Lidocaine(2-(diethylamino)-N-(2,6-dimethylphenyl) acetamide MW=270.8) is one of local anesthetics that has rapid and strong action properties. In this study, lidocaine gel formulation for enhanced drug delivery was designed. In solubility test and skin permeation test lidocaine was determined by HPL...
Lidocaine(2-(diethylamino)-N-(2,6-dimethylphenyl) acetamide MW=270.8) is one of local anesthetics that has rapid and strong action properties. In this study, lidocaine gel formulation for enhanced drug delivery was designed. In solubility test and skin permeation test lidocaine was determined by HPLC. The solubility of lidocaine in various vehicles was measured, and found to be higher in Transcutol(241.52±2.79mg/mL). To investigate the permeability of lidocaine, percutaneous absorption studies were performed using excised hairless mouse skin and the penetration of lidocaine via the skin was determined. In vitro permeation study was performed using buffered saline(PH 7.4 phosphate buffer : normal saline=1:1) as the receptor solution at 37℃. To increase the skin permeation of lidocine, the effects of various conditions such as the contents of liddocaine in gel (2, 5 and 6%), enhancers (Transcutol, Labrasol and propylene glycol), coenhancers (Labrafil, Labrafac and propylene glycol) and the contents of ethanol(30, 40 and 50%) were investigated. The skin permeation of lidocaine was increased when Transcutol and Labrafil were used as permeation enhancer and coenhancer, respectively, Skin permeation of lidocaine from gel was enhanced under the condition of 6% lidocaine contents, 50% of ethanol contents, Transcutol as enhancer and Labrafil as coenhancer. To evaluate the influence of ultrasound, various factors such as application modes(continuous mode and pulsed mode), frequency (1.0 and 3.0MHz) and intensity(1.0, 1,5 and 2.0 W/㎠) were investigated with 5% lidocaine hydro gel. The pronounced effect of ultrasound on the skin permeation of lidocaine was observed at all ultrasound energy levels. The highest permeation was observed at an intensity 2.0 W/㎠, frequency 1.0MHz and continuous output. The temperature of medium was not important factor to increase the penetration of lidocaine. The temperature of receptor phase did not show significant effect in skin permeation by phonophoresis. The effects of Transcutol and Labrafil as enhancer and coenhancer, respectively were equivalent also in both of with and without ultrasound on skin permeation rate. As the intensity of ultrasound increased, the permeation of lidocaine was accelerated. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1MHz and continuous treatment. The in vivo anesthetic effects were evaluated by two aspects as mechanical threshold and electrical threshold. Six healthy volunteers consented to the randomized, double-blind, and cross-over designed study in each group. In each subject, 3 groups were adapted such as A group(ultrasound with gel base only). B group(lidocaine gel) and C group(ultrasound with lidocaine gel). These 3 groups were treated in middle part of forearm being supine position and anesthetic effects were evaluated at 10, 15, 30, 45 and 60 minutes following each group application for 10 minutes. In mechanical threshold, B and C group showed increased anesthetic effects compared with A group but there was no significant difference. Variation of tactile detection threshold was showed same pattern. Following tactile detection threshold test B and C group was increased compared with A group. In 2 point discrimination test, the threshold of C group was increased significant difference compare to A and B group. Using blunt and sharp tip pressure pain threshold test B group and C group showed increased data compare to A group. In electrical detection threshold C and B group were increased compare to A group with difference significantly. Electrical pain threshold increase in significantly in case of C group compared to B and A group. In conclusion. lidocaine was potent anesthetic which could be block pain threshold effectively. And ultrasound could accelerate the skin penetration of lidocaine. The phonophoretic delivery system could be a good candidate for lidocaine as a local anaesthetic to improve significantly the skin permeation and in vivo anaesthetic effect.
Lidocaine(2-(diethylamino)-N-(2,6-dimethylphenyl) acetamide MW=270.8) is one of local anesthetics that has rapid and strong action properties. In this study, lidocaine gel formulation for enhanced drug delivery was designed. In solubility test and skin permeation test lidocaine was determined by HPLC. The solubility of lidocaine in various vehicles was measured, and found to be higher in Transcutol(241.52±2.79mg/mL). To investigate the permeability of lidocaine, percutaneous absorption studies were performed using excised hairless mouse skin and the penetration of lidocaine via the skin was determined. In vitro permeation study was performed using buffered saline(PH 7.4 phosphate buffer : normal saline=1:1) as the receptor solution at 37℃. To increase the skin permeation of lidocine, the effects of various conditions such as the contents of liddocaine in gel (2, 5 and 6%), enhancers (Transcutol, Labrasol and propylene glycol), coenhancers (Labrafil, Labrafac and propylene glycol) and the contents of ethanol(30, 40 and 50%) were investigated. The skin permeation of lidocaine was increased when Transcutol and Labrafil were used as permeation enhancer and coenhancer, respectively, Skin permeation of lidocaine from gel was enhanced under the condition of 6% lidocaine contents, 50% of ethanol contents, Transcutol as enhancer and Labrafil as coenhancer. To evaluate the influence of ultrasound, various factors such as application modes(continuous mode and pulsed mode), frequency (1.0 and 3.0MHz) and intensity(1.0, 1,5 and 2.0 W/㎠) were investigated with 5% lidocaine hydro gel. The pronounced effect of ultrasound on the skin permeation of lidocaine was observed at all ultrasound energy levels. The highest permeation was observed at an intensity 2.0 W/㎠, frequency 1.0MHz and continuous output. The temperature of medium was not important factor to increase the penetration of lidocaine. The temperature of receptor phase did not show significant effect in skin permeation by phonophoresis. The effects of Transcutol and Labrafil as enhancer and coenhancer, respectively were equivalent also in both of with and without ultrasound on skin permeation rate. As the intensity of ultrasound increased, the permeation of lidocaine was accelerated. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1MHz and continuous treatment. The in vivo anesthetic effects were evaluated by two aspects as mechanical threshold and electrical threshold. Six healthy volunteers consented to the randomized, double-blind, and cross-over designed study in each group. In each subject, 3 groups were adapted such as A group(ultrasound with gel base only). B group(lidocaine gel) and C group(ultrasound with lidocaine gel). These 3 groups were treated in middle part of forearm being supine position and anesthetic effects were evaluated at 10, 15, 30, 45 and 60 minutes following each group application for 10 minutes. In mechanical threshold, B and C group showed increased anesthetic effects compared with A group but there was no significant difference. Variation of tactile detection threshold was showed same pattern. Following tactile detection threshold test B and C group was increased compared with A group. In 2 point discrimination test, the threshold of C group was increased significant difference compare to A and B group. Using blunt and sharp tip pressure pain threshold test B group and C group showed increased data compare to A group. In electrical detection threshold C and B group were increased compare to A group with difference significantly. Electrical pain threshold increase in significantly in case of C group compared to B and A group. In conclusion. lidocaine was potent anesthetic which could be block pain threshold effectively. And ultrasound could accelerate the skin penetration of lidocaine. The phonophoretic delivery system could be a good candidate for lidocaine as a local anaesthetic to improve significantly the skin permeation and in vivo anaesthetic effect.
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