• Journal of Pharmaceutical Investigation
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• 제30권4호
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• pp.283-288
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• 2000

The purpose of the present study was to investigate the topical bioavailability of retinol (vitamin A) after its transdermal administration. For this purpose, we developed the convenient HPLC method to measure the retinol concentration in the biological fluids such as plasma and skin tissues. The low detection limit was $0.1\;{\mu}g/ml$ using a gradient HPLC system of UV detection. The initial plasma concentration of retinol was about $20\;{\mu}g/ml$ after its i.v. bolus administration (4.32 mg/kg). The half life $(t_{1/2{\alpha}})$ in the distributive phase was 1.3 min, while retinol was slowly disappeared in the post-distributive phase. On the other hand, the maximum plasma concentration $(C_{max})$ was about 776 ng/ml after appling to rat skin at a dose of 43.2 mg/kg. Furthermore, the concentration of retinol in the skin tissues was about 600 ng/g tissue at 12 hr after its transdermal administration. In conclusion, the initial plasma concentration of retinol was comparable with the skin concentration after its cutaneous absorption, followed by being decreased with the passage of the time.

• Journal of Pharmaceutical Investigation
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• 제39권3호
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• pp.177-183
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• 2009

A rapid and sensitive reversed-phase high performance liquid chromatography (HPLC) method was developed for the determination of piroxicam in the rabbit plasma. After a treatment of plasma sample by liquid-liquid extraction, the drug was analyzed on an HPLC system with ultraviolet detection at 330 nm. HPLC was carried out using reversed-phase isocratic elution with a C18 column, a mobile phase of a mixture of acetonitril, doubly deionized water and acetic acid 43.74:56.00:0.26 v/v%) at a flow rate of 1.1 mL/min. The chromatograms showed good resolution and sensitivity and no interference of plasma. The calibration curve for the drug in plasma sample was linear over the concentration range of 0.01-2.0 ${\mu}$g/mL. The intra- and inter-day assay accuracies of this method ranged from 86.82% to 108.33% of normal values and the precision did not exceed 13% of relative standard deviation. The plasma concentration of piroxicam decreased to below the quantifiable limit at 12 hr after the i.v. bolus administration to rabbits following dose of 0.375 mg/kg yielding a apparen t plasma half life of 1.38 hr. The transdermal route prolongs plasma levels of piroxicam. The bioavailability, calculated from the dose-adjusted ratio of the $AUC_{transdermal}$ to the $AUC_{i.v.}$, was 7.44%. The plasma concentration of piroxicam was detected by 48 hr after the transdermal administration of patch at a dose of 32 mg/kg. This method was suitable for cutaneous absorption studies of piroxicam in the rabbit after transdermal administration of different types of dosages of the drug.

• Journal of Pharmaceutical Investigation
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• 제32권4호
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• pp.259-265
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• 2002

Piroxicam is one of the NSAID, which is used in the systemic and topical treatment of a variety of inflammatory conditions. Conventionally, for topical use, the drug is formulated in gel. We designed an phonophoretic drug delivery system to investigate the piroxicam permeability and the influence of ultrasound application (continuous mode, pulsed mode), frequency (1.0 MHz, 3.0 MHz) and intensity $(1.0\;w/cm^2,\;1.5\;w/cm^2,\;2.0\;w/cm^2)$ with 0.5% piroxicam gel. Per cutaneous absorption studies were performed in vitro models to determine the rate of drug absorption via the skin. Permeation study using hairless mouse skin was performed at $37^{\circ}C$ using buffered saline (pH 7.4, 10% propylene glycol solution) as the receptor solution. Anti-inflammatory activity was determined using carrageenan-induced foot edema model in rat. A pronounced effect of ultrasound on the skin absorption of the piroxicam was observed at all ultrasound energy level studied. Ultrasound was carried out for 10 hr. The highest permeation was observed at intensity of $2.0\;w/cm^2$, frequency of 1.0 MHz and continuous output. The inclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory activity in vivo.

• Natural Product Sciences
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• 제16권3호
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• pp.185-191
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• 2010

Mast cell-mediated allergic disease is involved in many diseases such as anaphylaxis, asthma and atopic dermatitis. The discovery of drugs for the treatment of allergic disease is an important subject in human health. In the present study, the effect of water extract of Gleditsiae Spina (WGS) (Leguminosae), on compound 48/80-induced systemic allergic reaction, anti-DNP IgE antibody-induced local allergic reaction, and histamine release from human mast cell line (HMC-1) cells were studied. In addition, the effect of WGS on phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore A23187 (A23187)-induced gene expression and secretion of pro-inflammatory cytokines were investigated using HMC-1 cells. WGS was anally administered to mice for high and fast absorption. WGS inhibited compound 48/80-induced systemic allergic reaction. WGS dose-dependently decreased the IgE-mediated passive cutaneous anaphylaxis. WGS reduced histamine release from HMC-1 cells. In addition, WGS decreased the gene expression and secretion of pro-inflammatory cytokines in PMA plus A23187-stimulated HMC-1 cells. These findings provide evidence that WGS could be a candidate as an antiallergic agent.

• 한국동물학회지
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• 제23권4호
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• pp.219-228
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• 1980

도룡뇽 (Hynobius leechi Boulenger)의 피부과립선의 미세구조를 전자현미경으로 관찰하여 다음과 같은 결과를 얻었다. 1. 도룡뇽의 피부과립선은 선체부와 분비관으로 구성되며, 선체부는 선상피세포와 근상피세포, 분비관은 각질세포들로 구성되었다. 2. 피부과립선의 선상피세포는 세포질의 전자밀도가 높은 암세포와 세포질의 전자밀도가 낮은 명세포가 관찰되었다. 3. 피부과립선의 분비과립은 구형 또는 나형이었고, 높은 전자밀도를 보이는 과립, 중등도의 전자밀도를 보이는 과립 그리고 낮은 전자밀도를 보이는 과립들로 구분할 수 있었다. 또한 낮은 전자밀도를 보이는 과립중에는 과립막 인접부에 부분적으로 높은 전자밀도를 보이는 과립들이 관찰되었다. 4. 피부과립선내 분비과립들이 같은 세포내에서 전자밀도의 차이를 보이는 것은 분비과립의 성숙단계 및 성숙된 과립의 수분흡수 정도에 따른 농도차이에 기인하며, 그 화학적 조성은 유사하다고 생각한다.

• Archives of Pharmacal Research
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• 제19권2호
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• pp.116-121
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• 1996

Antisense oligonucleotides seem to provide a promising new tool for the therapy. Choi et al. (1995) reported antisense phosphorothioate oligonucleotides (PS-ODN, 25 mer) complementary to TGF-.betha. mRNA designed for scar formation inhibitor to eliminate scars, which was caused by undesired collagen deposition due to overexpression of TGF-.betha., in wounded skin. PS-ODN were evaluated in vitro for skin penetration using normal and tape-stripped damaged rat skin. The in vitro skin transports were carried out with partially modified PS-ODN (6S) and fully modified PS-ODN (25S). The cumulative amount of PS-ODN (6S) penetrated through normal rat skin was $0.234{\pm}0.041{\mu}g/cm^2$ and that of tape-stripped damaged rat skin was $1.077{\pm}0.301{\mu}g/cm^2$ over 8 hrs. PS-ODN (25S) can not be found in receptor medium through normal skin due to high molecular weight (Mol.Wt.=8,000) and polyanionic charge. However, the cumulative amount of PS-ODN (25S) penetrated across damaged rat skin in PBS was $0.340{\pm}0.296{\mu}g/cm^2$ over 8 hrs. The absense of dermis raised the cumulative amount of PS-ODN (6S) penetrated through rat skin. And the fluxes of PS-ODN (6S) and PSODN (25S) at 8hrs across damaged rat skin were $134.63{\pm}37.67{\mu}g/cm^2$ h, and $42.50{\pm}36.95ng/cm^2$ h, respectively. While PS-ODN (25S) was stable in 10% heat inactivated fetal bovine serum (FBS) during 24 hrs, PS-ODN (6S) was less stable than PS-ODN (25S), but was markedly stable than unmodified phosphodiester. It is suggested that the cumulative amount of PS-ODN (6S) penetrated through damaged rat skin is larger than that of PS-ODN (25S) since the former is easier to degrade by nuclease than the latter and then is apt to penetrate into skin. Thus, PS-ODN represents a logical candidate for further evaluation due to the potential for delivery into the wounded skin.

• 대한화장품학회지
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• 제50권2호
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• pp.153-161
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• 2024

비타민 D는 주로 자외선에 의해 피부에서 만들어지는 지용성 비타민이다. 멜라토닌과 함께 대표적인 '크로노바이오틱(chronobiotic)' 물질로써 피부가 낮과 밤을 구분하는데 중요한 역할을 한다. 하지만 비타민 D는 조효소 역할을 하는 비타민이자 여러 종류의 유전자 발현을 조절하는 호르몬적 역할을 하기 때문에 화장품에 직접적으로 사용할 수 없다. 따라서 화장품에 사용할 수 있는 비타민 D 전구체인 프로 비타민 D (7-dehydrocholesterol)의 피부 효능에 대해서 알아보고자 하였다. 그 결과, 프로 비타민 D는 멜라닌 생성 효소인 타이로시네이즈(tyrosinase)의 단백질 발현을 억제하여 멜라닌 생성을 억제할 수 있음을 확인할 수 있었다. 이와 같은 피부톤 케어 효과는 인공 피부에서도 검증되었다. 또한 프로 비타민 D는 피부 염증을 일으키는 TNFa의 발현을 억제하고, 자외선에 의해 비타민 D로 전환되면 항균 펩타이드인 CAMP (LL-37)의 발현을 증가시킨다는 것이 확인되었다. 프로 비타민 D가 멜라닌 생성을 억제하는 것은 멜라닌이 자외선을 흡수하여 프로 비타민 D가 비타민 D로 전환되는 것을 억제하기 때문인 것으로 보인다. 따라서 화장품 제형에 프로 비타민 D를 활용한다면 피부톤을 조절하고 피부 면역을 증진시킴과 동시에 일상 생활 속에서 자외선에 의해 비타민 D 전환되면 다른 피부 효능, 즉 피부 항노화, 장벽 기능 향상 등도 기대할 수 있을 것으로 생각한다.