• Korean Journal of Clinical Pharmacy
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• v.13 no.2
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• pp.97-105
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• 2003

아스코마이신(ascomycin)의 macrolactam 유도체인 피메크로리무스(pimecrolimus; 엘리델 [Elidel], SDZ ASM 981; Novartis Pharma AG, 바젤, 스위스)는 세포선택성을 지닌 염증성 사이토카인(cytokines) 억제제로서 아토피피부염, 알레르기성 접촉피부염, 자극성 접촉피부염 및 판형 건선 등 염증성 피부질환의 치료제로 개발되었다. T세포와 비만세포의 염증성 사이토카인 생산 분비를 억제하고 사전 형성된 염증성 매개물질의 비만 세포 분비를 저해한다. 국소 투여된 피메크로리무스는 알레르기성 접촉피부염(allergic contact dermatitis [ACD]) 돼지 모델에서 고역가 코르티코스테로이드 클로베타졸-17-propionate(corticosteroid clobetasol-17-propionate)와 동등한 효과를 나타낸다. 하지만 피메크로리무스는 클로베타졸과는 달리 피부 위축을 일으키지 않는다. 경구 투여시 피메크로리무스는 마우스와 랫트 ACD 치료에 있어서 타크로림무스(tacrolimus [FK 506])와 동등한 혹은 더 우수한 효과를 나타낸다. 또한 피메크로리무스는 아토피피부염 급성 징후 유사 모델인 저마그네슘 혈증 탈모 랫트(hypomagnesemic hairless rat)의 피부 염증과 소양증을 효과적으로 감소시킨다. 피메크로리무스는 랫트에서 다음과 같은 측면의 전신 면역반응 손상 효과가 타크로리무스 와 비교하여 낮게 평가된다: (1)국소 이식편대 숙주 반응, (2)양(sheep) 적혈구에 대한 항체 형성, (3)신장이식. 시험관내 평가시 돼지 피부를 통한 피메크로리무스 투과 속도가 타크로리무스보다 10배 낮게 측정되므로 생체에서 경피 흡수가 더 적게 될 것으로 판단된다. 상기 자료로 판단컨대 피메크로 리무스는 피부에 대한 항염증 활성이 높을 뿐 아니라 전신 면역반응 손상 부작용이 낮은것으로 사료된다.

• Proceedings of the Korean Society of Near Infrared Spectroscopy Conference
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• 2001.06a
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• pp.3115-3115
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• 2001

In this study, portable near infrared (NIR) system was newly integrated with a photodiode array detector, which has no moving parts and this system has been successfully applied for evaluation of human skin moisture. The good correlation between NIR absorbance and absolute water content of separated hairless mouse skin was, in vitro, showed depending on the water content (7.42-84.94%) using this portable NIR system. Partial least squares (PLS) regression was used for the calibration with the 1100-1650 nm wavelength range. For the practical use for the evaluation of human skin based on moisture, PLS model for human skin moisture was, in vivo, developed using the portable NIR system based on the relative water content values of stratum corneum from the conventional capacitance method. The PLS model showed a good correlation. This study indicated that the portable NIR system could be a powerful tool for human skin moisture, which may be much more stable to environmental conditions such as temperature and humidity, compared to conventional methods. Furthermore, in order to confirm the performance of newly integrated portable NIR system, scanning type conventional NIR spectrometer was used in the same experiments and the results were compared.

• The Journal of the Korean dental association
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• v.48 no.8
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• pp.607-614
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• 2010

Reconstruction after ablative oral cancer surgery is challenging mission. Soft tissue and hard tissue could be resected in case of advanced oral cancer. The final goal of oral reconstruction is to gain normal swallowing, chewing and speech. Nowadays, free flap reconstruction after oral cancer resection is more popular than pedicled flap. Microsurgical reconstruction with free flap could be used effectively in complicated cases of oral cavity defect. However, complications could be happened. So not only meticulous preoperative study about the extent of defects but also the donor site dressing after surgery were performed to prevent postoperative complication. The most favorite free flap for soft tissue reconstruction is radial forearm flap. It has a lot of advantages such as pliable, hairless, reliable vessels, appropriate diameter of radial artery and diverse flap design. And the most popular free flap for jaw reconstruction is free fibular flap. In this article, we report the classification of flap for reconstruction and reveal the pits and falls of radial forearm free flap and free fibular flap.

• Journal of Pharmaceutical Investigation
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• v.41 no.1
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• pp.1-7
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• 2011

The effects of different formulation variables including pressure sensitive adhesive (PSA), permeation enhancer, thickness of the matrix and loading amount of drug on the transdermal absorption of galantamine were investigated across the hairless mouse skin. The permeation profile of galantamine was different depending on the types of PSA, loading amount of drug, thickness of the matrix and type of enhancer used. Highest flux of galantamine was obtained from acrylic PSA but crystals were formed in the patch within 72 h. Among the PSAs screened, crystal formation was not observed only in the patches formulated in Styrene Butadiene Styrene (SBS) matrix. Permeation rate increased linearly as the concentration of galantamine in SBS matrix increased from 2.5 to 15% w/w. Among the enhancers screened, Brij$^{(R)}$ 30 provided highest flux of galantamine. Matrix thickness of 80 ${\mu}m$ was optimum for maintaining adhesiveness as well as consistently delivering galantamine for longer period of time.

• Journal of Pharmaceutical Investigation
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• v.24 no.4
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• pp.281-287
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• 1994

The effects of oleic acid, propylene glycol and 5% (w/w) oleic acid in propylene glycol on the electrical properties of hairless mouse skin were studied and the results were compared. The complex electrical impedance was measured as a function of frequency, and resistance and capacitance were determined from the Nyquist plot. Immediately after the treatment with oleic acid, resistance was 145% of the pretreatment value. However it decreased with time and, after 20 hours, it was about 25% of its pretreatment value. Capacitance increased; immediately after the treatment, it was about 125% of pretreatment value and it seemed to increase slowly with time. When the skin was treated with propylene glycol, resistance decreased about 5O% and capacitance increased about 65%. Similar results were observed when the skin was treated with 5% (w/w) oleic acid in propylene glycol, except that the magnitude of resistance drop was much larger. Oleic acid acted synergistically with propylene glycol. Together with the flux data in the literature, the results obtained in this work indicate that electrical resistance is closely related to the permeability of drug molecules through the skin. The results are discussed in terms of the mechanism of action of these penetration enhancers. Overall, this work provided further mechanistic insight into the role of SC lipids in skin resistance and capacitance.

• Journal of Pharmaceutical Investigation
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• v.27 no.4
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• pp.271-277
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• 1997

Because omeprazole(OMP) is very unstable in aqueous condition, $OMP-{\beta}-CD$, the inclusion complex of OMP and ${\beta}-cyclodextrin({\beta}-CD)$ was made and physicochemical properties of it were compared with those of OMP. Skin permeability of OMP and $OMP-{\beta}-CD$ in propylene glycol vehicle and the reciprocal action of ${\beta}-CD$ with various enhancers were examined through hairless mouse. Adhesive patches were prepared with polyisobutylene and the skin permeability and stability of OMP were investigated. The inclusion complex showed higher solubility and lower partition coefficient than OMP itself. DMSO, 1-methyl 2-pyrrolidone and sodium cholate had an enhancing effect. However ethanol and polysorbate 80 hardly showed the enhancing effect of OMP. When sodium lauryl sulfate and sodium cholate as enhancer were added in patch, the former case showed higher permeability of OMP.

• Journal of Pharmaceutical Investigation
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• v.25 no.1
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• pp.47-54
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• 1995

Transdermal patch formulations of estradiol to treat post-menopausal symptoms and prevent osteoporosis in women were developed and evaluated for the permeation characteristics through the excised hairless mouse abdorminal skin and the uterotropic effect on the ovariectomized rabbits. The design of patch formulations was optimized by varying several formulation parameters, such as type of enhancers, amount of enhancers, amount of drug loading and coating thickness. Compared to a commercially available transdermal product, several patch formulations showed the similar skin permeation profiles (following zero-order kinetics), but their skin permeation rates were lasted for the longer period (a week). In one-week uterotropic efficacy test in the ovariectimized rabbits, the selected patch formulations showed the positive effect in atrophy of the urogenital epithelium. The mean values of uterus weight in rabbits after application of patches containing estradiol were much higher than those in control group (containing no drug).

• Journal of Pharmaceutical Investigation
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• v.26 no.2
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• pp.99-103
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• 1996

Effects of glycerin and PEG 400 in donor and receptor solutions upon skin permeation of drug were investigated. Deoxycortisone was used as a model compound. In vitro skin permeation study with freshly excised hairless mouse skin was performed and the steady-state skin permeation rates of the drug were determined in different fractions of glycerin or PEG 400 in donor and receptor solutions. Glycerin in donor solution didn't show any effect on the skin permeation rate of deoxycortisone. However glycerin in receptor solution showed significant effect on the skin permeation rate of the drug. In glycerin, there's a critical concentration for balancing hydration and dehydration of skin. At low concentration, less than 20 %, glycerin showed the enhancement of the flux due to the hydration effect of skin. At high concentration, more than 30 %, glycerin retard the permeation rate which might be due to the dehydration effect on the dermis layer. Since dermis has more water content than the stratum corneum, the steady state skin permeation rates were more influenced when glycerin was in receptor solution than that of in donor solution. PEG 400 aqueous solutions doesn't affect the steady state permeation rate of deoxycortisone significantly.

• Journal of Pharmaceutical Investigation
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• v.41 no.6
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• pp.337-345
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• 2011

The objective of this work is to investigate the effect of chemical enhancer and current on the flux of donepezil hydrochloride (DH) through skin. Ethanol and N-methyl pyrrolidone (NMP) were used as chemical enhancers in combination with iontophoresis. We also have studied the effect of pH on flux and evaluated the role of electroosmosis. In vitro flux study was performed at $33^{\circ}C$, using side-by-side diffusion cell and full thickness hairless mouse skin. Passive flux of DH without enhancer was very small. As the concentration of enhancer increased, passive flux increased. After current application, flux increased markedly and the time to reach maximum decreased. Without enhancer, maximum flux was about 50 fold larger than that obtained without current. These results indicate that electromigration is playing a major role for the transport. As the enhancer concentration increased, flux also increased. NMP and ethanol increased not only the passive delivery, but also the iontophoretic delivery. Flux results indicate that ethanol has better ability than NMP in enhancing the transport of DH. The magnitudes of increase in flux by these enhancers indicate that there is a large synergistic effect in flux enhancement. Flux results from pH study showed that electroosmotic flow is reversed at low pH and the flux is hindered. These results provided some information on the flux enhancing ability of ethanol and NMP in combination with iontophoresis. The data also provided some mechanistic insights into the role of electromigration and electroosmosis on flux through skin.

• Journal of Pharmaceutical Investigation
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• v.35 no.3
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• pp.165-171
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• 2005

Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. However, it is difficult for itraconazloe to be delivered by topical system due to its poor aqueous solubility. First, niosomes containing drug were prepared with span 60, cholesterol. tocopherol and poloxamer 407 as vesicle forming agents in an effort to increase solubility of itraconazole. And then prepared niosomes were dispersed in O/W creams (containing xanthan gum, glycerin, vaseline, glyceryl monostearate and $Cerix^{\circledR}-5$) or gels (containing xanthan gum and poloxamer 407). Both creams and gels were evaluated with respect to their rheological properties, in vitro permeation through excised skin of hairless mouse. Creams or gels containing niosome showed pseudoplastic flow and hysteresis loop. For both creams and gels, viscosity was increased with increasing the content of glycerine or vaseline and the content of gel forming polymer, respectively. In creams, the permeability of drug to skin was decreased with increasing the viscosity of cream. The permeability of drug was affected by pH as well as viscosity of gel. In vitro permeation test results demonstrated that cream formulations showed better permeability than gels. In conclusion, these results suggest that creams formulation containing niosome can be useful for the topical delivery of intraconazole.