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Enhancement of skin permeation of vitamin C using vibrating microneedles
이초아,백종섭,곽동기,이혜진,박진호,조정원 대한임상약리학회 2017 Translational and Clinical Pharmacology Vol.25 No.1
This study was performed to evaluate the use of vibrating microneedles for the transdermal deliveryof vitamin C. The microneedles were designed to vibrate at three levels of intensity. In vitro permeationby vitamin C was evaluated according to the specific conditions such as vibration intensity(levels 1, 2 and 3), application time (1, 3, 5, 7 and 10 min), and application power (500, 700 and1,000 g). The highest permeation of vitamin C was observed at level 3 of vibration intensity, 5 minof application, and 1,000 g of application power. Vitamin C gel showed no cytotoxic effect againstPam212 cells or skin irritation effects. A pharmacokinetic study of the gel in rats was conductedunder optimized conditions. The AUC0-∞ and Cmax increased 1.35-fold and 1.44-fold, respectively,compared with those after vitamin C gel without application with vibrating microneedles. The presentstudy suggests that vibrating microneedles can be used to facilitate the skin permeability of vitaminC under optimal conditions.
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이초아,이경록,조정원 충남대학교 약학대학 의약품개발연구소 2014 藥學論文集 Vol.29 No.-
Skin whitening products are commercially available for cosmetic purposes in order to obtain a lighter skin appearance. They are also utilized for clinical treatment of pigmentary disorders such as melasma or postinflammatory hyperpigmentation. Whitening agents act at diverse levels of melanin synthesis in the skin. Many of them are known as competitive inhibitors of tyrosinase, the key enzyme in melanogenesis. Others inhibit the transformation of this activated enzyme or the transport of melanosomes from melanocytes to surrounding keratinocytes. To avoid systemic absorption, whitening agent is need to create optimal formulation such as liposome, microemulsion, solid lipid nanoparticles (SLN) and NLC (Nanostructure liquid crystal) as well as patch. Functional ingredients and innovative delivery systems are driving the new product development in the field of cosmetics. In this review we present an overview of whitening products that may decrease skin pigmentation by their interference with the pigmentary processes and may formulate cosmetic delivery systems possessing potential as smarter carrier systems.
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Preparation and characterization of mucoadhesive enteric-coating ginsenoside-loaded microparticles
백종섭,연원기,이초아,황성주,박정숙,김동출,조정원 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.5
Ginsenoside saponins are phytochemicallyextracted from red ginseng and have been regarded as theprincipal components manifesting the pharmacologicactivities. Saponins are very soluble in water but poorlyabsorbed when orally administrated. Moreover, they havesome disadvantages including the decomposition in acidmedium. The aim of this study was to develop oral formulationof ginsenosides composed of enteric-coatingpolymer and mucoadhesive polymer considering the lowstability in acid medium and the low permeability of saponins. Ginsenoside-loaded microparticles were prepared byspray dryer. The influences of various parameters such asthe ratio of saponin to polymer, feed concentration, feedrate, inlet/outlet temperature and additional excipientsduring spray-drying were investigated. In vitro releaseprofile of ginsenoside-loaded microparticles using additionalexcipients, ginsenoside saponin Rg1 or Rb1 showedan 18 or 13 % release in pH 1.2 when ethyl cellulose wasadded. Also, ginsenoside-loaded microparticles exhibitedmucoadhesive properties in the presence of chitosan. Theapplication of these polymers is being considered as thepotential strategy for improvement of bioavailability insaponin delivery, orally.
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The effect of Eudragit type on BSA-loaded PLGA nanoparticles
박민호,백종섭,이초아,김동철,조정원 한국약제학회 2014 Journal of Pharmaceutical Investigation Vol.44 No.5
Poly(D,L-lactide-co-glycolide) nanoparticle (PLGANP) have been broadly studied as a carrier for drugdelivery system of peptides and proteins. However, negativesurface charge of PLGA NP using only PLGAdecreases bioavailability under oral administration. In thisstudy, novel carriers for oral delivery system through anadditional bioadhesive polymer, Eudragit was introduced. Our purpose is to prepare PLGA NP using bovine serumalbumin (BSA) as a model drug and Eudragit and evaluatetheir physiochemical characteristics, eventually expand topeptide and protein drug such as insulin or exenatide. Inthis study, PLGA NP were spherical and the size wasaround 400–500 nm. The encapsulation efficiency (EE) ofPLGA NP when prepared with only PLGA was the highest,approximately 95.3 %. The polydispersity index valueswere low approximately 0.1, which meant their size wasregular. In mucoadhesion test, we knew PLGA NP preparedby using Eudragit RS or Eudragit RL had a highaffinity to mucin particles through zeta-potential change ofmucin particle to cover their surface. Also, PLGA NP didnot show cytotoxicity against Caco-2 cells. Especially,BSA-loaded PLGA NP using Eudragit RS 100 preparedhad high EE, low polydispersity index, spherical shapehaving a smooth surface, sustained release profile, noncytotoxicityand bioadhesive effect.
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Effect of chitosan on physicochemical properties of exenatide-loaded PLGA nanoparticles
박민호,백종섭,이초아,조정원 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.6
The aim of this study was to test stability of exenatide and compare physicochemical properties of PLGA nanoparticles. To make small, stable, uniform and highly encapsulated nanoparticles, various factors such as the components (polymer and stabilizer) and preparation condition (organic phase, temperature or sonication time)were considered. We tested the effect of organic phase,acid/base, ultrasonication time or temperature on exenatide to decide preparation condition of PLGA nanoparticles. And, PLGA nanoparticles were prepared by the double emulsion-solvent evaporation method and chitosan was selected as stabilizer. PLGA nanoparticles were characterized by yield, encapsulation efficiency, drug loading,particle size, zeta potential, polydispersity index and morphology. In this study, PLGA nanoparticles showed different physicochemical properties according to chitosan molecular weight. In case of particle size, PLGA nanoparticles using 0.5 g chitosan (4 kDa) showed biggest particle size (781.4 ± 24.1 nm) among PLGA nanoparticles prepared in this study and PLGA nanoparticles using 1 g chitosan (2 kDa) showed highest encapsulation efficiency (52.8 ± 1.7 %) among PLGA nanoparticles prepared in this study. And, all of PLGA nanoparticles using chitosan showed that polydispersity index was low and zeta-potential was increased. These results suggest that chitosan molecular weight affects physicochemical properties of PLGA nanoparticle.
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