• Polymer(Korea)
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• v.36 no.6
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• pp.705-711
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• 2012

In this study, the elastic liposome consisted of egg phospholipids and edge activator ($Tego^{(R)}$ care 450) was prepared in order to supplement the defect of the conventional liposome. We prepared elastic liposome containing quercetin, known as natural antioxidant, and evaluated the vesicles size, elasticity, loading efficiency, stability, and in vitro skin permeation. The mean diameter of quercetin loaded elastic liposome formulations ranged between 208.2~303.4 nm and loading efficiency was observed 64.1~87.5%. The highest loading efficiency (87.5%) and deformability (28.3) were observed at the optimal ratio of 90 : 10 (egg phospholipids : $Tego^{(R)}$ care 450) among 0.1% quercetin loaded elastic liposome formulations. The elastic liposome formulation was selected for further transdermal permeation study. The elastic liposome ($129.9{\mu}g/cm^2$) exhibited more skin permeability than general liposome ($114.8{\mu}g/cm^2$) and 1,3-butylene glycol ($75.1{\mu}g/cm^2$) solution. This results suggest that the elastic liposome formulation using $Tego^{(R)}$ care 450 as a major edge activator could be useful for the delivery of active ingredient through the skin transdermal.

• Applied Chemistry for Engineering
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• v.26 no.2
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• pp.165-172
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• 2015

Quercetin and its glycoside, rutin, are flavonoids, which are well known as natural antioxidants. In this study, cationic liposomes loaded with flavonoids (quercetin or rutin) were investigated for their effects on cell and skin permeability, and protective effects against UVA. The particle size of the empty cationic liposomes was in the range of 100~130 nm, and the zeta potential was + 33.05 mV. The entrapment efficiency of 0.5R/CL was higher than that of 0.5 Q/CL. The cellular uptake of the cationic liposomes was five-fold higher than that of liposomes. The skin permeability of quercetin and rutin was investigated using Franz diffusion cells. Compared to the initial loading dose, the amount of quercetin or rutin delivered to the skin by cationic liposomes was higher than that delivered by conventional liposomes or phosphate-buffered saline. From the protective effect of cationic liposomes against UVA ($25J/cm^2$), we found that the cell viability in cationic liposomes containing flavonoids was higher than that of using UVA irradiation only. These results indicate that cationic liposomes provide enhanced delivery of flavonoids (quercetin and rutin) into the skin and may be used for antiaging and antioxidant cosmetics.

• Journal of Pharmaceutical Investigation
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• v.29 no.1
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• pp.29-36
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• 1999

Aceclofenac is an non-steroidal antiinflammatory drug which has been used in the treatment of rheumatoidal rthritis and osteo-arthritis. In order to decrease the gastric ulcerogenic effects and contol the plasma level of aceclofenac, we have developed the transdermal delivery system of aceclofenac plaster, which were formulated employing matrix polymers of acrylates and penetration-enhancers such as $Lauroglycol^{\circledR}$, $Transcutol^{\circledR}$, oleic acid and linoleic acid. Using Franz diffusion cells mounted with a rat skin, transdermal penetration characteristics of the formulations were evaluated by the HPLC assay of aceclofenac and diclofenac, an active metabolite, in the receptor compartment of pH 7.2 phosphate buffered solution. Skin penetration was increased when the content of aceclofenac increased, showing the flux $(J,\;{\mu}g/cm^2/hr)$ of 0.37 and 2.50 for 2% and 6.75% of the content, respectively. The flux$(J,\;{\mu}g/cm^2/hr)$ from plasters made of $Durotak^{\circledR}$ 87-2074, $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 were 2.50, 2.77 and 4.39, respectively. $Durotak^{\circledR}$ 87-2074 showed the lowest penetration due to the carboxylic acid group in the polymer, which might form a strong hydrogen bonding with a secondary amine of aceclofenac. Although both $Durotak^{\circledR}$ 87-2510 and $Durotak^{\circledR}$ 87-2097 are amine-resistant adhesives, $Durotak^{\circledR}$ 872510 showed lower penetration than $Durotak^{\circledR}$ 87-2097 because of the hydroxyl group in $Durotak^{\circledR}$ 87-2510, which might form a weak hydrogen bonding with aceclofenac. These results reveal that the functional group in acrylic polymers would greatly affect the release of aceclofenac from the matrix, which is the rate-limiting step in the penetration of aceclofenac through rat skins. The penetration of aceclofenac from plasters using different penetration-enhancers increased in the following order: Transcutol < linoleic acid < oleic acid. And the flux from the plasters containing oleic acid as a penetrationenhancer was 2.22 times greater than that of creams, which suggest that a newly deveolped aceclofenac plaster could be used in the treatment of rheumatoidal arthritis and osteo-arthritis as an advanced transdermal delivery system.

• Journal of Pharmaceutical Investigation
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• v.37 no.4
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• pp.237-242
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• 2007

The chemical formula of indapamide is 3-(aminosulfonyl)-4-chloro-N-(2,3-dihydro-2-methyl-1H-indol-l-yl)-benzamide, Indapamide is an oral antipertensive diuretic agent indicated for the treatment of hypertensive and edema. Indapamide inhibits carbonic anhydrase enzyme. Transdermal drug delivery systems, as compared to their corresponding classical oral or injectable dosage form counterparts, offer many advantages. The most important advantages are improved systemic bioavailability of the pharmaceutical active ingredients (PAI), because the first-pass metabolism by the liver and digestive system are avoided; and the controlled, constant drug delivery profile (that is, controlled zero-order absorption). Also of importance is the reduced dose frequency compared to the conventional oral dosage forms (that is, once-a-day, twice-a-week or once-a-week). Other benefits include longer duration of therapeutic action from a single application, and reversible action. For example, patches can be removed to reverse any adverse effects that may be caused by overdosing. In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of Indapamide, the skin permeation rates of Indapamide from vehicles of different composition were determined using Franz cells fitted with excised hairless skins. Solubility of Indapamide in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of Indapamide, The solvents used were Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol. Lauroglycol90 increase the permeability of indapamide approximately 3.75-fold compared with the control. Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol showed flux of $0.06ug/cm^2/hr,\;0.4ug/cm^2/hr,\;0.21ug/cm^2/hr,\;0.72ug/cm^2/hr,\;0.29ug/cm^2/hr$, respectively.

• Journal of Pharmaceutical Investigation
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• v.40 no.5
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• pp.305-311
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• 2010

The present study was aimed at preparing microemulsion-based hydrogel (MBH) for the skin delivery of itraconazole. Microemulsion prepared with Transcutol as a surfactant, benzyl alcohol as an oil and the mixture of ethanol and phasphatidyl choline (3:2) as a cosurfactant were characterized by solubility, phase diagram, particle size. MBHs were prepared using 0.7 % of xanthan gum (F1-1) or carbopol 940 (F1-2) as gelling agents and characterized by viscosity studies. The in vitro permeation data obtained by using the Franz diffusion cells and hairless mouse skin showed that the optimized microemulsion (F1) consisting of itraconazole (1% w/w), benzyl alcohol (10% w/w), Transcutol (10% w/w) and the mixture of ethanol and phospahtidylcholine (3:2) (10% w/w) and water (49% w/w) showed significant difference in the flux (${\sim}1{\mu}g/cm^2/h$) with their corresponding MBHs (0.25-0.64 ${\mu}g/cm^2/h$). However, the in vitro skin drug content showed no significant difference between F1 and F1-1, while F1-2 showed significantly low skin drug content. The effect of the amount of drug loading (0.02, 1 and 1.5% w/w) on the optimized MBH (F1-2) showed that the permeation and skin drug content increased with higher drug loading (1.5%). The in vivo study of the optimized MBH (F1-2 with1.5% w/w drug loading) showed that this formulation could be used as a potential topical formulation for itraconazole.

• YAKHAK HOEJI
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• v.60 no.1
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• pp.36-45
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• 2016

This study was aimed to enhance the percutaneous absorption of tizanidine hydrochloride (TZ) across Strat-M$^{TM}$ artificial membrane and excised hairless mouse skin using various vehicles and chemical permeation enhancers. Solubility studies were performed using hydrophilic and lipophilic vehicles. To initially evaluate vehicle effects on skin permeation, Strat-M$^{TM}$ membrane was adopted using Franz-type diffusion cells loaded with 0.4 mg donor dose. Effects of fatty acids on the permeation of TZ from PG and PGMC were compared, and the effects of various hydrophilic vehicles in the presence of linoleic acid were studied using excised hairless mouse skin specimens. The mean solubility (mg/ml) of TZ in hydrophilic vehicles was higher: water > PG > DMSO > ethanol > PEG 200 > NMP > PEG 300 > PEG 400 > DGME, and solubilities in lipophilic vehicles such as PGMC, PGMC, IPM, Captex 200 and Captex 300 were much less than 1.0 mg/ml. Permeation rates through StratTM membrane from pure vehicles were in the rank order: PGMC ${\geq}$ LBF > DMSO ${\geq}$ NMP ${\geq}$ PGML ${\geq}$ PG ${\geq}$ PEG 200 ${\geq}$ DGME ${\geq}$ EtOH. However, permeation rates of TZ through hairless mouse skin from pure vehicles were very low, although PG showed the highest flux ($1.66{\pm}0.28{\mu}g/cm^2{\cdot}hr$). Therefore, PG was selected in further studies. Addition of enhancers (3 v/v%) into PG markedly increased the flux (${\mu}g/cm^2{\cdot}hr$): oleyl alcohol ($14.9{\pm}3.1$) ${\geq}$ oleic acid ($14.5{\pm}1.6$) ${\geq}$ linoleic acid ($13.7{\pm}1.3$) > capric acid ($4.4{\pm}0.6$) > caprylic acid ($2.1{\pm}0.4$). Among hydrophilic vehicles with linoleic acid, PG and DMSO revealed relatively higher permeation for TZ. Increase of donor dose in PG resulted in dose-dependent permeation fluxes. These results suggest that permeation properties of TZ from nonaqueous solutions are markedly different between Strat-$M^{TM}$ membrane and excised hairless mouse skin, and transdermal delivery of TZ would be feasible with a combination of PG and enhancers.

• Journal of Pharmaceutical Investigation
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• v.29 no.3
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• pp.217-225
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• 1999

These studies were designed to determine the effect of hydroalcoholic gel system (lower alkanol concentration: 40-60%) compared to general hydrogel system (lower alkanol concentration: 10-35%) on transdermal delivery of piroxicam and its anti-inflammatory activity. Piroxicam was incorporated into a hydroalcoholic gel and a hydrogel containing polymers, solvents, and cosolvents. The pH of gel was about 6.3-7.3 and the solvent mixtures were composed of water and various concentrations of ethanol (35, 40, 50, and 60%). For the in vitro study, the skin permeation of piroxicam from the gel formulations was investigated using Franz modified diffusion cells fitted with hairless mouse skin. For the in vivo study, the anti-inflammatory activity of hydroalcoholic gel was compared to other commercial products (piroxicam hydrogel and ketoprofen hydrogel) in rat and human. The anti-inflammatory activity was determined using carrageenan induced foot edema model in rat. For the clinical study, it was evaluated from determining efficacy and acceptability with 98 patients suffering from musculoskeletal pain. A novel piroxicam hydroalcoholic gel was successfully formulated in the range of 40-50% of ethanol as solvent, more than 10% of propylene glycol, 5% of $Transcutol^{\circledR}$ and 1 % of benzyl alcohol. The skin permeation of piroxicam using hydroalcoholic gel system was greater than that of general hydrogel system $(flux\;:\;139.1-148.2\;{\mu}g/cm^2/hr\;vs.43.0-84.5 {\mu}g/cm^2/hr)$ in vitro. In carrageenan-induced edema model, the anti-inflammatory activity of hydroalcoholic gel was better than that of piroxicam hydrogel for edema inhibition (75.1 % vs. 62.9%, p

• Journal of Korean Society of Occupational and Environmental Hygiene
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• v.31 no.2
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• pp.173-183
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• 2021

Objectives: This study evaluated the skin permeability of lawsone in henna hair dyes to understand the exposure characteristics of henna hair dyes in the human body. It examined the protective effects of protectants by applying protectants A, B, and C to test skin. Methods: Skin absorption tests were conducted using Franz diffusion cells according to OECD test guideline 428. After applying one kind of natural henna hair dye and chemical henna hair dye, respectively, to a standardized pig skin model, samples of receptor fluid were collected at 1h, 3h, 6h, and 24h. The skin permeation of lawsone was determined using HPLC. After the skin absorption experiment, the skin to which hair dye was applied was analyzed to determine the residual amount of lawsone in the skin. Results: The cumulative permeation of both natural and chemical henna hair dyes increased over time, and the natural henna hair dye had a flux value (t=3.194, p<.05) high both in the K_p value (t=3.207, p<.05) and the residual amount (t=22.701, p<.001). For skin treated with a protectant, the cumulative permeation of natural henna hair dye 24h control and the cumulative permeation of protectant A, B, and C increased over time. Flux and K_p values were in the order control > protectant A > protectant C > protectant B. The residual amount (F=4.469, p<.05) was in the order of protectant C > protectant A > protectant B > control. At 3h, the dye application time of natural henna hair dye, the lawsone flux value (F=4.454, p<.05) and K_p value (F=4.455, p<.05) were higher in the control group than in the protectant groups. The 24h cumulative permeation of the chemical henna hair dye increased with time in both the control and the protectant groups, and the flux and K_p values were in the order of protectant A > protectant C > protectant B > control. The residual amount (F=7.901, p<.01) was in the order of protectant B > protectant A> protectant C > control. Conclusions: Within the normal dyeing time for henna hair dye (three hours for natural henna hair dyes and 30 minutes for chemical henna hair dyes) lawsone skin penetration was not observed even when no protective agent was applied. After that time, however, evidence of skin penetration and retention of lawsone and the protective effect of protective agents were observed.