• 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.

• 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.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.33 no.4
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• pp.219-225
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• 2007

Bis-ethylhexyloxyphenolmethoxyphenyltrizine (BEMT) is one of the most widely used chemical UVA+UVB double absorbers in sunscreen products. But topical application of BEMT is restricted due to its defects in product. The purpose of this study is to adopt the sunscreen product of solid lipid nano-particles containing BEMT (BEMT-SLN). The particle diameters, the encapsulation efficiencies and the crystallization index (C.I.) are about 330nm, 93.3 % and the 4.3 %. As a result, in vitro penetration and release of BEMT were generally higher in O/W emulsion than the SLN formulation. However in vivo study, it was shown that the rate of release could be decreased by 80 % in the SLN formulation. The sun protection factor (SPF) of the SLN formulation increased by 100 % in the in vitro UV protection test. Therefore, SLN formulation potentiated the UV-blocking power of BEMT. This study suggest that SLN can be used for the encapsulation of BEMT.

• 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.

• 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 SkinEthic^TM 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.

• Applied Chemistry for Engineering
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• v.22 no.1
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• pp.91-97
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• 2011

The efficacies of anti-atopic preparations were investigated in hairless mice suffering from 2,4-dinitro-chlorobenzene (DNCB)-induced atopic dermatitis-like lesion. Solid lipid nanoparticle (SLN) containing ceramide and astaxanthin was prepared by a melt-homogenization method using Aminsoft-CT 12 (Cocoyl glutamate) as an emulsifier. And then, the SLNs were coated with silk fibroin (SF) by taking advantage of an electrostatic interaction between the surface of SLNs and SF. SLNs were included in lotion (FL) and cream (FC) types of preparations. Anti-atopic efficacies of the preparations were investigated in terms of appearance of skin surface, spleen index, serum IgE level, and serum cytokine level. SLN-containing preparations suppressed IgE production and IL-4 expression, but promoted $IFN-{\gamma}$ expression.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.31 no.2 s.51
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• pp.141-146
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• 2005

Unstable cosmetic active ingredients could rapidly break down in chemical and photochemical process. Therefore, it has become a very important issue to encapsulate active ingredient for the stabilization. 7-Dehydrocholesterol (7-DHC), a precursor of vitamin $D_3$, has been shown to increase levels of protein and mRNA for heat shock protein in normal human epidermal keratinocytes. However, topical dermal application of 7-DHC is restricted due to its poor solubility and chemical unstability. In this study, 7-DHC was incorporated into nano-emulsion (NE), solid lipid nano-particle (SLN), and chitosan coated solid lipid nano-particle (CASLN), respectively. In order to prepare NE and SLN dispersion, high-pressure homogenization at temperature above the melting point of lipid was used Hydrogenated lecithin and polysorbate 60 were used as stabilizer for NE and SLN. CASLN was prepared by high speed homogenizing after adding chitosan solution to the SLN dispersion and showed positively charged particle properties. Decomposition rate of 7-DHC in NE, SLN and CASLN was studied as a function of time at different temperature. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies were performed to characterize state of lipid modification. It appeared that CASLN is the most effective to stabilize 7-DHC and may be used for a useful topical dermal delivery system.

• Journal of Pharmaceutical Investigation
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• v.28 no.4
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• pp.249-255
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• 1998

Solid Lipid Nanoparticle(SLN), one of the colloidal carrier systems, has many advantages such as good biocompatibility, low toxicity and stability. In this paper, the effects of drug lipophilicity and surfactant on the drug loading capacity, particle size and drug release profile were examined. SLNs were prepared by homogenization of melted lipid dispersed in an aqueous surfactant solution. Ketoprofen, ibuprofen and pranoprofen were used as model drugs and tweens and poloxamers were tested for the effect of surfactant. Mean particle size of prepared SLNs was ranged from 100 to 150nm. The drug loading capacity was improved with the most lipophilic drug and low concentration of surfactant. Particle size and polydispersity of SLNs were changed according to the used lipid and surfactant. The rates of drug release were controlled by the loading drug and surfactant concentration. SLN system with effective drug loading efficiency and proper particle size for the intravenous or oral formulation can be prepared by selecting optimum drug and surfactant.

• Journal of Pharmaceutical Investigation
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• v.33 no.4
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• pp.319-322
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• 2003

Many studies have been attempted to overcome the problems of paclitaxel related to the extremely low aqueous solubility of paclitaxel and the unexpected side-effects caused by $Cremophor^{\circledR}$ EL in a commercial paclitaxel formulation, $Taxol^{\circledR}$. In order to formulate a new delivery system suitable for intravenous administration without toxic excipients, in this study, paclitaxel was incorporated into solid lipid nanoparticles (Px-SLN) by hot homogenization technique using a microfluidizer. Particle size and zeta potential were measured by a Zetasizer. In vitro drug release experiment was performed by a dialysis diffusion method. Each Px-SLN or $Taxol^{\circledR}$ was intravenously administered to the male Sprague-Dawley rats at a dose of 5 mg/kg as paclitaxel. Blood samples were deproteinated with acetonitrile and assayed for paclitaxel by the validated HPLC/MS/MS method. Mean particle size and zeta potential were measured as 72.1 nm (< Polydispersity 0.3) and -41.5 mV, respectively. The content of paclitaxel in SLN was 1.42 mg/ml and the drug loading efficiency was $71.2{\pm}4.3%$. The $AUC_t$ of Px-SLN was 3.4-fold greater than that of $Taxol^{\circledR}$. The Px-SLN might be a promising candidate for an alternative formulation for the parenteral delivery of paclitaxel.

• Journal of Pharmaceutical Investigation
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• v.35 no.1
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• pp.33-38
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• 2005

Recently increasing attention has been focused on solid lipid nanoparticles (SLN) as a parenteral drug carrier due to its numerous advantages that can come from both polymeric particle and fat emulsions, together with the possibility of controlled release and increasing drug stability. Lipophilic drugs such as paclitaxel, cyclosporin A, and all-trans retinoic acid have been successfully entrapped in SLN but the incorporation of hydrophilic drugs in SLN is very limited because of their very low affinity to the lipid. Therefore, as a new approach to improve the loading of hydrophilic drugs, a w/o/w emulsion technique has been developed. The primary objective of the current study was to improve the loading efficiency of a model hydrophilic drug, glycine (Log P = -3.44) into SLN. The proposed preparation process is as follows: A heated aqueous phase consisting of 0.1 ml of glycine solution in water (100 mg/ml), and poloxamer 188 (5 mg) were then added to a molten oil phase containing precirol (100 mg) and lecithin (5 mg). This mixture was dispersed by sonicator, leading to a w/o emulsion. A double emulsion (w/o/w) was formed after the addition of 2% poloxamer solution to the above dispersed system. After cooling the double emulsion, solid lipid nanosuspensions were successfully formed. The lipid nanoparticles had the mean particle size of 441.25 nm, and the average zeta potential of -20.98 mV. The drug loading efficiency was measured to be 8.54% and the drug loading amount was measured to be 0.92%. The w/o/w emulsion method showed an increased loading efficiency compared to conventional o/w emulsion method.