The dermal delivery of lignocaine: influence of ion pairing

Valenta, Claudia; Siman, U.; Kratzel, Martin; Hadgraft, Jonathan

doi:10.1016/s0378-5173(99)00453-6

Cited by 76 publications

(45 citation statements)

References 15 publications

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“…The steady state lignocaine flux was increased up to 2.45-fold using different counter ions. The highest flux was measured from lignocaine morpholinopropane sulfonate (L-mps) (Valenta et al, 2000). Riserdronate is an inhibitor of osteoclastic activity used for treating various disorders of bones.…”

Section: Ion-pairmentioning

confidence: 99%

Permeation enhancer strategies in transdermal drug delivery

et al. 2014

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Today, $74% of drugs are taken orally and are not found to be as effective as desired. To improve such characteristics, transdermal drug delivery was brought to existence. This delivery system is capable of transporting the drug or macromolecules painlessly through skin into the blood circulation at fixed rate. Topical administration of therapeutic agents offers many advantages over conventional oral and invasive techniques of drug delivery. Several important advantages of transdermal drug delivery are prevention from hepatic first pass metabolism, enhancement of therapeutic efficiency and maintenance of steady plasma level of the drug. Human skin surface, as a site of drug application for both local and systemic effects, is the most eligible candidate available. New controlled transdermal drug delivery systems (TDDS) technologies (electrically-based, structure-based and velocity-based) have been developed and commercialized for the transdermal delivery of troublesome drugs. This review article covers most of the new active transport technologies involved in enhancing the transdermal permeation via effective drug delivery system.

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Section: Ion-pairmentioning

confidence: 99%

Permeation enhancer strategies in transdermal drug delivery

et al. 2014

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“…Ions permeate the skin at a much lower rate relative to neutral compounds. Techniques such as ion pairing, 5 chemical enhancers, 6 and electric current 7 were successfully used to enhance ionic drug permeation. Iontophoresis involves the use of low-density electric current (approximately 0.5 mA/cm 2 ) to drive charged molecules across the skin.…”

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confidence: 99%

Iontophoretic transdermal delivery of buspirone hydrochloride in hairless mouse skin

Al-Khalili

Meidan²,

Michniak³

2003

AAPS PharmSci

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INTRODUCTIONBuspirone hydrochloride (BH) is an orally administered anxiolytic that is structurally and pharmacologically distinct from all other anxiolytics, including benzodiazepines and barbiturates. It differs from other anxiolytics in that it does not possess anticonvulsant or muscle relaxant properties, does not impair psychomotor function, and does not cause sedation or physical dependence. BH is used to treat generalized anxiety disorder and anxiety caused by alcohol craving or smoking cessation, as well as attention deficit hyperactivity disorder in children.Since 1984, BH has been used in children and adolescents with anxiety disorders, and researchers have reported significant improvement with its use.1 The reported side effects were very mild, and many clinical trials have shown the superiority of BH over other traditional stimulant-based treatments. 2,3The transdermal delivery of buspirone hydrochloride across hairless mouse skin and the combined effect of iontophoresis and terpene enhancers were evaluated in vitro using Franz diffusion cells. Iontophoretic delivery was optimized by evaluating the effect of drug concentration, current density, and pH of the vehicle solution. Increasing the current density from 0.05 to 0.1 mA/cm 2 resulted in doubling of the iontophoretic flux of buspirone hydrochloride, while increasing drug concentration from 1% to 2% had no effect on flux. Using phosphate buffer to adjust the pH of the drug solution decreased the buspirone hydrochloride iontophoretic flux relative to water solutions. Incorporating buspirone hydrochloride into ethanol:water (50:50 vol/vol) based gel formulations using carboxymethylcellulose and hydroxypropylmethylcellulose had no effect on iontophoretic delivery. Incorporation of three terpene enhancers (menthol, cineole, and terpineol) into the gel resulted in a synergistic effect when combined with iontophoresis. Menthol was the most active enhancer, and when combined with iontophoresis it was possible to deliver 10 mg/cm 2 /day of buspirone hydrochloride.Although BH is rapidly absorbed in humans, it undergoes extensive first-pass metabolism such that the unchanged compound accounts for only 1% of the radioactivity in the plasma after oral administration of a 20-mg single dose of BH. Moreover, the average elimination half-life of unchanged BH after single doses of 10 to 40 mg is about 2 to 3 hours. 4 Consequently, treatment with BH typically requires 3 daily doses of between 5 and 20 mg each. Because of the chronic nature of the treatment, a reduction in the number of daily doses would be advantageous, as it should radically improve patient compliance. Thus, an effective transdermal buspirone delivery system would be expected to have a great impact on therapy success.

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“…On the one hand, this increase in the solubility may cause increase in the concentration of the dissolved form in the semisolid base and thus increase in the skin permeation [37] . On the other hand, this increase in the solubility is due to the increase in the degree of ionization, ionized species are considered to have lower intrinsic permeability than parent molecules [1,40,41] .…”

Section: Hydrophilic Basesmentioning

confidence: 99%

Dermal and Transdermal Delivery of Active Substances from Semisolid Bases

Jankowski¹,

Dyja²,

Sarecka-Hujar³

2017

pharmaceutical-sciences

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Jankowski, et al.: Dermal and Transdermal Delivery from SemisolidsThe selection of a semisolid base type (hydrophobic, hydrophilic or emulsion) has an essential influence on the skin and transdermal delivery of active substances. The cutaneous and percutaneous absorption may be influenced by interactions occurring between base components and skin on the one hand and interactions between base components and the active ingredient on the other hand. The present article discusses the utility of different types of semisolid bases as carriers of active substances and summarizes results of studies comparing delivery of active substances from different semisolid bases.

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The dermal delivery of lignocaine: influence of ion pairing

Cited by 76 publications

References 15 publications

Permeation enhancer strategies in transdermal drug delivery

Permeation enhancer strategies in transdermal drug delivery

Iontophoretic transdermal delivery of buspirone hydrochloride in hairless mouse skin

Dermal and Transdermal Delivery of Active Substances from Semisolid Bases

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