• Archives of Plastic Surgery
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• 제43권6호
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• pp.498-505
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• 2016

Background Algae have traditionally been used for promotion of hair growth. Use of hair regrowth drugs, such as minoxidil, is limited due to side effects. The aim of this study was to examine a mixture of Saccharina japonica and Undaria pinnatifida (L-U mixture) on hair growth and to compare the promoting effect of hair growth by a 3% minoxidil and a L-U mixture. Methods To evaluate the hair growth-promoting activity, saline, 50% ethanol, 3% minoxidil, and the L-U mixture were applied 2 times a day for a total of 14 days on the dorsal skin of C57BL/6 mice after depilation. Analysis was determined by using a high-resolution hair analysis system, real-time polymerase chain reaction, and H&E staining. Results On day 14, the hair growth effect of the L-U mixture was the same as that of the 3% minoxidil treatment. The L-U mixture significantly (P<0.05) stimulated hair growth-promoting genes, as vascular endothelial growth factor (VEGF) and insulin-like growth factor -1. Increase of VEGF was observed in the L-U mixture group compared with minoxidil and the negative control. In contrast, the L-U mixture suppressed the expression of transforming growth factor-${\beta}1$, which is the hair loss-related gene. In histological examination in the L-U mixture and minoxidil groups, the induction of an anagen stage of hair follicles was faster than that of control groups. Conclusions This study provides evidence that the L-U mixture can promote hair growth in mice, similar to the effect from minoxidil, and suggests that there is potential application for hair loss treatments.

• 대한화장품학회지
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• 제49권2호
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• pp.127-139
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• 2023

본 연구에서는 의약품 원료로 잘 알려진 minoxidil과 화장품 원료인 diaminopyrimidine oxide (DAO) 활성성분으로 사용하여 니오좀(niosome)의 물성평가와 더불어 인공피부에 대한 경피투과율을 비교하였다. 나노입자의 니오좀을 제조하기 위해 고압유화(high pressure homogenization) 방법을 이용하였으며 제타사이저(zetasizer)로 물성평가를 진행하였다. 활성성분을 포함한 니오좀의 입자크기는 HLB에 따라 평균 99 ~ 123 nm, 제타전위(zeta potential)는 -60 ~ -81 mV의 범위로 측정되었다. DSC (differential scanning colorimetry)를 통해 결정성 성분인 minoxidil이 니오좀 내에 무결정 상태로 균일하게 용해되어 있음을 확인하였다. 경피투과량을 확인 및 비교하기 위해 in vitro Franz diffusion cell 방법으로 측정하였으며, 니오좀 제형이 대조군인겔 제형보다 minoxidil의 경우 3.4배, DAO의 경우 11.1배 높은 투과율을 보였다. 또한 minoxidil과 DAO 니오좀의 경피투과 비교 시 유사한 경향을 보였으며, 상대적으로 DAO의 투과량이 많았다. HLB 값을 달리한 니오좀 제형을 Cryo-TEM을 이용하여 형상을 관찰하였으며, 모두 소포체가 형성되었으며 SUV (small unilamella vesicle)와 LUV (large unilamella vesicle)의 중간 형태임을 확인하였다. 본 연구를 통하여 탈모에 효과적인 약물인 minoxidil과 화장품 원료인 DAO 성분을 니오좀 제형에 캡슐화시킴으로써 효과적으로 피부에의 전달을 기대할 수 있다.

• 약학회지
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• 제30권5호
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• pp.228-231
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• 1986

The effect of temperature and pH on the degrdation of minoxidil in the aqueous solution was investigated and the stability of pharmaceutical preparation for solution was also studied. The degradation of minoxidil in the aqueous solution was first order type reaction and the rate constant at $20^{\circ}C$ in pH 7.0 phosphate buffer solution was 9.464${\times]10^{-3} day^{-1}$ and calculated activation energy was 11.7 kcal/mol. The degradation of minoxidil was acid-base catalytic reaction and the most stable range of pH was about 5.0. The liquid pharmaceutical preparation was very stable in 3 months.

• 폴리머
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• 제37권3호
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• pp.393-398
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• 2013

본 실험에선 미녹시딜을 함유한 수용성 고분자 젤로부터 solvent casting 방법으로 250과 $750{\mu}m$ 두 가지 길이의 미녹시딜이 함유된 용융형 고분자 마이크로 니들(micro-needle)을 제작하였다. 제작된 미녹시딜을 함유한 용융형 고분자 마이크로 니들은 기계적 강도가 입증된 고분자 니들과 동일한 형태 및 기계적 강도를 나타냈으며, 성공적으로 피부를 투과함을 확인하였다. 제조된 고분자 마이크로 니들의 경우 피부 적용 후 최소 30분 이상은 부착되어야 전체 니들의 50% (v/v) 이상이 피부 내로 용융되었으며, 니들 적용부위에서 서서히 약물의 방출 및 확산을 확인할 수 있었다. 또한 C57BL/6 동물 모델을 통해 미녹시딜이 함유된 250, $750{\mu}m$ 길이의 고분자 마이크로 니들이 무처리군 혹은 미녹시딜 처리군에 비해 발모에 긍정적인 영향을 나타냄을 확인할 수 있었다.

• 한국임상약학회지
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• 제25권3호
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• pp.171-177
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• 2015

Background: Androgenetic alopecia (AGA), one of alopecias, requires continuous treatment in order to prevent or stop it, and patient's compliance is very important. Currently, only two drugs (finasteride, minoxidil) have been approved for AGA by Food and Drug Administration of United States (US FDA). However, another ${\alpha}-2$ reductase inhibitor, dutasteride, is approved by Korea Ministry of Food and Drug Safety (MFDS) through a phase III trial. For treatment, pharmacotherapy of AGA usually combines topical minoxidil 7% with one of oral <${\alpha}-2$ reductase inhibitor. Objectives: We evaluated the comparative efficacy and adverse effect between topical minoxidil 7%/finasteride 1 mg and topical minoxidil 7%/dutasteride 0.5 mg pharmacotherapy for outpatients with AGA. Also we evaluated the relationship between therapeutic effect and regular hospital visit. Method: This study was performed retrospectively based on electronic medical record (EMR) data of total 98 patients (topical minoxidil 7% with dutasteride 0.5 mg ($Avodart^{(R)}$) or finasteride 1 mg ($Alopecia^{(R)}$, $Propecia^{(R)}$) with diagnosis of AGA from department of dermatology at a secondary hospital from January $1^{st}$, to May $31^{st}$, 2014. Results: The efficacy and adverse event of topical minoxidil 7%/dutasteride 0.5 mg (DUTA group) were 100% and 45.7%, and of topical minoxidil 7%/finasteride 1 mg (FINA group) were 92.1% and 33.3%, respectively. The mean onset time of responses and adverse events in the FINA group were 3.86 months and 4.43 months. Those in the DUTA group were 3.97 months and 5.06 months. Conclusion: Both FINA and DUTA group were highly effective, but the DUTA group showed higher efficacy and adverse effects than those in the FINA group. Dutasteride may be another alternative in AGA treatment.

• Biomolecules & Therapeutics
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• 제4권3호
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• pp.275-279
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• 1996

We have synthesized the cinnamyl derivative of minoxidil, N-2-cinnamylamino-4-amino-6-piperidinopyrimidine 3-oxide(MINAMYL). Physicochemical properties and structural analysis on this compound were examined. And also, we have screened its antialopecic effect.

• 대한본초학회지
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• 제26권4호
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• pp.9-14
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• 2011

Objective : Present study was carried out to investigate the effect of Gyungohkgo-gamibang extract on hair growth and protein expression in an alopecia model of C57BL/6 mice. Methods : Mice were divided into 3 experimental groups including normal (vehicle), Gyungohkgo-gamibang extract (YNS-10) and 5% minoxidil-treated group. The test materials were daily applied with 0.1 ml per mouse on shaved dorsal skin for 3 weeks. The hair growth was monitored by photograph at 5, 10, 15, 21 days after topical application. Then the changes of hair density and hair thickness in the hair-removed area were evaluated by phototrichogram using folliscope. Also the expression level of growth factors related to hair growth was measured by western blotting. Results : Application of minoxidil or YNS-10 stimulated the hair growth compared to vehicle treatment. Therefore hair density of minoxidil or YNS-10 application was increased about 200% and 210% more than in vehicle application on 14 day, respectively. And hair thickness of both minoxidil group and YNS-10 group was increased about 220% and 210 % more than in vehicle spreading on 14 day, respectively. Futhermore the protein expression of IGF-1 and VEGF were significantly up-regulated on 7 day in YNS-10 and minoxidil-spreaded group compared to vehicle-applied group. Conclusion : These data suggest that YNS-10 has potent stimulating activity on hair growth in C57BL/6 mice and potential usefulness as ingredients of hair tonic and hairrestore.

• 약학회지
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• 제39권5호
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• pp.511-515
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• 1995

N-4-salicyloamide-2-ainino-6-piperidinopyrimidine 3-oxide(SALMI) was synthesized by condensation of chloride compound of salicylic acid with minoxidil in organic solvent, and was identified by MS, UV and IR etc.

• KSBB Journal
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• 제27권2호
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• pp.121-126
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• 2012

In order to explore structural features of minoxidil analogs with a view of enhancing lysyl hydroxylase (LH) inhibitory activity, molecular holographic QSAR (HQSAR) and CoMSIA (comparative molecular similarity indices analysis) were performed. The results from the atomic contributions with optimized the HQSAR 6-2 model indicated that, in case of pyrimidine-1-N-oxide substituent, C2 atom of pyrimidine ring and C'3-C'4 bond of 4-piperidinol group showed the highest impact on the inhibitory activity towards LH enzyme. It was also evident from the information of the optimized CoMSIA F5 model that the inhibitory activity mainly depended on the hydrophobic field contribution (36%) and the hydrogen bond (H-bond) field contribution (49.2%) of substrate molecule. Particularly, it is predicted that the functional groups which disfavor H-bond acceptors in large space around the piperidinol group and also the functional groups which favor the H-bond acceptors at C'4 (& C'5) atom in $R_5$ group play a role for increased inhibitory activity. With this in mind, it is likely that a novel candidate having more improved inhibitory activity on hair growth could be designed in the future.

• Biomolecules & Therapeutics
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• 제31권1호
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• pp.116-126
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• 2023

Mainly due to the slanted focus on the mechanism and regulation of neuronal aging, research on astrocyte aging and its modulation during brain aging is scarce. In this study, we established aged astrocyte culture model by long-term culturing. Cellular senescence was confirmed through SA-β-gal staining as well as through the examination of morphological, molecular, and functional markers. RNA sequencing and functional analysis of astrocytes were performed to further investigate the detailed characteristics of the aged astrocyte model. Along with aged phenotypes, decreased astrocytic proliferation, migration, mitochondrial energetic function and support for neuronal survival and differentiation has been observed in aged astrocytes. In addition, increased expression of cytokines and chemokine-related factors including plasminogen activator inhibitor -1 (PAI-1) was observed in aged astrocytes. Using the RNA sequencing results, we searched potential drugs that can normalize the dysregulated gene expression pattern observed in long-term cultured aged astrocytes. Among several candidates, minoxidil, a pyrimidine-derived anti-hypertensive and anti-pattern hair loss drug, normalized the increased number of SA-β-gal positive cells and nuclear size in aged astrocytes. In addition, minoxidil restored up-regulated activity of PAI-1 and increased mitochondrial superoxide production in aged astrocytes. We concluded that long term culture of astrocytes can be used as a reliable model for the study of astrocyte senescence and minoxidil can be a plausible candidate for the regulation of brain aging.