• Archives of Pharmacal Research
• /
• 제29권5호
• /
• pp.412-417
• /
• 2006

Triamcinolone acetonide (TA) is a corticosteroid that is used in the systemic and topical treatment of many inflammatory diseases. In this study, a phonophoretic drug delivery system was designed to enhance the TA permeability and the influence of ultrasound was examined. In order to establish the transdermal delivery system for TA, a hydrophilic carbopol gel containing TA was prepared after adopting phonophoresis. A permeation study through mouse skin was performed at $37^{\circ}C$ using a Franz diffusion cell, and the ultrasound treatment was carried out for 10 h. The level of TA permeation through the skin was evaluated under various ultrasound conditions including the frequency (1.0, 3.0 MHz), intensity (1.0, $2.5W/cm^2 $), and duty cycle (continuous, pulse mode) using a 0.5% TA gel. The highest permeation was observed under the ultrasound treatment conditions of low frequency, high intensity, and in continuous mode.

• Journal of Pharmaceutical Investigation
• /
• 제33권1호
• /
• pp.21-28
• /
• 2003

Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

• Journal of Pharmaceutical Investigation
• /
• 제36권4호
• /
• pp.253-262
• /
• 2006

This study was performed to investigate the effects of treatment for dermatitis using the herbal gel preparations. Scutellariae Radix(SR) and Zingiberis Rhizoma(ZR) were used for the purpose of herbal preparations. Baicalin, baicalein are the ingredients of SR, having biological effects like anti-inflammatory, anti-oxidative, anti-bacterial and antiallergic action. 6-Gingerol is one of the ingredients of ZR having biologicai effects like anti-inflammatory and analgesic action. The three types of hydrogels(SRE, SRH, SZH) were formulated with Carbopol 940, Labrasol, Triethanolamine etc. Baicalin was hydrolysed to baicalein by $\beta$-glucuronidase for the purpose to increase rate of skin permeation. Content of ingredients by HPLC determination, rate of skin permeation using Franz type diffusion cell, anti-oxidative activity for the free radical, hydroxyl radical, superoxide, anti-inflammatory by using carrageenan injection, efficacy on the dermatitis induced by 2,4-dinitro-chlorobenzene(DNCB) were experimented. Baicalein showed higher permeability than baicalin, so it is considered that baicalein was more suitable form than baicalin for transdermal absorption by its lipophilic property. In the anti-oxidative experiments, SZH gel was the most effective scavenging activity than the other gels in all experiments. In anti-inflammatory test, SRM and SZH gel more decreased edma rapidly than SRE gel. In case of using SZH gel, treatment period for the dermatitis was more declined than that of other gel groups. These results suggests that the SZH hydrogel could be suitable preparations for the treatment of dermatitis.

• Journal of Pharmaceutical Investigation
• /
• 제40권5호
• /
• pp.305-311
• /
• 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.