Evaluation of Penetration Enhancement of Lidocaine by Nonionic Surfactants Through Hairless Mouse Skin In Vitro

Sarpotdar, Pramod P.; Zatz, Joel L.

doi:10.1002/jps.2600750216

Cited by 82 publications

(36 citation statements)

References 7 publications

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“…The enhancer effect is only observed when the micellar structure is broken, or if some bonding process with the surfactant is interrupted. This transition depends on the concentration of the surfactant (Sarpotdar and Zatz, 1986). The catalyzing activity of ionic surfactant depend fundamentally on the destruction of membranes of which they originate, being that they have an affinity for α-proteins (keratine), and when they form complexes, provoke reversible desnaturation and filament distension.…”

Section: Surfactantsmentioning

confidence: 99%

Percutaneous absorption enhancers: mechanisms and potential

Rodrigues

Zanluchi²,

Grebogi

2007

Braz. arch. biol. technol.

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Transdermal applications of drugs present many advantages in terms of absorption, however this is not easily obtained through the transdermal route. The principle barrier is the stratum corneum and one of the strategies that have been found to promote cutaneous drug penetration is through the use of absorption enhancers. Many substances have been identified as absorption enhancers. Although the list of substances that promote absorption is growing, in most cases, there is a direct correlation between the effects of absorption enhancers and their skintoxicity. The use of these substances depends therefore on studies which focus on local and systemic toxicity, as well as action mechanisms.

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Section: Surfactantsmentioning

confidence: 99%

Percutaneous absorption enhancers: mechanisms and potential

Rodrigues

Zanluchi²,

Grebogi

2007

Braz. arch. biol. technol.

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“…It is also employed as a topical local anaesthetic in various small surgical procedures like venipuncture, suturing of wounds, etc [16]. The topical application of lidocaine recommends some potential benefits such as rapid onset of action, minimum systemic toxicity, etc [17]. These benefits favour the topical delivery of lidocaine for local action.…”

Section: Introductionmentioning

confidence: 99%

Use of Cashew Bark Exudate Gum in the Preparation of 4 % Lidocaine HCL Topical Gels

Hasnain

Rishishwar

Ali

2017

Int J Pharm Pharm Sci

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Objective: The objective of the current work was to prepare and evaluate ex vivo skin permeation of cashew bark exudate gum based 4 % lidocaine HCl topical gels.Methods: In the current work, 4 % lidocaine HCl topical gels were prepared by using different concentrations of cashew bark exudate gum, HPMC K4M, lidocaine HCl, methyl paraben (as preservative) and glycerin (as plasticizer). The formulated topical gels were evaluated for pH, viscosity, and ex vivo skin permeation through excised porcine ear skin membrane. Results:The pHs of these formulated 4 % lidocaine HCl topical gels were found within the range of 6.04±0.02 to 6.52±0.04; whereas, the viscosities were measured within the range, 4.38±0.02 x 10 6 to 4.74±0.04 x 10 6 cps. Sustained ex vivo permeation of lidocaine was measured over 7 h. Highest ex vivo permeation flux was measured when 0.1 % menthol was incorporated as a permeation enhancer. It was also higher than that of the marketed 4 % lidocaine HCl topical gel. The stability study by freeze thaw cycle method revealed physically stable gels without the occurrence of syneresis. Conclusion:The results clearly indicate a promising potential of the use of cashew bark exudate gum as a gelling material with HPMC K4M to prepare 4 % lidocaine HCl topical gels of good skin permeation capability.

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“…Sarpotdar and Zatz [8] report an in vitro study of the penetration enhancement of LC through hairless mouse skin in the presence of propylene glycol. They observed that the concentration of propylene glycol strongly affects the steady state flux [8].…”

Section: Introductionmentioning

confidence: 99%

“…They observed that the concentration of propylene glycol strongly affects the steady state flux [8].…”

Section: Introductionmentioning

confidence: 99%

Development of bioadhesive chitosan gels for topical delivery of lidocaine

2006

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Lidocaine (LC) is a local anesthetic agent. The aim of this study is prolonging the anesthetic effect of this drug for transdermal delivery. Gels of LC hydrochloride were prepared with three different molecular weights (MW) and concentrations of chitosan. lecithin was used as permeation enhancer. Viscosity, bioadhesion, drug release from synthetic membranes, drug permeation through the biological barrier (rat skin) and antinocicetive effect of gels were studied. Increasing the concentration of chitosan caused to decrease the bioadhesion. Drug release studies in gels showed that increasing the concentration and MW of chitosan caused an increase in both the rate and extent and also in flux of drug probably because of the increase in repulsive forces between LC and chitosan cations. The flux of drug through the rat skin was higher for 3% high MW chitosan gel (H3) compared to the standard gel. LC was effective topically in hind paw formalin assay. It was most active immediately after its administration. The analgesic activity of LC in H3 gel could cover the duration of the formalin nociception. The maximal response of LC in comparable doses of H3 and standard gel was about 52% and 36% analgesia in the second phase, respectively compared to the control group.The higher response of the H3 gel may be attributed to the bioadhesive effect of chitosan base and the higher concentrations of LC compared to the standard gel.

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Evaluation of Penetration Enhancement of Lidocaine by Nonionic Surfactants Through Hairless Mouse Skin In Vitro

Cited by 82 publications

References 7 publications

Percutaneous absorption enhancers: mechanisms and potential

Percutaneous absorption enhancers: mechanisms and potential

Use of Cashew Bark Exudate Gum in the Preparation of 4 % Lidocaine HCL Topical Gels

Development of bioadhesive chitosan gels for topical delivery of lidocaine

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