• 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 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.

• Biomolecules & Therapeutics
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• v.10 no.1
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• pp.1-6
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• 2002

The particle size of medicinal materials is an Important physical property that affects the phar-maceutical behaviors such as dissolution, chemical stability, and bioavailability of solid dosage forms. The size reduction of raw medicinal powder is needed to formulate insoluble drugs or slightly soluble medicines and to improve the pharmaceutical properties such as the solubility, the pharmaceutical mixing, and the dispersion. The objective of the present study is to evaluate physiological activity of amorphous and nano-particle prep-arations of insoluble drug, ursodeoxycholic acid (UDCA), which were made by three types of fine grinding mills. The change of physical properties of ground UDCA was conformed by Mastersiger microplus and X-ray diffraction. We have investigated hepatoprotective effects of the nano-particle preparations of UDCA by plan-etary mill, vibration rod mill and jet mill in $CCI_4$-induced oxidatively injured mouse liver. The results showed that nano-particle preparations of UDCA all decreased reactive oxygen sepecies generation and lipid peroxi-dation in $CCI_4$-induced oxidative stress mice. Among them, nano-particle preparations by vibration rod mill and jet mill showed more significantly hepatoprotective effects compared to intact UDCA and planetary mill-ground UDCA. These results suggest that ground UDCA with vibration rod mill and jet mill shows a high amorphous state and the improved dissolution.

• Journal of Pharmaceutical Investigation
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• v.37 no.1
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• pp.51-55
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• 2007

Solid lipid nanoparticles (SLNs) have been regarded to behave similar to the vegetable oil emulsions because emulsions of lipid melts are formed before lipid droplets being solidified to turn into SLNs. Compared to lipid emulsion, however, it has been more difficult to obtain stable SLNs and needs more extensive considerations on stabilizer and manufacturing process. In the present study, we tried to prepare phosphatidylcholine-based trymyristin (TM) SLNs using high pressure homogenization method and optimize the manufacturing variables such as homogenization pressure, number of homogenization cycles, cooling temperature, co-stabilizer and freeze-drying with cryoprotectants. Nano-sized TM particles could be Prepared using egg Phosphatidylcholine and pegylated phospholipids ($PEG_{2000}$PE) as stabilizers. Based on the optimization study, the dispersion was manufactured by homogenization under the pressure of 100 MPa for more than 5 cycles, and solidifying the intermediately formed lipid melt droplets by dipping in liquid nitrogen followed by thawing at room temperature. In addition, TM SLNs could be freeze-dried and then redispersed easily without significant particle size changes after freeze drying with 10% and 12.5% sucrose or trehalose. The TM SLNs established in this study can be used as delivery system for drugs and cosmetics.

• Journal of Pharmaceutical Investigation
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• v.40 no.6
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• pp.373-378
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• 2010

In order to develop a topical preparation which has a high occlusive property with skin moisturization, nano-structured lipid carrier (NLC) systems along with solid lipid nanoparticle (SLN) were designed. Various NLC dispersions were successfully formulated with Compritol 888 ATO as a solid lipid, Labrafil M 1944 CS as an oil, and Tween 80 as a surfactant. The increase of oil content (5 to 50%) led to the decrease in the occlusion factor in the order of SLN > NLC-5 > NLC-15 = NLC-30 > NLC-50. Particle size of lipid particulates was in the range of 100 to 160 nm. NLC-based carbogels were prepared by the employment of humectants such as urea, glycerin, and Tinocare GL to carbomer gel. NLC-30 gel formulations containing 4 or 8 % of lipid particles showed improved occlusive effect in vitro, compared to NLC-free gel base. Even though NLC-free gel base revealed comparable occlusion effect by itself, the occlusion factor of 4 % NLC-30 gel was about 2-fold higher than that of NLC-free gel base.

• 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.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.1
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• pp.15-23
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• 2008

This study is on encapsulation of a new whitening agent, LA-PEG using solid lipid nanoparticle(SLN) method, one of nanoparticle preparation method. Classical method has high capsulation efficiency for hydrophobic compounds but has demerit of low capsulation efficiency($2{\sim}3%$) for hydrophilic compounds. Purpose of this study is preparation of SLN that has higher skin penetration effect compared with general liposome, and also has higher encapsulation efficiency of hydrophilic compounds. For SLN preparation, coconut oil, macadamia oil, and jojoba oil were used. As a result, SLN preparation using coconut oil(include LA-PEG) has the most high encapsulation efficiency and also has the smallest average particle size(270 nm). SLN prepared with macadamia oil and 1% of Tween 60 has the largest particle size. Base made with coconut oil and 2% of Tween 60 showed the fastest release and base made with macadamia oil and 2% of Tween 20 showed the latest release.