• Journal of Pharmaceutical Investigation
• /
• v.28 no.4
• /
• pp.249-255
• /
• 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
• /
• v.41 no.6
• /
• pp.381-386
• /
• 2011

Multi-drug resistance (MDR) has been known as a major hurdle in cancer chemotherapy. One of the most clinically significant causes of MDR was the efflux of anticancer agents mediated by p-glycoprotein (p-gp) over-expressed in MDR cancer cells. To overcome MDR, there have been several strategies such as co-administration with p-gp inhibitors and encapsulation of anticancer drugs into drug delivery systems. In the present study, curcumin was evaluated for its potential as p-gp inhibitor and MDR reversal activity when combined with paclitaxel incorporated into lipid nanoparticles (PTX/LN). Western blot assay showed curcumin did not modulate the level of p-gp expression in MCF-7/ADR which is a MDR variant of human breast cancer cell line, MCF-7, and over-expresses p-gp. However, curcumin inhibited p-gp-mediated efflux of calcein in a dose-dependent manner even though it showed lower activity compared to verapamil, a well-known p-gp inhibitor. Incorporation of paclitaxel into lipid nanoparticles partially recovered the anticancer activity of paclitaxel in MCF-7/ADR. The combined use of curcumin and PTX/LN exhibited further full reversal of MDR, suggesting susceptibility of PTX/LN to the efflux system. In conclusion, combined approach of using p-gp inhibitors and incorporation of the anticancer agents into nano-delivery systems would be an efficient strategy to overcome MDR.

• Proceedings of the PSK Conference
• /
• 2004.10a
• /
• pp.152.2-153
• /
• 2004

• Bulletin of the Korean Chemical Society
• /
• v.35 no.8
• /
• pp.2290-2294
• /
• 2014

For the present study, rhEGF was encapsulated into solid lipid nanoparticles (SLNs). The SLNs were prepared by the $W_1/O/W_2$ double emulsification method combined with the high pressure homogenization method and the physical properties such as particle size, zeta-potential and encapsulation efficiency were measured. The overall particle morphology of SLNs was investigated using a transmission electron microscopy (TEM). The percutaneous skin permeation and accumulation property of rhEGF was evaluated using Franz diffusion cell system along with confocal laser scanning microscopy (CLSM). The mean particle size of rhEGF-loaded SLNs was $104.00{\pm}3.99nm$ and the zeta-potential value was in the range of -$36.99{\pm}0.54mV$, providing a good colloidal stability. The TEM image revealed a spherical shape of SLNs about 100 nm and the encapsulation efficiency was $18.47{\pm}0.22%$. The skin accumulation of rhEGF was enhanced by SLNs. CLSM image analysis provided that the rhEGF rat skin accumulation is facilitated by an entry of SLNs through the pores of skin.

• Journal of Pharmaceutical Investigation
• /
• v.26 no.4
• /
• pp.245-256
• /
• 1996

Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage; low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile, SLN as a new drug delivery system is known to entrap rugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods, ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about $0.1\;{\mu}m$, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative, $-9{\sim}-13mV$ and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN. $T_{max}$ was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.

• Journal of the Korean Applied Science and Technology
• /
• v.38 no.4
• /
• pp.915-921
• /
• 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.

• 한국생물공학회:학술대회논문집
• /
• 2003.10a
• /
• pp.655-659
• /
• 2003

Solid lipid nanoparticle (SLN) system has been attracted increasing attention during last few years as a potential drug delivery carrier However, the SLN have disadvantage of low encapsulation efficiency for hydrophilic drug. In this study, for increase it's encapsulation efficiency, we prepared the $Eudragit^{\circledR}$ L100-55 (eudragit) coated SLN(E-SLN) based on solvent evaporation method and melt dispersion technique, and analyzed their physicochemical properties in terms of particle size, morphology, and encapsulation efficiency. As a result, they have a ${\pm}150$ nm particle size, spherical shape, and $10^{\sim}25$ % loading efficiency. SLN consists of coconut oil as core material, ascorbic acid and okyong-san as hydrophilic drug.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.30 no.2
• /
• pp.201-205
• /
• 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.