• Title/Summary/Keyword: lipid penetration

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Effect of Charge Carrier Lipid on Skin Penetration, Retention, and Hair Growth of Topically Applied Finasteride-Containing Liposomes

  • Lee, Sang-Im;Nagayya-Sriraman, Santhosh-Kumar;Shanmugam, Srinivasan;Baskaran, Rengarajan;Yong, Chul-Soon;Yoon, Sang-Kwon;Choi, Han-Gon;Yoo, Bong-Kyu
    • Biomolecules & Therapeutics
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    • v.19 no.2
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    • pp.231-236
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    • 2011
  • The aim of this study was to investigate the effect of charge carrier lipid on the skin penetration, retention, and hair growth of topically applied finasteride-containing liposomes. Finasteride-containing liposomes were prepared by traditional thin film hydration method using Phospholipon$^{(R)}$ 85 G and cholesterol with or without charge carrier lipid (1,2 dimyristoyl-sn-glycero-3-phosphate or 1,2-dioleoyl-trimethylammonium-propane for anionic and cationic charge, respectively). Freshly prepared finasteride-containing liposome suspension was applied on the hairless mouse skin, and skin penetration and retention were measured using Keshary-Chien diffusion cell. Non-liposomal formulation (ethanol 10% solution containing 0.5 mg/ml of FNS) was also used as a control. The amount of finasteride in the diffusion cell and mouse skin was measured by HPLC. The hair growth was evaluated using depilated male C57BL/6N mice. Mean particle size of all finasteride-containing liposomes was less than a micron, and polydispersity index revealed size homogeneity. Skin penetration and retention studies showed that significantly less amount of finasteride was penetrated when applied as anionic liposome while more amount of the drug was retained. Specifically, in liposome prepared with 10% anionic charge carrier lipid, penetration was 12.99 ${\mu}g/cm^2$ while retention was 79.23 ${\mu}g/cm^2$ after 24 h of application. In hair growth study, finasteride-containing anionic liposomes showed moderate efficacy, but the efficacy was not found when applied as cationic liposomes. In conclusion, topical application of finasteride using anionic liposome formulation appears to be useful option for the treatment of androgenetic alopecia to avoid systemic side effects of the drug.

Investigation of Tacrolimus Loaded Nanostructured Lipid Carriers for Topical Drug Delivery

  • Nam, So-Hee;Ji, Xu Ying;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.956-960
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    • 2011
  • The objective of this investigation was to develop nanostructured lipid carriers (NLCs) of tacrolimus by the hot homogenization technique by sonication. NLCs are commonly prepared by emulsification and lyophilization. The feasibility of fabricating tacrolimus-loaded NLCs was successfully demonstrated in this study. The developed NLCs were characterized in terms of their particle size, zeta potential, entrapment efficiency (EE) of tacrolimus, and morphology. Studies were conducted to evaluate the effectiveness of the NLCs in improving the penetration rate through hairless mouse skin. Tacrolimus-loaded NLCs were found to have an average size of $123.4{\pm}0.3\;nm$, a zeta potential of $-24.3{\pm}6.2\;mV$, and an EE of 50%. In vitro penetration tests revealed that the tacrolimus-loaded NLCs have a penetration rate that is 1.64 times that of the commercial tacrolimus ointment, Protopic$^{(R)}$.

Lipid Penetration Characteristics of Carrageenan-Based Edible Films (카라기난 필름 및 카라기난 코팅 종이포장지의 유지투과 특성)

  • Rhim, Jong-Whan;Hwang, Keum-Tack;Park, Hyun-Jin;Kang, Seong-Gook;Jung, Soon-Teck
    • Korean Journal of Food Science and Technology
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    • v.30 no.2
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    • pp.379-384
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    • 1998
  • Biodegradable carrageenan films and carrageenan-coated papers were developed and their characteristics of lipid permeation was investigated for possible substitution of PE-coated papers used in packaging of oily or greasy foods. Both carrageenan coated papers and free carrageenan films were highly resistant to lipid penetration. Among the carrageenans tested, ${\kappa}-carrageenan$ film showed the most resistant followed by ${\lambda}-$ and i-carrageenan films. The resistance to lipid increased as the thickness of ${\kappa}-carrageenan$ layer increased. Carrageenan coated papers with $4\;and\;5\;kg/ream\;(278m^2)$ showed the lipid resistance comparable to that of the PE-coated paper. Free films also showed the same trends of the lipid resistance as the carrageenan coated papers, but the degree of lipid resistance was approximately ten times higher than that of carrageenan coated paper. Degree of lipid penetration of carrageenan films and carrageenan-coated papers increased exponentially against time. ${\kappa}-carrageenan$ coated papers over 4 kg/ream showed to have an adequate lipid barrier property for being utilized for packaging greasy food products.

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Design and Characterization of Ascorbyl Glucoside loaded Solid Lipid Nanoparticles to improve skin penetration (피부 투과 개선을 위한 고형지질나노입자내 Ascorbyl glucoside 봉입 설계 및 특성화)

  • Yeo, Sooho
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.3
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    • pp.662-668
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    • 2021
  • The aim of the present study was to design ascorbyl glucoside (AG) loaded solid lipid nanoparticles (SLNs) to improve skin penetration of AG. AG loaded SLNs were prepared using double emulsion method. The prepared AG loaded SLNs investigated particle characteristics (particle size, polydispersity index, zeta potential, loading capacity). Skin penetration study was carried out using SkinEthic RHE as one of the reconstructed human epidermis models. The mean particle size and zeta potential of SLNs were 172.65 - 347.19 nm and -22.90 - -41.20 mV, respectively. The loading capacity of AG loaded SLNs demonstrated that loading efficiency and loading amount were ranged from 44.18% to 57.77% and 12.83% to 16.15%, respectively. The results of penetration showed that all SLNs enhanced the skin penetration of AG and the amount of AG from SLNs were approximately 3.7 - 7.4 times higher than that from AG solution. Therefore, AG loaded SLN might be a promising topical drug delivery system.

The penetration site of local anesthetics into liposomal membrane

  • Han, Suk-Kyu;Bae, Song-Ja;Il-Yun;Kim, Nam-Hong
    • Archives of Pharmacal Research
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    • v.8 no.4
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    • pp.205-211
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    • 1985
  • The distribution of local anesthetics between the hydrocarbone interior and surface area of the lipid bilayer of liposomal membrane was calculated employeg fluorescence probe technique. The quenching of fluorescence probe technique. The quenching of fluorescence probe technique. The quenching of fluorescence of 12-(9-anthroyl) stearic acid and N-octadecyl naphthyl-2-amini-6-sulfonic acid by the local anesthetics in liposomal system was used to calculate the distribution. The Stern-Volmer equation was modified and employed for this calculation. The results showed that procaine hydrocloride and benzocaine were mainly distributed on the surface area of the lipid bilayer of the liposoal membrane, while tetracaine hydrochloride penetrated effectively into the hydrocarbon interior and showed even distribution in the lipid bilayer.

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A Study on the Design of Solid Lipid Nanoparticles for enhanced Skin Penetration of Pantothenic Acid (Pantothenic acid의 피부 투과 개선을 위한 고형지질나노입자설계 연구)

  • Yeo, Sooho
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.4
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    • pp.915-921
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    • 2021
  • In this study, we designed pantothenic acid (PA) loaded solid lipid nanoparticles (SLNs) for enhanced skin penetration of PA that is used for moisturizing agent in cosmetics with hydrophilic property. SLNs were prepared using various lipids and surfactants. PA loaded SLNs were fabricated using double emulsion method. The fabricated PA loaded SLNs assessed particle size, polydispersity index, zeta potential, loading capacity. Skin penetration study was conducted using artificial skin tissue originated from human epidermis as one of the reconstructed human epidermis models. The mean particle size and zeta potential of SLNs ranged from 192.15 nm to 369.87 nm and -21.39 mV to -40.55 mV, respectively. The loading efficiency and loading amount of PA loaded SLNs were ranged from 44.36% to 57.16% and 12.60% to 16.36%, respectively. The results of penetration demonstrated that all SLNs improved PA skin penetration. In addition, the amount of PA from SLNs were approximately 3.8 - 8.8 times higher than that from PA solution. Therefore, the fabricated SLNs demonstrated the enhancment of skin penetration of PA. Particularly, the SLN, which used glyceryl behenate and Span 60, showed optimal skin penetration of PA.

A Study on the Design of Stearic Acid-Based Solid Lipid Nanoparticles for the Improvement of Artificial Skin Tissue Transmittance of Serine (Serine 의 인공피부조직 투과 개선을 위한 Stearic Acid 기반 고형지질나노입자의 설계 연구)

  • Yeo, Sooho
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.47 no.2
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    • pp.179-184
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    • 2021
  • Stratum corneum known as a skin barrier, which maintains water in skin, is the outer layer of the skin. Natural moisturizing factors (NMF) are one of the constituents in stratum corneum and amino acids are the highest components among NMF. In this study, we designed stearic acid-based solid lipid nanoparticles (SLNs) for improved skin penetration of serine (Ser). Ser-capsulated SLN was manufactured by double-melting emulsification method. The mean particle size and zeta potential of SLNs were 256.30 ~ 416.93 nm and -17.60 ~ -35.27 mV, respectively. The higher the degree of hydrophobicity or hydrophilicity of emulsifiers, the smaller the particle size and the higher the stability and capsulation rate. In addition, skin penetration was conducted using SkinEthicTM RHE which is one of the reconstructed human epidermis models. The results of Ser penetration demonstrated that all SLNs enhanced than serine solution. The amount of enhanced Ser penetration from SLNs were approximately 4.1 ~ 6.2 times higher than that from Ser solution. Therefore, Ser-loaded SLN might be a promising drug delivery system for moisturizing formulation in cosmeceutical.

Lamellar-bio nano-hybrid; The Study for Stability of Catechin (Green Tea: EGCG) Using 3-Dimensional Liposome (라멜라-바이오 나노하이브리드: 3 Dimension-liposome을 이용한 카테킨(EGCG)에 안정화에 대한 연구)

  • Hong Geun, Ji;Jung Sik, Choi;Hee Suk, Kwon;Sung Rack, Cho;Byoung Kee, Jo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.2
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    • pp.201-205
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    • 2004
  • In these several years, as many people have been attracted by the functional cosmetics, there are a lot of study to enhance the stability of active ingredients for light, heat, oxygen, etc. in the academic and industrial field. Especially, catechin is well known as strong anti-oxidant, anti-inflammatory and reducing agent for oxidative stress but it is very unstable for light, heat, oxygen. etc. In this study, the stability and skin penetration of catechin are improved by 3-dimensional method. As I-dimension, porous silica is prepared using sol-gel method, and then catechin is adsorbed in pores of silica. As 2-dimension, solid lipid nanoparticles (SLN) are obtained using non-phospholipid vesicles. Finally 3-dimension is completion through lamellar phase self-organization that combines SLN catechin with skin lipid matrix. We used laser light scattering system, cyro-SEM, chromameter, HPLC and image analyzer to analyze our 3-dimentional systems. According to chromameter date, the color stability of 3-dimensional catechin is enhanced by 5-10 times compared with general liposome systems. We also confirmed through HPLC analysis that 3-dimensional catechin is more long lasting. The effect of skin penetration and wrinkle reduction are improved, too.

Effects of $\beta$-Mercaptoethanol on Lipid Peroxidation and Fertilization Ability In Vitro by Xanthine-Xanthine Oxidase System in Pig

  • Sa S.J.;H.T. Cheong;B.K. Yang;Kim, C.I.;Park, C.K.
    • Proceedings of the KSAR Conference
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    • 2002.06a
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    • pp.74-74
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    • 2002
  • This study was undertaken to evaluate the effects of β-mercaptoethanol on lipid peroxidation and fertilization ability in vitro by xanthine (X)-xanthine oxidase (XO) system in boar spermatozoa frozen-thawed. When spermatozoa were inseminated in medium with X and/or XO, the penetration rates in all conditions were higher in medium with that than without β-mercaptoethanol. However, significant differences were not observed between medium with and without β-mercaptoethanol. The lipid peroxidation of sperm was evaluated on the basis of malondialdehyde (MDA) production. (omitted)

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Design of Solid Lipid Nanoparticles to Improve Penetration of Niacinamide through Artificial Skin Tissue (나이아신아마이드의 인공피부조직 투과 개선을 위한 고형지질나노입자의 설계 연구)

  • Yeo, Sooho
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.47 no.2
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    • pp.133-138
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    • 2021
  • In this study, Niacinamide (NI) was loaded into solid lipid nanoparticles (SLNs) and skin permeability was evaluated to improve skin permeability of NI, which was a skin whitening substance. NI was able to effectively load within SLN with a double-melting emulsification method, producing stable particles with average particle sizes of 263.30 to 436.93 nm and a zeta potential of -34.77 to -57.60 mV. Artificial skin tissue (SkinEthicTM RHE) derived from skin keratinocytes derived from human epidermal tissue was used for the skin permeation study of NI. Skin transmittance and deposition experiments of NI confirmed that all SLN formulations improved skin transmittance and deposition rates of NI, approximately 5.4 ~ 7.6 and 9.5 ~ 20.8 improvement over SLN applications. Therefore, SLN manufactured in this study have shown sufficient results to improve the skin permeability of the functional whitening substance, NI.