• 한국식품과학회지
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• 제52권5호
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• pp.467-475
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• 2020

자외선(Ultraviolet radiation)은 피부 주름 형성과 피부 건조를 특징으로 하는 광노화의 주요 원인이다. 모자반과(Sargassaceae)에 속하는 모자반(Sargassum fulvellum)은 항염증, 항산화, 항아토피 활성을 갖고 있다. 특히, 모자반은 인간 각질세포(keratinocyte)와 실험동물의 피부에서 UVB에 의한 염증 반응을 완화시키는 것으로 보고되었다. 그러나, 현재까지 모자반 추출물의 광노화 억제 효과에 대해서는 보고된 바가 없다. 본 연구에서는 광노화를 유도하기 위하여 UVB를 SKH-1 무모 마우스의 등 부분에 8주간 처리하였으며, 동시에 모자반 추출물을 300 mg/kg의 농도로 매일 경구 투여하였다. 현상학적으로, 모자반 추출물은 주름 형성, 홍반 및 피부 두께를 감소시켰으며, 피부 탄력을 증가시켰다. 모자반 추출물은 콜라겐 합성 유전의 발현을 증가시키고, matrix metalloproteinase의 발현을 감소시킴으로써 콜라겐의 하이드록시프롤린(hydroxyproline) 함량을 증가시켰다. 추가적으로, 모자반 추출물의 경구 투여는 무모 마우스의 피부 수분 함량을 증가시켰으며, 경피수분손실(transepidermal water loss)을 감소시켰다. 모자반 추출물은 각질세포막 형성에 관여하는 involucrin, loricrin, transglutaminase의 발현과 자연보습인자 관련 생체지표인 filaggrin 및 caspase-14의 발현을 증가시켰다. 종합적으로, 모자반 추출물은 피부의 콜라겐 손실과 건조를 완화함으로써 광노화 억제 활성을 제공하였다. 모자반 추출물은 피부 광노화를 억제하기 위한 기능성 식품 소재로서 활용될 수 있을 것으로 판단된다.

• Journal of Pharmaceutical Investigation
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• 제37권4호
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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.

• 동의생리병리학회지
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• 제28권2호
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• pp.206-216
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• 2014

To investigate the anti-photoaging effect of fermented Red Ginseng(RG) in SKH-1 mice. We examined the effects of extracts of non-fermented RG(NRG group), fermented RG(FRG group) and fortified fermented RG(FFRG group) on skin wrinkles formation, histological changes related to the number of epidermal cell layers, epidermal thickness, neutrophil infiltration into dermis, degradation of collagen fibers, and the number of mast cells, and immunohistochemical changes related to cytokines and enzymes in photoaging skin caused by UVB irradiation of SKH-1 mice. The oral administration(300 mg/Kg B.W./day) and topical application($100{\mu}{\ell}/mouse/day$) of extracts of NRG, FRG and FFRG inhibited increases in epidermal thickness and wrinkle formation compared to control group in dorsal skin induced by UVB irradiation. We observed more increased stainability of acid fuschin and aniline blue in dermis of FFRG group than those of other groups. Furthermore, NRG, FRG and FFRG prevented the disruption of collagen fibers within papillary layer of dermis, and decreased number of mast cells in the dorsal skins induced by UVB irradiation. We observed fine wrinkle formation in FFRG group. Treatment with NRG, FRG and FFRG decreased immunohistochemical density of myeloperoxidase related to inflammation in the photoaging skin. We observed more decreased immunohistochemical density of myeloperoxidase in FFRG group than those of other groups. Immunohistochemical density of PCNA and Ki-67 in FFRG group was more decreased than those of other groups. Our study suggests that fermented red ginseng extracts participates in inhibitory effects in the morphological processes related to photoaging skin on UVB irradiated SKH-1 mice.

• Biomolecules & Therapeutics
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• 제24권5호
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• pp.529-535
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• 2016

Atopic dermatitis (AD) results from gene and environment interactions that lead to a range of immunological abnormalities and breakdown of the skin barrier. Protease-activated receptor 2 (PAR2) belongs to a family of G-protein coupled receptors and is expressed in suprabasal layers of the epidermis. PAR2 is activated by both trypsin and a specific agonist peptide, SLIGKV-$NH_2$ and is involved in both epidermal permeability barrier homeostasis and epithelial inflammation. In this study, we investigated the effect of lobaric acid on inflammation, keratinocyte differentiation, and recovery of the skin barrier in hairless mice. Lobaric acid blocked trypsin-induced and SLIGKV-$NH_2$-induced PAR2 activation resulting in decreased mobilization of intracellular $Ca^{2+}$ in HaCaT keratinocytes. Lobaric acid reduced expression of interleukin-8 induced by SLIGKV-$NH_2$ and thymus and activation regulated chemokine (TARC) induced by tumor necrosis factor-a (TNF-${\alpha}$) and IFN-${\gamma}$ in HaCaT keratinocytes. Lobaric acid also blocked SLIGKV-$NH_2$-induced activation of ERK, which is a downstream signal of PAR2 in normal human keratinocytes (NHEKs). Treatment with SLIGKV-$NH_2$ downregulated expression of involucrin, a differentiation marker protein in HaCaT keratinocytes, and upregulated expression of involucrin, transglutamase1 and filaggrin in NHEKs. However, lobaric acid antagonized the effect of SLIGKV-$NH_2$ in HaCaT keratinocytes and NHEKs. Topical application of lobaric acid accelerated barrier recovery kinetics in a SKH-1 hairless mouse model. These results suggested that lobaric acid is a PAR2 antagonist and could be a possible therapeutic agent for atopic dermatitis.

• 대한수의학회지
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• 제48권4호
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• pp.413-421
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• 2008

It was previously found that PG102, a water-soluble extract derived from Actinidia arguta, was able to modulate Th1/Th2 pathways and suppress IgE production resulting in dramatic amelioration of atopic dermatitis in NC/Nga mouse and hairless rat models. In order to evaluate the subacute toxicity of PG102, female and male SD rats were daily fed with various doses of PG102 for 4 weeks. Six week old SD rats were randomly divided into 4 groups and orally administrated with 100-, 300-, and 1,000- mg/kg of PG102 as well as the vehicle only. At the end of the study, no significant differences in the body and organ weights were observed between control and treated rats of both genders. Hematological and blood chemical analysis showed little differences between the animal groups. Neither gross abnormalities nor histopathological changes were found. PG102 produced little or no subacute toxicity and could be used as a safe nutraceutical for the treatment of individuals with allergic diseases including atopic dermatitis.

• Journal of Pharmaceutical Investigation
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• 제41권1호
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• pp.9-17
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• 2011

The objective of this work is to study transdermal delivery of calcitonin using iontophoresis and to evaluate various factors which affect the transdermal transport. We have studied the effect of polarity, current density, drug concentration, penetration enhancers (isopropyl myristate [IPM] and ethanol) and laser treatment on transdermal flux and the results were compared. We also investigated the iontophoretic flux from microemulsions containing calcitonin together with oleic acid (OA) or IPM. In vitro flux study was performed at $33^{\circ}C$, using side-by-side diffusion cell and full thickness hairless mouse skin. Anodal delivery at pH 3.0 was much larger than cathodal and passive delivery, due to the positive charge of calcitonin. Cumulative amount delivered (CUM) by cathodal or passive delivery was close to zero for 10 hours. The pretreatment of skin by neat IPM markedly increased the CUM anodically. CUM increased as the current density, drug concentration or the duration of IPM treatment increased. Microemulsion containing IPM or oleic acid was prepared and the phase diagram was constructed. CUM also increased when IPM was incorporated into a microemulsion. OA microemulsion showed similar enhancing effect to IPM microemulsion. The delivery of calcitonin from 70% (v/v) ethanol aqueous solution showed a large increase in flux. Laser treatment of skin before flux experiment exhibited about 2 fold increase in total calcitonin amount transported for 12 hours, when compared to that delivered by IPM microemulsion. Based on these results, we have evaluated the possibility of delivering enough amount of calcitonin to reach the therapeutic level. The data suggest that it is highly possible to deliver clinically effective amount of calcitonin using iontophoresis patch with small area (<10 $cm^2$).

• Journal of Pharmaceutical Investigation
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• 제27권1호
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• pp.65-69
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• 1997

To formulate the topical analgesic preparation of a new capsaicin derivative, DA-5018, a skin penetration evaluation system was established and the effect of composition of formulation on skin penetration using this system was evaluated, The effect of massage on hairless mouse skin penetration and inter-day variation of this effect were investigated using test formulations(cream). In massage group, compared with non-massage group, absolute penetration amount of DA-5018 increased and this experimental system was found to be reproducible, The effects of pH of water phase, ratio of oil/water and the concentration of active ingredient in cream on skin penetration were investigated. The permeation of DA-5018 from the cream increased with increasing pH of water phase to 9. But at pH 10, the permeation of DA-5018 decreased, because of the physical instability of the cream. The permeation of DA-5018 from the cream increased with increasing the ratio of oil/water of the cream. The increase of the content of DA-5018 to 0.3% increased the permeation of DA-5018, but at high concentration(1.0%), the permeation of DA5018 decreased, due to the instability of the cream.

• Journal of Pharmaceutical Investigation
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• 제37권3호
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• pp.167-171
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• 2007

Itraconazole is one of the most potent antifungal agents available in the market today. However, the low bioavailability due to its poor-water solubility calls for an alternative formulation to the current oral type. A topical itra-conazole-containing formulation may be of use for several reasons including the opportunity to reduce adverse events and generate high local tissue levels, more rapid drug delivery, and lower systemic exposure. The purpose of the present study was to investigate the vehicles for topical skin delivery of itraconazole. The effect of formulations on the hairless mouse skin permeation and deposition of itraconazole was determined using Franz diffusion cells at $37^{\circ}C$. Benzyl alcohol in micro-emulsion significantly increased the solubility of itraconazole, thereby increasing the skin permeation rate. However, lipo-some formulation showed the lowest solubility and permeation rate of itraconazole. Although the solubility of itraconazole in hydrogel formulation was lower than that in microemulsion, skin permeation rate was significantly higher probably due to its adhesive property. Therefore, microemulsion-based hydrogel formulation is expected to synergistically increase the skin permeation rate and skin deposition of itraconazole.

• Journal of Pharmaceutical Investigation
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• 제37권3호
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• pp.149-158
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• 2007

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. To increase the skin permeation of lidocine, the effects of $Labrasol^{(R)}$, $Labrafil^{(R)}$, $Labrafac^{(R)}$ and $Transcutol^{(R)}$ were investigated. The skin permeation of lidocaine was increased when $Labrasol^{(R)}$ and $Transcutol^{(R)}$ were used as permeation enhancer. To evaluate the influence of ultrasound, various factors such as application modes (continuous mode and pulsed mode), frequency (1.0 and 3.0 MHz) and intensity (1.0, 1.5 and 2.0 w/$cm^2$) were investigated with lidocaine hydrogel. The pronounced effect of ultrasound on the skin permeation of lidocaine was observed at all ultrasound energy levels. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1 MHz, 2.0 w/$cm^2$ and continuous treatment. As the intensity of ultrasound increased, the permeation of lidocaine was accelerated. 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 K group (ultrasound with gel base only), L group (lidocaine gel) and B group (ultrasound with lidocaine gel). 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 the skin permeation and in vivo anaesthetic effect.

• 대한한의학회지
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• 제38권4호
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• pp.62-81
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• 2017

Objectives: As interests in the beauty of skin is growing continuously, more people are focusing on white and clean skin. Melanin is the major factor that determines skin color. The abnormal concentration of melanin causes various skin diseases such as vitiligo, freckles, and melasma. This study investigated the inhibitory effect of Eriobotryae Folium extracts (EF) with phreatic water (PW) on the melanin synthesis. Methods: The effect of EF on melanin synthesis was evaluated by using mouse melanoma cells (B16F10). To define the mechanisms, real-time PCR and western blot were used. We also evaluated the inhibitory effects of EF and PW on melanin synthesis by using HRM-2 melanin-possessing hairless mice. After UVB irradiation, melanin differences between the skin parts that were treated and untreated with EF and PW. Levels of mRNA were measured by real-time quantitative PCR and histological analysis of the dorsal skin was conducted by hematoxylin and eosin staining. Results: EF inhibited various mechanisms of melanogenesis, and the effect was increased when combined with PW. In vitro experiments have shown that EF inhibited the expressions of tyrosinase related protein-1 (TRP-1) mRNA, tyrosinase mRNA, microphthalmia-associated transcription factor (MITF) mRNA and the tyrosinase inhibitory activation, but it stimulated the extracellular regulated kinase (ERK) mRNA expression. In vivo experiments have shown that EF prevented melanogenesis in the mice dorsal skin and inhibited TRP-1 mRNA expression. Also these effects were increased when combined with PW. Conclusions: EF and PW might be a new and effective treatment for whitening and treating pigmentation of skin.