The Possibility of Lidocaine Ion Pair Absorption Through Excised Hairless Mouse Skin

Nash, Robert A.; Mehta, Deepak B.; Matias, Jonathan R.; Orentreich, Norman

doi:10.1159/000211033

Cited by 19 publications

(9 citation statements)

References 16 publications

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“…These ion-pairs seem to be weakly associated as reported for lidocaine-alkanoate ion-pair. 9) They are still polar compared with non-ionic forms of the original drugs. Therefore, a relatively high partition coefficient between non-aqueous vehicle and skin can be expected.…”

Section: Discussionmentioning

confidence: 99%

“…However, the ion-pair probably dissociates as soon as it reaches the high dielectric region of the skin as suggested by the present study on salicylate-lidocaine ion-pair and by a previous study on lidocaine-alkanoate ion-pair. 9) Ion-pair formation could be a useful tool for ionic drugs to facilitate transdermal absorption. Combined use of ion-pairs with chemical enhancers as revealed in this study and other enhancement systems such as microemulsions 21) will develop into future clinical transdermal therapeutic systems for ionic drugs.…”

Section: Discussionmentioning

confidence: 99%

“…For salicylate, enhancement of skin permeation by ion-pair formation with alkylamines and quaternary ammonium ions in ethanol-pyopylene glycol (2 : 1 v/v) 6,7) and in aqueous medium 8) has been reported. Ion-pair absorption of lidocaine-n-alkanoate from ethanolic medium 9) and ion-pair complex of cromolyn from isopropyl myristate (IPM) has also been reported. 10) In this study we examined the solubility increase of salicylate in non-aqueous vehicle by ion-pair formation with either alkylamines or benzylamine.…”

mentioning

confidence: 97%

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Enhanced Skin Permeation of Salicylate by Ion-Pair Formation in Non-aqueous Vehicle and Further Enhancement by Ethanol and l-Menthol

et al. 2006

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 97%

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Enhanced Skin Permeation of Salicylate by Ion-Pair Formation in Non-aqueous Vehicle and Further Enhancement by Ethanol and l-Menthol

et al. 2006

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“…As shown in the Table 4, each formulation may utilize different types of counterion approaches to improve permeability. There are several other examples where counterion approach has increased transdermal permeability [70,71]. There are also reports in literature where the ion-pairing approach have been explored for ocular formulations [72].…”

Section: Ion-pairingmentioning

confidence: 99%

Current and evolving approaches for improving the oral permeability of BCS Class III or analogous molecules

Dave

Gupta

et al. 2016

Drug Development and Industrial Pharmacy

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The Biopharmaceutics Classification System (BCS) classifies pharmaceutical compounds based on their aqueous solubility and intestinal permeability. The BCS Class III compounds are hydrophilic molecules (high aqueous solubility) with low permeability across the biological membranes. While these compounds are pharmacologically effective, poor absorption due to low permeability becomes the rate-limiting step in achieving adequate bioavailability. Several approaches have been explored and utilized for improving the permeability profiles of these compounds. The approaches include traditional methods such as prodrugs, permeation enhancers, ion-pairing, etc., as well as relatively modern approaches such as nanoencapsulation and nanosizing. The most recent approaches include a combination/hybridization of one or more traditional approaches to improve drug permeability. While some of these approaches have been extremely successful, i.e. drug products utilizing the approach have progressed through the USFDA approval for marketing; others require further investigation to be applicable. This article discusses the commonly studied approaches for improving the permeability of BCS Class III compounds. AbstractThe Biopharmaceutics Classification System (BCS) classifies pharmaceutical compounds based on their aqueous solubility and intestinal permeability. The BCS Class III compounds are hydrophilic molecules (high aqueous solubility) with low permeability across the biological membranes. While these compounds are pharmacologically effective, poor absorption due to low permeability becomes the rate-limiting step in achieving adequate bioavailability.Several approaches have been explored and utilized for improving the permeability profiles of these compounds. The approaches include traditional methods such as prodrugs, permeation enhancers, ion-pairing, etc., as well as relatively modern approaches such as nanoencapsulation and nanosizing. The most recent approaches include a combination/ hybridization of one or more traditional approaches to improve drug permeability. While some of these approaches have been extremely successful, i.e. drug products utilizing the approach have progressed through the USFDA approval for marketing; others require further investigation to be applicable. This article discusses the commonly studied approaches for improving the permeability of BCS Class III compounds.

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“…Mathematical models have been developed to predict salicylate flux from these physicochemical parameters . Nash et al (1992) tested the ion pair absorption hypothesis with respect to the topical route of drug delivery. The experiment consisted of preparing various lidocaine-n-alkanoate ion pairs, then characterizing them by proton magnetic resonance spectroscopy, elemental analysis and conductivity.…”

Section: Transdermal Deliverymentioning

confidence: 99%

Ion-paired Drug Delivery: An Avenue for Bioavailability Improvement

Suresh¹,

Paul²

2011

Sierra Leone j. biomed. res.

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Ion-pairing is reported to improve the lipophilicity and subsequently the transport rate of polar drugs across lipid membranes. Lipophilisation of ionic drugs with high aqueous solubilities by ion-pair formation with appropriate counter-ion have proven to be promising for several applications. The aim of this review is to present the usefulness of ion-pair for improving the poor bioavailability of ionic drugs through various routes. The review covers an update on the applications of this strategy to improve drug delivery through various routes of administration including ocular, oral, parenteral and transdermal. It is discussed how ion-pair complexes assist in introducing functionality that would allow formation of a neutral molecule which can be subsequently encapsulated into delivery systems to be distributed by various routes of administration.

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The Possibility of Lidocaine Ion Pair Absorption Through Excised Hairless Mouse Skin

Cited by 19 publications

References 16 publications

Enhanced Skin Permeation of Salicylate by Ion-Pair Formation in Non-aqueous Vehicle and Further Enhancement by Ethanol and l-Menthol

Enhanced Skin Permeation of Salicylate by Ion-Pair Formation in Non-aqueous Vehicle and Further Enhancement by Ethanol and l-Menthol

Current and evolving approaches for improving the oral permeability of BCS Class III or analogous molecules

Ion-paired Drug Delivery: An Avenue for Bioavailability Improvement

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