• Title/Summary/Keyword: topical delivery

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Nanoemulsions and Nanoparticles Employed as Delivery Vehicles for Topical Active Ingredients to Enhance Stability and Efficacy

  • Arthur Georgalas
    • Proceedings of the SCSK Conference
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    • 2003.09b
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    • pp.307-307
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    • 2003
  • Strategies to make finished products more stable and efficacious can take advantage of formulation technologies- ingredients and techniques - to improve their delivery into the skin by both enhanced penetration and delayed release. Nanometer range particles and emulsion droplets can be formed with a selection of either silicone copolyol or conventional organic surfactants and dispersion shear rates sufficient to generate stable submicron droplets. By incorporating these into systems with biomimetic liquid crystalline gel networks in either simple or multiple phase emulsions the skin delivery can be enhanced as shown in tape stripping experiments. Such systems can stabilize labile actives, such as Vitamin C and retinol, and aid delivery. Laboratories in U.S and Europe investigated actives including green tea polyphenols, salicylic acid and methyl and benzyl nicotinate.

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Chitosan-Based Film of Tyrothricin for Enhanced Antimicrobial Activity against Common Skin Pathogens Including Staphylococcus aureus

  • Han, Sang Duk;Sung, Hyun Jung;Lee, Ga Hyeon;Jun, Joon-Ho;Son, Miwon;Kang, Myung Joo
    • Journal of Microbiology and Biotechnology
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    • v.26 no.5
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    • pp.953-958
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    • 2016
  • Chitosan-based film-forming gel is regarded as a promising vehicle for topical delivery of antimicrobial agents to skin wounds, since it protects from microbial infection and the cationic polymer itself possesses antibacterial activity. In this study, possible synergistic interaction against common skin pathogens between the cationic polymer and tyrothricin (TRC), a cyclic polypeptide antibiotic, was investigated, by determining the concentration to inhibit 90% of bacterial isolates (MIC). The addition of the polysaccharide to TRC dramatically reduced the MIC values of TRC by 1/33 and 1/4 against both methicillin-resistant and methicillin-susceptible Staphylococcus aureus, respectively. The synergism of TRC and chitosan combination against both strains was demonstrated by the checkerboard method, with a fractional inhibitory concentration index below 0.5. Moreover, co-treatment of TRC and chitosan exhibited antibacterial activity against Pseudomonas aeruginosa, due to the antibacterial activity of chitosan, whereas TRC itself did not inhibit the gram-negative bacterial growth. These findings suggested that the use of chitosan-based film for topical delivery of TRC could be an alternative to improve TRC antimicrobial activity against strains that are abundant in skin wounds.

Formulation Design and Evaluation of Niosome Containing Itraconazole for Dermal Delivery System (니오좀 시스템을 이용한 이트라코나졸 외용제의 제제 설계 및 평가)

  • Cho, Hye-Jung;Kyong, Kee-Yeol;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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    • pp.165-171
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    • 2005
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. However, it is difficult for itraconazloe to be delivered by topical system due to its poor aqueous solubility. First, niosomes containing drug were prepared with span 60, cholesterol. tocopherol and poloxamer 407 as vesicle forming agents in an effort to increase solubility of itraconazole. And then prepared niosomes were dispersed in O/W creams (containing xanthan gum, glycerin, vaseline, glyceryl monostearate and $Cerix^{\circledR}-5$) or gels (containing xanthan gum and poloxamer 407). Both creams and gels were evaluated with respect to their rheological properties, in vitro permeation through excised skin of hairless mouse. Creams or gels containing niosome showed pseudoplastic flow and hysteresis loop. For both creams and gels, viscosity was increased with increasing the content of glycerine or vaseline and the content of gel forming polymer, respectively. In creams, the permeability of drug to skin was decreased with increasing the viscosity of cream. The permeability of drug was affected by pH as well as viscosity of gel. In vitro permeation test results demonstrated that cream formulations showed better permeability than gels. In conclusion, these results suggest that creams formulation containing niosome can be useful for the topical delivery of intraconazole.

Enhanced Topical Delivery of Arbutin using Intense Pulsed Light (IPL) (Intense Pulsed Light(IPL)를 이용한 알부틴의 경피 흡수 개선)

  • Choi, Joon-Ho;Chung, Suk-Jae;Shim, Chang-Koo;Kim, Dae-Duk
    • Journal of Pharmaceutical Investigation
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    • v.39 no.2
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    • pp.121-125
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    • 2009
  • The objective of this study was to investigate the feasibility of applying the Intense Pulsed Light (IPL) as a tool to enhance the skin absorption of arbutin, a well-known skin-whitening agent. Arbutin solution or skin formulation was applied on the back of hairless mouse skin in vivo after IPL treatment, and then the skin deposition of arbutin was determined by HPLC. IPL treatment significantly increased the amount of arbutin in the skin after 6 hours when arbutin solution was applied 20 times. IPL also enhanced the skin deposition of arbutin when arbutin formulation was applied, although it was not significantly different. Significant increase of surface skin temperature was observed by IPL treatment, which might be a mechanism of the enhanced skin absorption of arbutin. These results suggest the feasibility of using IPL as a tool to increase the skin absorption of whitening agents, although further research needs to be conducted to understand its exact mechanism.

Enhanced Transdermal Delivery of Pranoprofen from the Bioadhesive Gels

  • Shin, Sang-Chul;Cho, Cheong-Weon
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.928-933
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    • 2006
  • Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at $32^{\circ}C$, $37^{\circ}C$ and $42^{\circ}C$ according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.

In-vitro Tests of Topical Skin Protectants using a Flow-Through Diffusion Cell System Containing Excised Hairless Mouse Skin (생체 피부조직을 이용한 피부보호제 in-vitro 시험평가)

  • Lee, Eun Young;Choi, Hoo Kyun;Kim, Sang Woong;Seo, Dong Sung;Joe, Hae Eun;Yu, Chi Ho;Kim, Chang Hwan;Cho, Young
    • Journal of the Korea Institute of Military Science and Technology
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    • v.25 no.4
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    • pp.434-442
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    • 2022
  • Highly toxic chemical warfare agents(CWA) could be used in chemical warfare and terrorism. The protection of skin is crucial for civilians and soldiers, because the primary routes of exposure to CWA are inhalation and skin absorption. Thus, topical skin protectants(TSP) have been studied and developed in many countries to complement protective equipments. In this study, in-vitro test procedure was optimized and established using a flow-through diffusion cell system containing excised hairless mouse skin in an attempt to assess the effectiveness of various TSP formulations against nerve agent simulants. In addition, the test results on the formulations including the ingredients used in SERPACWA(Skin Exposure Reduction Paste Against Chemical Warfare Agent) and IB-1(TSP of Israel) were included, indicating that the formulations with perfluorinated compounds were more effective than the glycerin-based formulations.

Safety Evaluation of Topical Valproate Application

  • Choi, Sun Young;Seop, Song Yi;Hyun, Moo Yeol;Yoo, Kwang Ho;Kim, Beom Joon;Kim, Myeung Nam;Cho, Jae-We
    • Toxicological Research
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    • v.29 no.2
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    • pp.87-90
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    • 2013
  • The potential role of topical valproate (VPA) in hair regrowth has been recently suggested. However, safety reports of VPA as a topical formulation are lacking. Therefore, in the present study, we investigated whether VPA causes skin irritation in humans. We first performed a cell viability test and showed that VPA did not exhibit toxicity toward HaCaT keratinocytes, fibroblasts, and RBL-3H mast cells. We then performed clinical patch test and skin irritation test through transdermal drug delivery with the help of microneedle rollers. No significant findings were obtained in the clinical patch test. In the skin irritation test, only 1 patient showed erythema at 1 hr, but the irritation reaction faded away within a few hours. Erythema and edema were not observed at 24 hr. We concluded that VPA has minimal potential to elicit skin irritation. Therefore, we consider that VPA can safely be applied to human skin.

Transdermal Permeation of $[{^3}H]Acyclovir$ Using Niosome (니오솜을 이용한 $[^{3}H]$아시클로버의 경피투과)

  • Park, Sae-Hae;Lee, Soon-Young;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.28 no.1
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    • pp.43-50
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    • 1998
  • Niosomes are vesicles formed from synthetic non-ionic surfactants, offering an alternative to chemically unstable and expensive liposomes as a drug carrier. Non-ionic surfactant and cholesterol mixture film leads to the formation of vesicular system by hydration with sonication method. The formation of niosome was ascertained by negative staining of TEM. The entrapment efficiency of niosomal suspension was gradually increased with increasing the ratio of cholesterol to surfactant. It was found that the niosome with 6 : 4 (polyoxyethylene 2-cetyl ether: cholesterol) ratio was more stable than those with other ratios. The topical application of acyclovir(ACV) in the treatment of herpes simplex virus type 1(HSV-1) skin disease has a long history. There are an increasing number of reports, however, in which topical ACV therapy is not as effective as oral administration. Lack of efficacy with topical ACV has been hypothesized to reflect the inadequate delivery of drug to the skin. We investigated the permeation of niosome containing $[^{3}H]ACV$ in hairless mouse skin using Franz diffusion cell model. Permeation coefficient(P) of aqueous ACV was $6.7{\times}10^{-4}\;(cm/hr)$ and that of ACV in niosome was $23.4{\times}10^{-4}\;(cm/hr)$, suggesting about 3.5 times increase in the transdermal permeation.

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Study on the Influence of Cubic Liquid Crystalline Phases of Monoolein on the Stability and Transdermal Delivery of Retinylpalmitate (Monoolein액정상이 Retinylpalmitate의 안정성과 경피전달에 미치는 효과에 관한 연구)

  • Lee, Kyoung-Gum;Kang, Myung-Joo;Choi, Young-Wook;Lee, Jae-Hwi
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.243-247
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    • 2007
  • Retinoids have many important and diverse functions and particularly, have been widely used as anti-aging agent and for the treatment of acne and psoriasis in cosmetics. However, retinoids have low stability against the air, light, water, oxygen and heat, thus, to stabilize the retinoids in formulations is very critical procedure. In this study, cubic liquid crystalline phase of monoolein was applied to stabilize the retinylpalmitate (RP) and to enhance the transdermal permeation. Cubic liquid crystalline phase significantly enhanced the stability of RP. After 15 days, the content of RP in the cubic formulation was 94.7% while the content of RP in ethanol solution was below 0.5% at room temperature. Although BHT containing crystalline phase showed the slightly increased stability of RP, there were no significant differences in RP stability between with or without antioxidants (ascorbic acid, ${\alpha}$-tocopherol, BHT, BHA) at $40^{\circ}C$. The skin retention of RP in crystalline formulations was approximately $5.3{\sim}6.4$ times greater than that of o/w cream formulation. Incorporation of RP into cubic liquid crystalline phase of monoolein effectively stabilized the RP and worked as excellent topical vehicle for RP. Liquid crystalline phase is considered to be suitable formulation for RP for topical delivery system as a stabilizer and permeation enhancing agent.