuler, Gary I.

AU - Ostrov, David A.

AU - Hall, C. Dennis

AU - Katritzky, Alan R.

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AB - Lidocaine is the most widely utilized intraoral injected dental anesthetic, used for more than 500 million dental injections per year. Local anesthesia is essential for pain-free dentistry, yet intraoral injections are often considered painful and a source of anxiety for many patients. Any new anesthetics that will reduce the stress and anxiety of dental injection are expected to be beneficial. A novel chemical approach to taste modulation is proposed, in which the lidocaine cation is coupled with anionic sweeteners such as saccarinate and acesulfamate. The ionic conjugates synthesized using anion exchange techniques, were much less bitter, demonstrated a high local anesthetic potential in animal studies, and were as safe as the original hydrochloride. Based on the currently robust market for lidocaine it is expected that the resulting anesthetics will be in high demand in clinical practices worldwide.

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Ionic conjugates of lidocaine and sweeteners as better tasting local anesthetics for dentistry

Abstract

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