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      • KCI등재

        Characterization and regulated naproxen release of hydroxypropyl cyclosophoraose-pullulan microspheres

        Choi, Jae Min,Lee, Benel,Jeong, Daham,Park, Kyeong Hui,Choi, Eun-Ji,Jeon, Yong-Joon,Dindulkar, Someshwar D.,Cho, Eunae,Do, Sun Hee,Lee, Kyungho,Lee, Im-Soon,Park, Seyeon,Jun, Bong-Hyun,Yu, Jae-Hyuk,Ju THE KOREAN SOCIETY OF INDUSTRIAL AND ENGINEERING 2017 JOURNAL OF INDUSTRIAL AND ENGINEERING CHEMISTRY -S Vol.48 No.-

        <P><B>Abstract</B></P> <P>Hydroxypropyl cyclosophoraose-pullulan (HPCys-Pul) microspheres were designed as a novel hybrid system of biocompatible pullulan matrice and pendant hydroxypropyl cyclosophoraoses with drug complexing ability. The HPCys-Pul microspheres were prepared by emulsion crosslinking method, and characterized using thermogravimetric analysis, Fourier transform infrared spectroscopy, scanning electron microscopy, and solid state NMR spectroscopy. By virtue of hydroxypropyl cyclosophoraoses, the developed microspheres can encapsulate 4.2-fold more naproxen than pullulan microspheres. Korsmeyer–Peppas model was introduced for describing release kinetics. <I>In vivo</I> naproxen release analysis was carried out in Sprague-Dawley (SD) rats. From those results HPCys-Pul microsphere will be a promising platform for controlled drug delivery.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Hybrid microspheres of biocompatible polysaccharide pullulan (Pul) and hydroxypropyl cyclosophoraoses (HPCys) were prepared. </LI> <LI> The HPCys-Pul microspheres showed both effective encapsulation and controlled release of naproxen (NPX). </LI> <LI> Those microspheres were completely characterized by TGA, XRD, FE-SEM, FT-IR, and solid-state NMR spectroscopy. </LI> <LI> Hybrid HPCys-Pul microspheres resulted in a pH-regulated release system as well as enhanced entrapment efficiency for NPX. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

      • KCI등재

        Characterization and regulated naproxen release of hydroxypropyl cyclosophoraose-pullulan microspheres

        최재민,Benel Lee,정다함,박경희,최은지,전용준,Someshwar D Dindulkar,조은애,도선희,이경호,이임순,박세연,전봉현,유재혁,정선호 한국공업화학회 2017 Journal of Industrial and Engineering Chemistry Vol.48 No.-

        Hydroxypropyl cyclosophoraose-pullulan (HPCys-Pul) microspheres were designed as a novel hybridsystem of biocompatible pullulan matrice and pendant hydroxypropyl cyclosophoraoses with drugcomplexing ability. The HPCys-Pul microspheres were prepared by emulsion crosslinking method, andcharacterized using thermogravimetric analysis, Fourier transform infrared spectroscopy, scanningelectron microscopy, and solid state NMR spectroscopy. By virtue of hydroxypropyl cyclosophoraoses, thedeveloped microspheres can encapsulate 4.2-fold more naproxen than pullulan microspheres. Korsmeyer–Peppas model was introduced for describing release kinetics. In vivo naproxen releaseanalysis was carried out in Sprague-Dawley (SD) rats. From those results HPCys-Pul microsphere will be apromising platform for controlled drug delivery.

      • SCISCIESCOPUS

        Enhancing bio-availability of β-naphthoflavone by supramolecular complexation with 6,6′-thiobis(methylene)-β-cyclodextrin dimer

        Choi, Jae Min,Cho, Eunae,Lee, Benel,Jeong, Daham,Choi, Youngjin,Yu, Jae-Hyuk,Jung, Seunho Elsevier 2016 Carbohydrate polymers Vol.151 No.-

        <P><B>Abstract</B></P> <P>The aryl hydrocarbon receptor (AhR) is a ligand activated transcriptional regulator, which governs key biological processes including detoxification of carcinogens. β-Naphthoflavone (β-NF) is a non-toxic flavonoid, and a potent AhR agonist. Thus, β-NF can induce the representative detoxifying enzyme cytochrome P4501A1, thereby enhancing the detoxification potential. However, its low water solubility hampers the use. We found that supramolecular complexation of β-NF with the synthetic 6,6′-thiobis(methylene)-β-cyclodextrin (β-CD-S) dimer significantly enhanced β-NF’s role as an AhR agonist. The water solubility of β-NF was increased to 469 fold by effective supramolecular complexation with the β-CD-S dimer, and caused significant induction of cytochrome P4501A1. Stable formation of the supramolecular complex of β-NF with β-CD-S-dimer was verified by various analyses. In summary, supramolecular complexation of β-NF with β-CD-S dimer greatly enhanced bio-availability of β-NF as an AhR agonist. Our findings provide an easy, non-destructive, and alternative approach to enhance the bio-availability of therapeutics.</P> <P><B>Highlights</B></P> <P> <UL> <LI> 6, 6′-Thiobis(methylene)-β-cyclodextrin dimer (β-CD-S-dimer) was synthesized. </LI> <LI> The β-CD-S-dimer was used to enhance β-naphthoflavone’s water solubility. </LI> <LI> The solubilized β-NF by complexation significantly induced the cytochrome P4501A1 activity. </LI> <LI> β-NF supramolecular complex with β-CD-S-dimer enhanced the bio-functionality of β-NF. </LI> <LI> Various instrumental analyses were performed to verify the formation of a supramolecular complex. </LI> </UL> </P>

      • Solubility and bioavailability enhancement of ciprofloxacin by induced oval-shaped mono-6-deoxy-6-aminoethylamino-β-cyclodextrin

        Choi, Jae Min,Park, Kyeonghui,Lee, Benel,Jeong, Daham,Dindulkar, Someshwar D,Choi, Youngjin,Cho, Eunae,Park, Seyeon,Yu, Jae-hyuk,Jung, Seunho Elsevier 2017 Carbohydrate polymers Vol.163 No.-

        <P><B>Abstract</B></P> <P>Ciprofloxacin is a broad-spectrum fluoroquinolone antibiotic used to treat bacterial infections; however, its limited aqueous solubility inhibits its broader clinical uses. This study investigated the complexation effect of mono-6-deoxy-6-aminoethylamino-β-cyclodextrin on the aqueous solubility and bioavailability of ciprofloxacin. During complexation, the oval-shaped cavity induced by mono-aminoethylamine substitution on the primary rim of β-cyclodextrin, was considered to be a key factor according to NMR spectroscopy and molecular modeling studies. The ciprofloxacin with mono-6-deoxy-6-aminoethylamino-β-cyclodextrin complex was characterized using FE-SEM, DSC, FT-IR, T1 relaxation, 2D NOESY, and DOSY NMR spectroscopy and molecular modeling studies. The solubility property of ciprofloxacin complexed with mono-6-deoxy-6-aminoethylamino-β-cyclodextrin was enhanced by seven-fold compared to that of pure ciprofloxacin. Furthermore antibacterial activity of that complex against methicillin-resistant <I>Staphylococcus aureus</I> was enhanced and it clearly showed the growth inhibition. The mono-6-deoxy-6-aminoethylamino-β-cyclodextrin has the potential to be utilized for other oblong guest molecules besides ciprofloxacin based on the novel induced elliptical cavity.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Mono-6-deoxy-6-aminoethylamino-β-cyclodextrin (Et-β-CD) was synthesized. </LI> <LI> Oval-shaped cavity within Et-β-CD was induced by mono aminoethylamine substitution. </LI> <LI> Ciprofloxacin (CIP)/Et-β-CD complex was thoroughly characterized. </LI> <LI> CIP/Et-β-CD complex effectively enhanced the bioavailability and solubility of CIP. </LI> </UL> </P>

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