• Macromolecular Research
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• v.16 no.8
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• pp.682-685
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• 2008

The aim of this work was to develop and evaluate solid lipid nanoparticles (SLN) containing all-trans-retinoic acid (ATRA) for topical delivery. SLN composed of coconut oil and curdlan improved the suspension instability of ATRA in aqueous solution. The photodegradation of ATRA by light was reduced by incorporation in SLN. The loading efficiency of ATRA in SLN was higher than 95% (w/w). The amounts of ATRA released from SLN at $4^{\circ}C$ and at $37^{\circ}C$ were less than 15% and more than 60% (w/w) for 96 h, respectively. The ATRA-loaded SLN can be used as a potential carrier for topical delivery.

• Journal of Pharmaceutical Investigation
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• v.35 no.4
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• pp.233-241
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• 2005

Ursolic acid (UA), a bioactive triterpene acid, has been known to increase collagen content in human skin in addition to other actions such as anti-inflammatory, skin-tumor prevention and anti-invasion. However, it is poorly soluble in water. Therefore, we firstly prepared microemulsion system with benzyl alcohol, ethanol and Cremophor EL, RH 40 and Brij 35 as surfactant in order to increase solubility of UA and then prepared microemulsion was dispersed in o/w cream base for the topical delivery of UA in an effort to improve anti-wrinkle effect. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using benzyl alcohol as an oil, Cremophor EL, RH 40 and Brij 35 as a surfactant. The droplet size of microemulsions was characterized by dynamic light scattering. The accumulation of VA in the skin from topical cream was evaluated in vitro using hairless mouse skins. The mean droplet size was $26.8{\pm}6.6$ nm for microemulsions II with Cremophor EL. All UA creams showed pseudoplastic flow and hysterisis loop in their rheogram, depending on the type of materials added in topical creams. The in vitro accumulation data demonstrated the UA topical cream prepared with the combination of Poloxamer 407 and Xanthan gum as a copolymer showed higher accumulation percentage than those prepared with either Poloxamer 407 or Xanthan gum. These results suggest that UA topical cream using microemulsion systems may be promising for the topical delivery of UA.

• Journal of Pharmaceutical Investigation
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• v.36 no.2
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• pp.103-107
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• 2006

In order to develop hydroquinone analogues for topical delivery, a structure-activity relationship study has been performed. A series of 2-substituted hydroquinones were tested for their ability to inhibit mushroom tyrosinase, alter melanin release and exert cytotoxicity in B6-F10 melanocytes. The electronic property of the 2-substituents did not affect the tyrosinase inhibition nor melanocyte toxicity. However, lipophilicity did affect to some degree the tyrosinase inhibition. The discrepancy in the structure-activity relationship may be due to the poor aqueous solubility of select analogues. Compounds with steric bulk at the 2-position seems to be less soluble, not enabling the analogue to interact effectively with the tyrosinase enzyme. Among the analogues tested, 2-isopropyl hydroquinone seems to be the most promising candidate for topical delivery, being the least toxic analogue with moderate melanin release inhibition.

• Medical Lasers
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• v.10 no.3
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• pp.181-184
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• 2021

Scars can cause great psychological stress among patients. Currently, there are numerous topical agents, laser and surgical treatments available for skin rejuvenation and scar minimization. Laser-assisted drug delivery (LADD) is a treatment method that increases drug delivery by stimulating the skin physically and chemically to enhance the penetration of topical agents. This is one of the areas of great interest in the treatment of various skin diseases in addition to its use for cosmetic purposes. In particular, LADD is relatively non-invasive and has advantages in terms of accessibility and stability. Poly-L-lactic acid (PLLA) is a collagen stimulator known to gradually restore skin volume by inducing inflammation and fibroplasia. Herein, we report a case of treatment of an atrophic scar with fractional carbon dioxide laser-assisted PLLA delivery.

• Biomolecules & Therapeutics
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• v.17 no.3
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• pp.305-310
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• 2009

The aim of this study was to determine if a meloxicam hydrogel could be administered in vivo via phonophoretic transdermal delivery using pulsed ultrasound by examining its anti-hyperalgesic effects in a rat carrageenan inflammation model. Carrageenan (1%) was injected into the plantar surface of the right hindpaw, and meloxicam hydrogel was administered via phonophoretic transdermal delivery. Changes in the mechanical and thermal hyperalgesia, as well as swelling, showed that phonophoretic delivery of meloxicam exhibited significantly better anti-hyperalgesic and anti-inflammatory effects than pulsed ultrasound. Topical and systemic application of meloxicam hydrogel using phonophoresis showed similar anti-hyperalgesic effects. These findings suggest that the transdermal administration of a meloxicam hydrogel using phonophoresis by pulsed ultrasound might be useful for treating acute inflammation.

• Journal of Pharmaceutical Investigation
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• v.37 no.3
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• pp.167-171
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• 2007

Itraconazole is one of the most potent antifungal agents available in the market today. However, the low bioavailability due to its poor-water solubility calls for an alternative formulation to the current oral type. A topical itra-conazole-containing formulation may be of use for several reasons including the opportunity to reduce adverse events and generate high local tissue levels, more rapid drug delivery, and lower systemic exposure. The purpose of the present study was to investigate the vehicles for topical skin delivery of itraconazole. The effect of formulations on the hairless mouse skin permeation and deposition of itraconazole was determined using Franz diffusion cells at $37^{\circ}C$. Benzyl alcohol in micro-emulsion significantly increased the solubility of itraconazole, thereby increasing the skin permeation rate. However, lipo-some formulation showed the lowest solubility and permeation rate of itraconazole. Although the solubility of itraconazole in hydrogel formulation was lower than that in microemulsion, skin permeation rate was significantly higher probably due to its adhesive property. Therefore, microemulsion-based hydrogel formulation is expected to synergistically increase the skin permeation rate and skin deposition of itraconazole.

• Journal of Ginseng Research
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• v.42 no.4
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• pp.512-523
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• 2018

Background: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD. Methods: MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model. Results: A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient $r^2=0.929-0.947$). Conclusion: The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD.

• Journal of Pharmaceutical Investigation
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• v.15 no.4
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• pp.230-230
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• 1985

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.295.2-295.2
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• 2003

Lipid nanodispersion (LN) composed of biocompatible lipids and surfactants is an alternative parenteral drug delivery system especially for lipophilic drugs. It has been studied for versatile applications such as oral, parenteral, topical, ocular, vaccine, and peptide drug delivery. The purpose of this study was to produce a novel LN system for intravenous injection using the high pressure homogenization. (omitted)

• 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$^{(R)}$.