• Title/Summary/Keyword: ethosomes

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Enhanced Transdermal Delivery of Drug Compounds Using Scalable and Deformable Ethosomes (에토좀 입자크기와 멤브레인 특성 조절을 통한 약물의 경피흡수능 향상)

  • An, Eun-Jung;Shim, Jong-Won;Choi, Jang-Won;Kim, Jin-Woong;Park, Won-Seok;Kim, Han-Kon;Park, Ki-Dong;Han, Sung-Sik
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.36 no.2
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    • pp.105-113
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    • 2010
  • This study introduces a flexible approach to enhance skin permeation by using ethosomes with deformable lipid membranes as well as controllable sizes. To demonstrate this, a set of ethosomes encapsulating an anti-hair loss ingredient, Triaminodil$^{TM}$, as a model drug, were fabricated with varying their size, which was achieved by solely applying the different level of mechanical energy, while maintaining their chemical composition. After characterization of the ethosomes with dynamic light scattering, transmission electron microscopy, and deformability measurements, it was found that their membrane deformability depended on the particle size. Moreover, studies on in vitro skin permeation and murine anagen induction allowed us to figure out that the membrane deformability of ethosomes essentially affects delivery efficiency of Triaminodil$^{TM}$ through the skin. It was noticeable in our study that there existed an optimum particle size that can not only maximize the delivery of the drug through the skin, but also increase its actual dermatological activity. These findings offer a useful basis for understanding how ethosomes should be designed to improve delivery efficiency of encapsulated drugs therein in the aspects of changing their length scales and membrane properties.

Characterization and Transdermal Delivery of Ethosomes Loaded with Liquiritigenin and Liquiritin (리퀴리티게닌과 리퀴리틴을 담지한 에토좀의 특성 및 경피 전달)

  • Im, Na Ri;Kim, Hae Soo;Lim, Ji Won;Kim, Kyeong Jin;Noh, Geun Young;Park, Soo Nam
    • Applied Chemistry for Engineering
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    • v.26 no.5
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    • pp.563-568
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    • 2015
  • Liquiritin and its aglycone, liquiritigenin are flavonoid found in licorice that show anti-oxidant and anti-aging properties. In this study, ethosomes loaded with hydrophobic liquiritigenin or liquiritin were prepared as a transdermal delivery system. The particle size, entrapment efficiency, and skin permeability of ethosomes were evaluated. Ethosome containing liquiritigenin was stable up to 2 mM and ethosome containing liquiritin was stable up to 0.75 mM concentration. The particle size of ethosomes containing 0.75 mM liquiritigenin and liquiritin was 143.85 and 158.90 nm, respectively and the entrapment efficiency was 47.51 and 54.61%, respectively. The entrapment efficiency was improved with increasing concentrations of drugs. Ethosomes loaded with liquiritigenin or liquiritin were superior in skin permeation ability compared to that of 20% ethanol solution and conventional liposomes. These results suggest that ethosomes containing 0.50 mM liquiritigenin or liquiritin are effective for the skin permeation and may be used as an antiaging and antioxidant ingredient in cosmetic formulation.

Characterization and Transdermal Delivery of Ethosomes Loaded with Eucommia ulmoides Extract (두충 추출물을 담지한 에토좀의 특성 및 경피 전달)

  • Gu, Hyun A;Kim, Hae Soo;Kim, Moon Jin;Yu, Eun Ryeong;Joe, Gijung;Jang, Jindong;Kim, Bohyeon;Park, Soo Nam
    • Applied Chemistry for Engineering
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    • v.24 no.6
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    • pp.639-644
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    • 2013
  • In this study, ethosomes loaded with Eucommia ulmoides extracts that have anti-inflammatory and anti-aging activities on the skin were prepared as cosmetic materials. The particle size, physical property, and entrapment efficiency of ethosomes to identify their stabilities during 4 weeks were measured. Ethosomes containing 0.01~0.05% E. ulmoides extracts did not show either precipitation or separation. The mean particle size of these ethosomes was 136.4 nm, and monodisperse. The particle size of ethosome containing 0.05% E. ulmoides extracts was 151.15 nm and the entrapment efficiency was 81.79%. Therefore, in vitro skin permeation experiment was performed with ethosome containing 0.05% E. ulmoides extracts that showed the high loading efficiency and stability during 4 weeks. The order of skin permeation of E. ulmoides extracts was ethosome (77.16%) > liposome (62.80%) > ethanolic solutoin (41.59%). These results suggest that ethosomes containing 0.05% E. ulmoides extracts are effective for the skin permeation and may be used as a cosmetic formulation containing plant extracts.

A Study on the Factors Affecting Entrapment Efficiency and Particle Size of Ethosomes (Ethosomes의 포집효율과 입자크기에 영향을 주는 인자에 관한 연구)

  • Jin, Byung Suk;Lee, Sang Mook;Lee, Kwang Hee
    • Applied Chemistry for Engineering
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    • v.17 no.2
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    • pp.138-143
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    • 2006
  • Ethosome is a liquid crystalline vesicle prepared by hydration of ethanol-dissolved lecithin with a solution containing hydrophilic components. Investigation of factors affecting the entrapment efficiency and particle size of ethosomes was carried out, because the high entrapment efficiency and small particle size are prerequisite in developing ethosomes as a drug delivery system. The variations of properties of ethosomes with constituent composition and preparation method were examined using a calcein as a hydrophilic marker. It was observed that the amount of ethanol and calcein solution, phosphatidyl choline content in lecithin, preparation temperature, stirring rate, and PBS addition method had a considerable effect on the properties of ethosome. Sonication treatment resulted in the reduction of entrapment efficiency of ethosome, which was due to the release of entrapped components in the vesicles by strong sonication vibration.

Skin Absorption and Physical Property of Ceramide-added Ethosome (세라마이드 함유 에토좀의 물성과 피부흡수)

  • Hyeon, Tong-Il;Yoon, Kyung-Sup
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.3
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    • pp.801-812
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    • 2021
  • In order to delivery biotin to skin, ethosomes containing both biotin and ceramide were researched by using high pressure homogenizer. Biotin was utilized as a drug and ceramide NP was utilized as a supporter of bilayer. The biotin was entrapped in aqueous core, while ceramide NP was packed in the bilayer of the ethosomes. Looking at the physical properties of vesicles containing ceramide NP, the sized was 80~130 nm, the polydispersity index was 0.09~0.16, and the zeta potential was -40~-49 mV. In vesicles without ceramide NP, the size was 124.80±1.46 nm, and the zeta potential and polydispersity index were -45.48±1.27 mV and 0.088±0.018, respectively. Therefore, the ethosome with ceramide NP has improved physical properties of vesicles compared to the ethosome without ceramide NP. Skin absorption rates of ethosomes with ceramide NP were 6.13~14.98%, while skin absorption rate of ethosome without ceramide NP was 7.08% at 12 h. In conclusion, ethosomes containing ceramide NP not only improved the skin absorption efficiency, but had also a positive effect on the stability of vesicles.

Coencapsulation of L-Ascorbic Acid and α-Tocopherol in Ethosomes and Their Properties (친수성 L-ascorbic acid와 소수성 α-tocopherol을 모두 포집하는 ethosome의 특성)

  • Lim, Yoon Mi;Jun, Yoon Kyung;Park, Seyeon;Jin, Byung Suk
    • Applied Chemistry for Engineering
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    • v.25 no.4
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    • pp.368-373
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    • 2014
  • Coencapsulation of hydrophilic L-ascorbic acid and hydrophobic ${\alpha}$-tocopherol in ethosome vesicles was attempted and their properties were investigated in this study. The size of vesicles decreased with increasing concentration of L-ascorbic acid solution encapsulated in ethosome. The vesicle size and encapsulation efficiency of ethosomes increased slightly when ${\alpha}$-tocopherol was added into the HPC-forming liquid crystalline membrane of ethosome. However, the vesicle size increased highly and the encapsulation efficiency decreased abruptly at mixing ratios above 25 wt% due to the formation of an imperfect liquid crystalline structure within a vesicle membrane. It was observed that antioxidant activity was maintained for 5 weeks at $40^{\circ}C$ when L-ascorbic acid and ${\alpha}$-tocopherol were coencapsulated in ethosome. The L-ascorbic acid in ethosome was stable compared to that in aqueous solution under UV radiation.

A Study for Preparation of Nano Ethosome Loaded with Resveratrol (레스베라트롤을 함유한 나노 에토좀 제조에 관한 연구)

  • Seo, Dong Hoan;Yoon, Jong Hyuk;Kim, Youn Joon;Byun, Sang Yo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.41 no.2
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    • pp.105-112
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    • 2015
  • Resveratrol is a natural polyphenol. It protects skin from skin injury, ultraviolet radiation and pathogenic attack. This study is to find the optimum condition for the preparation of ethosome loading amount of resveratrol in ethosome. Ethosomes were prepared by modified hydrated liquid crystal method. Investigation of factors affecting the entrapment efficiency and particle size of ethosomes was carried out. The particle size of ethosome were measured by particle analyzer. The loading efficiency of resveratrol in ethosome was measured by HPLC. The particle sizes were 111.2 ~ 112.8 nm and the loading efficiency of resveratrol was 81.25 ~ 88.75%. The optimum conditions for the preparation of ethosome was obtained from of lecithin : resveratrol : cholesterol : ethanol at a weight ratio of 2.0 : 0.08 : 0.05 : 20.0.

Cellular Protective Effect and Liposome Formulation for Enhanced Transdermal Delivery of Persicaria hydropiper L. Extract (여뀌 추출물의 세포 보호 작용과 피부 흡수 증진을 위한 리포좀 제형 연구)

  • Kim, Jung-Eun;Lee, Hye-Jin;Lim, Myoung-Sun;Park, Min-A;Park, Soo-Nam
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.38 no.1
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    • pp.15-31
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    • 2012
  • In our previous studies, the antioxidant, anti-aging, and antibacterial activities of Persicaria hydropipier L. extract, and the moisturizing effect of cream containing P. hydropipier extract were investigated. In this study, the cellular protective effects of P. hydropipier extract and isoquercitrin, main component from P. hydropipier in $^1O_2$-induced photohemolysis of human erythrocytes and ultraviolet B (UVB)-exposed HaCaT cells were investigated. Liposomes such as ethosome and elastic liposome for enhanced transdermal delivery were prepared. Size, loading efficiency, stability, and cumulative permeated amounts of ethosomes and elastic liposomes were evaluated. P. hydropipier extract and isoquercitrin showed more prominent cellular protective effect than (+)-${\alpha}$-tocopherol, known as lipid antioxidant at $5{\mu}g/mL$. P. hydropipier extract didn't show any characteristics of cytotoxicity at $50{\mu}g/mL$. When HaCaT cells were exposed to a single large dose ($400mJ/cm^2$) of UVB, the extract protected the cells against UVB radiation in a concentration dependent manner ($12.5{\sim}50{\mu}g/mL$). Cell viability of HaCaT cells exposed to UVB $400mJ/cm^2$ was increased by treatment with P. hydropipier extract or isoquercitrin from 36 % (cell viability of positve control groups) to 90 % (cell viability of P. hydropipier extract or isoquercitrin- treated groups). The size of 0.04 % P. hydropiper extract loaded ethosomes was 173.0 nm and the loading efficiency was 55.58 %. 0.04 % P. hydropiper extract loaded ethosomes were stable with as monodisperse particles for 1 week. The ethosome exhibited more skin permeability than general liposome and ethanol solution. The optimal ratio of lipid to surfactant ($Tego^{(R)}$ care 450) of 0.1 % P. hydropiper extract loaded elastic liposomes was observed to be 95 : 5. Vesicle size of 0.1 % P. hydropiper extract loaded elastic liposome was 176.5 nm. The deformability index of the elastic liposome was 16.4. The loading efficiency was 68.8 %. The elastic liposome containing P. hydropiper extract showed more skin permeability than liposome without surfactant ($Tego^{(R)}$ care 450).

Preparation and Characterization of EGCG Entrapped Ethosome (EGCG가 포집된 Ethosome의 제조와 특성조사)

  • Gwak, Hyo Jung;Jin, Byung Suk
    • Applied Chemistry for Engineering
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    • v.18 no.2
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    • pp.130-135
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    • 2007
  • Entrapment of (-)-epigallocatechin gallate (EGCG) into ethosome was carried out for improving its stability against decomposition. Solubility of EGCG was increased by the addition of ethanol into water, which enable ethosome to entrap appropriate amount of EGCG. It was observed that the EGCG solution concentration and constituent lipid composition had a considerable effect on the particle size and entrapment efficiency of ethosomes. The formation of liquid crystalline phase in ethosome was investigated by polarized optical microscopy. By comparing the stability of EGCG in solution and in ethosome exposed to UV or high temperature, we evaluated the EGCG stabilization effect through its entrapment in ethosome. Incorporation of tocopherol into ethosome retarded the decomposition of EGCG under UV.

Ethosome Formulation for Enhanced Transdermal Delivery of Artemisia princeps Pampanini Extracts (사자발쑥 추출물의 피부 흡수 증진을 위한 에토좀 제형에 관한 연구)

  • Yang, Hyun Gab;Kim, Hye Jin;Kim, Hae Soo;Park, Soo Nam
    • Applied Chemistry for Engineering
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    • v.24 no.2
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    • pp.190-195
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    • 2013
  • In our previous studies, the antioxidant, anti-aging, and antibacterial activities of Artemisia princeps Pampnini (A. princeps Pamp.) extract were reported. In this study, ethosome formulations for the enhanced transdermal delivery of A. princeps Pamp. extract were prepared. The particle size, loading efficiency and skin permeation of them were evaluated. The ethosome loaded with 0.06% ethyl acetate fraction of A. princeps Pamp. extract was more stable and maintained the constant particle size for 3 weeks after being prepared. The particle size of ethosome containing 0.06% ethyl acetate fraction was $287.05{\pm}0.25nm$ and the loading efficiency was $51.96{\pm}0.01%$. The ethosome formulation exhibited the greater enhancement of skin permeation than of general liposome and 20% ethanol solution in skin permeability experiments.