• Journal of Pharmaceutical Investigation
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• v.36 no.6
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• pp.401-403
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• 2006

Topical preparations such as cream for Acyclovir(ACV), a potent anti-viral agent for the treatment of herpes simplex and herpes zoster, have been marketed in the world since 1993. However, the skin penetration rate of ACV from generic cream formulations sold in Europe has been found to be lower than the original $Zovirax^{\circledR}$ cream. In this study, we formulated ACV into a novel organogel system and compared the skin penetration characteristics with $Zovirax^{\circledR}$ cream. The rate and amount of skin penetration of ACV from the organogels were 6.3-fold greater than those obtained with $Zovirax^{\circledR}$ at an ACV concentration of 5%. The solubilizing effect of oil phase and anti-nucleation effect exhibited by sodium alginate contained in water phase are most likely attributed to enhanced ACV skin penetration property.

• Journal of the Korean Applied Science and Technology
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• v.24 no.2
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• pp.117-123
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• 2007

• Journal of Pharmaceutical Investigation
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• v.27 no.1
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• pp.65-69
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• 1997

To formulate the topical analgesic preparation of a new capsaicin derivative, DA-5018, a skin penetration evaluation system was established and the effect of composition of formulation on skin penetration using this system was evaluated, The effect of massage on hairless mouse skin penetration and inter-day variation of this effect were investigated using test formulations(cream). In massage group, compared with non-massage group, absolute penetration amount of DA-5018 increased and this experimental system was found to be reproducible, The effects of pH of water phase, ratio of oil/water and the concentration of active ingredient in cream on skin penetration were investigated. The permeation of DA-5018 from the cream increased with increasing pH of water phase to 9. But at pH 10, the permeation of DA-5018 decreased, because of the physical instability of the cream. The permeation of DA-5018 from the cream increased with increasing the ratio of oil/water of the cream. The increase of the content of DA-5018 to 0.3% increased the permeation of DA-5018, but at high concentration(1.0%), the permeation of DA5018 decreased, due to the instability of the cream.

• 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 Pharmaceutical Investigation
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• v.30 no.4
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• pp.273-278
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• 2000

Several topical preparations containing lidocaine, a widely used local anesthetic agent, have been developed and marketed recently for the treatment of premature ejaculation. In this study, microemulsion(ME)-based hydrogels containing lidocaine were prepared by dispersing ME to hydrogel bases such as Carbopol, sod. alginate, and sod. carboxymethylcellulose. Lidocaine-containing ME was thermodynamically stable over 6 months and had a diameter ranging from 10 to 100 nm. In vitro skin penetration of lidocaine from ME-based hydrogels followed apparent zero-order kinetics. ME-based hydrogel showed higher drug penetration during fifteen minutes after application than alcoholic hydrogel, reference preparation. Tail flick test in rat was introduced to compare in vivo local anesthetic effects of different hydrogels, and the results showed that ME-based hydrogels are superior to other hydrogels. In optical microscopy, recrystallization of lidocaine was observed within 5 min after application of reference hydrogel, but there was no change in ME-based hydrogels even after 30 minnute. These results indicated that ME-based hydrogels had some advantages in skin penetration, anesthetic effect and physical stability compared with alcoholic hydrogels. Finally it is possible to conclude that ME-based hydrogels containing lidocaine is a good topical drug delivery system for the treatment of premature ejaculation.

• 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 Pharmaceutical Investigation
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• v.31 no.4
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• pp.225-232
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• 2001

The present study was carried out to observe the effect of liposome dispersed gel formulation (Lipogel) on topical delivery of ascorbyl palmitate (AsP). Neutral and negatively charged MLV liposomes containing AsP were prepared with dimyristoylphosphadtidylcholine (DMPC) and dicetyl phosphate (DCP), and dispersed to poloxamer gel matrix. In the hydrolysis study in rat's skin homogenates, AsP hydrolyzed to ascorbic acid (AsA) according to the first-order kinetics with the rate constant of $2.46{\times}10^{-2}\;min^{-1}$. In the passive skin penetration study using Franz diffusion cell, lipogel systems exhibited the greater values in the flux $(J_s)$ and the amount penetrated $(Q_p)$ compared to control hydrogels containing diethyleneglycol monoethyl ether $(Transcutol^{\circledR})$ as a solubilizing agent and a penetration enhancer for AsP. The total amount penetrated $(Q_{Total})$, which is expressed as a summation of $Q_P\;and\;Q_L$, for lipogel system was about 1.4 times higher in average than that of control hydrogel. However the amount localized in the skin $(Q_L)$ was similar in both formulations. As a result, lipogel system enhanced the skin penetration of AsP, possibly due to the increase in local concentration of AsP by preferential adsorption of liposome to the skin and the enhancing effect of phospholipid in liposome composition. Moreover it was expected that the penetrated AsP would generate AsA during skin penetration by the skin esterase. In conclusion, lipogel formulation was considered as a good candidate for topical delivery of AsP.

• Biomolecules & Therapeutics
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• v.19 no.2
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• pp.231-236
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• 2011

The aim of this study was to investigate the effect of charge carrier lipid on the skin penetration, retention, and hair growth of topically applied finasteride-containing liposomes. Finasteride-containing liposomes were prepared by traditional thin film hydration method using Phospholipon$^{(R)}$ 85 G and cholesterol with or without charge carrier lipid (1,2 dimyristoyl-sn-glycero-3-phosphate or 1,2-dioleoyl-trimethylammonium-propane for anionic and cationic charge, respectively). Freshly prepared finasteride-containing liposome suspension was applied on the hairless mouse skin, and skin penetration and retention were measured using Keshary-Chien diffusion cell. Non-liposomal formulation (ethanol 10% solution containing 0.5 mg/ml of FNS) was also used as a control. The amount of finasteride in the diffusion cell and mouse skin was measured by HPLC. The hair growth was evaluated using depilated male C57BL/6N mice. Mean particle size of all finasteride-containing liposomes was less than a micron, and polydispersity index revealed size homogeneity. Skin penetration and retention studies showed that significantly less amount of finasteride was penetrated when applied as anionic liposome while more amount of the drug was retained. Specifically, in liposome prepared with 10% anionic charge carrier lipid, penetration was 12.99 ${\mu}g/cm^2$ while retention was 79.23 ${\mu}g/cm^2$ after 24 h of application. In hair growth study, finasteride-containing anionic liposomes showed moderate efficacy, but the efficacy was not found when applied as cationic liposomes. In conclusion, topical application of finasteride using anionic liposome formulation appears to be useful option for the treatment of androgenetic alopecia to avoid systemic side effects of the drug.

• Archives of Pharmacal Research
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• v.19 no.3
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• pp.183-190
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• 1996

There are a wide variety of semi-solid ointments used for healing the skin diseases, whose therapeutic and skin penetration abililties may greatly differ from one another depending on the compositions of ointment vehicles. A computer optimization technique was applied to obtain the optimum formula of o/w type ointment giving the in vitro maximum absorption rate through hairless rat skin membrane. Some of the formulations were selected to find out a relationship between skin penetration of ointment and its Theological characteristics. The experimental value of absorption rate obtained from the ointment by optimum formula agreed well with the theoretical value obtained from a polynomial regression analysis, Three kinds of ointments selected among 15 formulations were obtained with a concentric cylinder type rheometer (Model; Rheolab SM-HM Physica, Germany) at 20, 30, 40 and $50^{\circ}C$ for rheograms of rhelolgical properties of o/w type ointments. As the temperature was raised, all products showed a decrease in both shear stress and yield values. The higher skin penetration, the lower shear stress showed.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.41 no.3
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• pp.201-208
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• 2015

Organogels are semi-solid systems that consist of an apolar solvent as the liquid phase within a three-dimensional networked structure. In this study, we developed a stable and skin penetration-enhanced Lecithin Organogel (LO) containing genistein, which is one of the poorly soluble active ingredients in both polar and apolar phase. After screening of various components (type of gelators, organic and aqueous phase), hydrogenated lecithin (HL), sunflower oil (SO), dipropylene glycol (DPG), and polyethylene glycol (PEG) were mainly used in this formulation. Phase ternary diagram was employed for optimization of the composition in the LO. The formulated LO were evaluated for its organoleptic characteristics, stability, pH, rheology, phase transition temperatures, microscopic analysis and skin penetration. The optimized stable LO system can be utilized as an effective and stable cosmetic formulation that can carry poorly soluble active ingredients at high concentration for topical dermal delivery.