• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.43-51
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• 1995

The in vitro skin permeability of 16 drugs with a wide span of lipophilicity (log P ranging from -0,95 to 4.40) was evaluated with an ethanol/panasate 800 (tricaprylin, P-800) (40/60) lipophilic binary vehicle and an ethanol/water (60/40) hydrophilic binary vehicle with lauric acid, The skin permeability of the drugs was enhanced by the use of the ethanol/P-800 (40/60) binary vehicle or the ethanol/water (60/40) binary vehicle with lauric acid; permeation rate was increased and lag time' was decreased. The relationship between lipophilicity and skin permeation rate of the drugs showed parabolic shapes with their peaks at much greater hydrophilic range compared with other past references. In the in vivo skin absorption of theophylline using abdominal rat skin, the ethanol/P-800 (40/60)-7% (w/w) ethycellulose gel produced a good feature as a sustained-release preparation, and the ethanol/water (60/40)-3 % (w/w) HPMC gel with lauric acid showed the highest BA value. The results suggest that the lipophilicity of a drug is a main factor for prediction of the skin permeability of the drug and that the ethanol/P-800 (40/60) binary vehicle and ethanol/water (60/40) binary vehicle with lauric acid would be good candidates for clinical transdermal application of hydrophilic drugs.

• 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 (SkinEthic^TM 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.

• Biomolecules & Therapeutics
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• v.22 no.4
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• pp.321-327
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• 2014

Collagen pentapeptide (Lys-Thr-Thr-Lys-Ser, KTTKS) and its palmitoylated derivative (pal-KTTKS) have received a great deal of attention as cosmeceutical ingredients for their anti-wrinkle effects. The objective of this study was to evaluate stability and permeability of KTTKS and pal-KTTKS in hairless mouse skin. In this study, a liquid chromatography-tandem mass spectrometric method was developed for the quantification of pal-KTTKS, and used for stability and permeability studies. Stability studies were performed using skin extracts and homogenates. Both KTTKS and pal-KTTKS were rapidly degraded, but pal-KTTKS was more stable than KTTKS. When protease inhibitors were added, the stability of both compounds (KTTKS and pal-KTTKS) improved significantly. In the skin permeation study, neither KTTKS nor pal-KTTKS was detected in the receptor solution, which indicates that neither compound could permeate through the full-thickness hairless mouse skin in the experimental conditions of this study. While KTTKS was not detected in any of the skin layers (the stratum corneum, epidermis, and dermis), pal-KTTKS was observed in all skin layers: $4.2{\pm}0.7{\mu}g/cm^2$ in the stratum corneum, $2.8{\pm}0.5{\mu}g/cm^2$ in the epidermis, and $0.3{\pm}0.1{\mu}g/cm^2$ in the dermis. In conclusion, this study indicated that pal-KTTKS had greater stability and permeability than that of un-modified KTTKS, and may be a useful anti-wrinkle and anti-aging cosmeceutical agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.39 no.1
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• pp.39-46
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• 2013

Bicationic minerals such as calcium and magnesium are known to protect the skin barrier. The principal objective of this study was to evaluate the skin barrier protective effects of mineral water, which is composed of calcium, magnesium, manganese, and fluorine. UVB irradiation induces a destruction of tight junction (TJ) components. The TJ permeability barrier was also disrupted by UVB irradiation. We employed a skin equivalent model to assess the efficacy of mineral water in this regard. Mineral water maintained the structure of the skin equivalents following UVB irradiation. The results of the TJ permeability assay showed that mineral water helped to maintain the TJ permeability barrier after UVB irradiation in skin equivalent model. Mineral water supported the structure of TJ components and restored the occludin protein level in differentiated normal human keratinocytes after UVB irradiation. In conclusion, we found out the protective effect of mineral water against UVB irradiation.

• Food Science of Animal Resources
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• v.33 no.3
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• pp.356-362
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• 2013

We investigated the skin permeability and various biological activities of porcine homogenate of placenta (HP) with the highest protein contents (452.89 ${\mu}g/mg$). The content of protein in subcritical extract of HP (SPE) was decreased from the initial content of 452.9 ${\mu}g/mg$ to 262.7 ${\mu}g/mg$ at 3 h subcritical extract. The contents of amino type nitrogen (A-N) were sharply increased from 35.1 ${\mu}g/mg$ of initial content to 305.9 ${\mu}g/mg$ at 3 h subcritical extract. The HP showed a noticeable activity in terms of antioxidant capacity for ferric reducing antioxidant power (FRAP) assay and especially for 2,2'-Azinobis- (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) method. HP, SPE-0.5, SPE-2 and SPE-3 showed inhibitory effect on elastase activities with an $IC_{50}$ of 46.1, 42.9, 31.6 and 34.7 ${\mu}g/mL$, respectively. SPEs showed more significantly inhibitory effect than HP (p<0.05). The skin permeability of the SPEs was higher than that of the HP. SPE-3 showed highest skin permeation and the permeability was significantly higher than that of HP. SPE-2 also showed significantly higher permeation than HP after 4 h. As expected, increase of extraction time significantly increased skin permeability in the subcritical extract of HP (SPE). From these results, in terms of cost and source availability, porcine placenta extracted with subcritical extraction has advantages over untreated PE and have potential as a cosmetic ingredient.

• Journal of Environmental Health Sciences
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• v.30 no.2
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• pp.65-70
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• 2004

Hair is based upon the skin which enroll the body of high living animals and have multiple membrane structure. This study were used rats and carried out to find out the effects of commercial permanent wave products to skin which are composed of thioglycolic acid and bases. Results were as follows. Permanent wave penetrated to 3 hours later with steady state in skins and was not significant changeable after 20hr later. In case of neutralizer with thioglycolic acid lag time and permeability coefficient in healthy skin were 3.38hr and 0.96$\mu\textrm{g}$/$\textrm{cm}^2$/hr, in old skin were 3.14hr and 0.l28$\mu\textrm{g}$/$\textrm{cm}^2$/hr, and in wounded skin were 3.08hr and 0.157$\mu\textrm{g}$/$\textrm{cm}^2$/hr. In conclusion, lag time and permeability coefficient in old skin and wounded skin were faster than healthy skin. In vivo which was studied by general time and method of permanent wave. We found out that fine rinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin. Also, permanent wave drugs could induced rash and eruption at the skin by the naked eye.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.43 no.3
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• pp.189-194
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• 2017

Skin has a strong barrier function to protect the body from external harmful factors. This strong barrier function of the skin makes for any effective substance difficult to permeate through the skin. The purpose of this study was to evaluate skin permeability of the reduced particle size by non-invasive method. The particles were prepared by high-pressure emulsification. The niacinamide prepared in a high-pressure emulsification was absorbed 1.56 times higher than the control sample. In addition, it was found from the sixth layer of keratin that was removed by tape-stripping method. This was significantly deeper penetration. The whitening efficacy of the sample containing niacinamide was evaluated before and after 6 weeks of use. The skin color was significantly improved in both pigmented area and non-pigmented area. Through this study, it was possible to visually and quantitatively confirm the permeability confirm the permeability of the reduced particle sample into skin.

• Journal of Pharmaceutical Investigation
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• v.33 no.3
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• pp.163-169
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• 2003

In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

• Journal of Biomedical Engineering Research
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• v.39 no.1
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• pp.30-35
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• 2018

Conventional drug delivery methods mainly include subcutaneous injection and oral administration. Subcutaneous injection has the advantages of delivering the correct concentration, but it might cause pain and trauma to patients. Although oral administrations do not accompany pain as the subcutaneous injection, unexpected side effects may occur because they undergo digestion process and it is not easy for many drugs to be exposed to targeted sites with proper concentration. While dissolving microneedles have been extensively studied to overcome the limitations of conventional subcutaneous injection, the effects on microneedle shapes for drug release have not been fully explored. In this study, the characteristics of hyaluronic acid microneedles for cone and quadrangular pyramidal shapes were examined by the size, volume, contact surface area, skin permeability, and dissolution rate. As a result, the cone shapes of hyaluronic acid microneedles had high skin permeability, and the quadrangular pyramid of shapes hyaluronic acid microneedles showed a fast dissolution rate, given by the large contact area on the skin. Based on the results, we could confirm that the shape of a dissolving microneedles can affect skin permeability and the drug delivery rate.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.24 no.3
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• pp.38-44
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• 1998

The skin permeation and the skin primary irritation of two UV filters from caprylic capryl triglyceride (oil), oil in water (O/W) and water in oil (W/O) emulsions, were evaluated. We selected octyl moth-oxycinnamate (OMC) broadly used in cosmetics and polymeric sunscreen agent (PSA, average MW: 2,000) synthesized by the coupling reaction of 2-ethylhexyl 4-hydroxycinnamate with poly vinylbenzyl chloride, as model UV filters. For in vitro skin permeation experiments, Franz diffusion cells (effective diffusion area:1.766cm) and the excised skin of female hairless mouse aged 8 weeks were used. Oil or emulsion containing UV filters was applied in the donor compartment. The skin primary irritation was evaluated with fe-male guinea pigs (8-10 weeks,350-400 g). In oil and emulsions, the skin permeability and the skin primary irritation of PSA were lower than those of OMC. The skin permeability of UV filters was lower when they were in oil-in-water emulsion (OIW) than water-in-oil emulsion (W/O). We suggest that O/W system would be more useful when compared with W/O system, and PSA could be a good candidate for a future sunscreen agent for reducing the skin irritation.