• Polymer(Korea)
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• v.33 no.4
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• pp.353-357
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• 2009

Spray drying is an effective and stable process, which has been widely used to produce pharmaceutical powders. In the traditional spray drying process, it was not quite easy to control the aggregation and the size of particles. Particularly, the preparation of polymeric particles was relatively hard compared to the preparation of food and pharmaceutical ingredients, typically organic materials of small molecular weights. In this study, modification of a conventional spray dryer was tried to use electrical charge and co-axial nozzles to prepare polymeric particles. Poly(ethylene glycol) and poly (D,L-lactide-co-glycolide) were used as the inner polymeric materials, and lactose as the outer shell materials. The results showed that electrohydrodynamic spray-dried particles had a relatively uniform size and particle morphology, and the aggregation of particles could be suppressed compared to the conventional spray-dried particles. The electrohydrodynamic spray-dried powders consisted of spherical particles of $2{\sim}5{\mu}m$ diameters.

• Macromolecular Research
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• v.15 no.5
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• pp.437-442
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• 2007

Poly(ethylene glycol) methyl ether (PEG)-poly(${\beta}$-amino ester) (PAE) block copolymers were synthesized using a Michael-type step polymerization, and the construction of pH-sensitive polymeric micelles (PM) investigated. The ${\beta}$-amino ester block of the block copolymers functioned as a pH-sensitive moiety as well as a hydrophobic block in relation to the ionization of PAE, while PEG acted as a hydrophilic block, regardless of ionization. The synthesized polymers were characterized using $^1H-NMR$, with their molecular weights measured using gel permeation chromatography. The $pK_b$ values of the pH-sensitive polymers were measured using a titration method. The pH-sensitivity and critical micelle concentration (CMC) of the block copolymers in PBS solution were estimated using fluorescence spectroscopy. The pH dependent micellization behaviors with various bisacrylate esters varied within a narrow pH range. The critical micelle concentration at pH 7.4 decreased from 0.032 to 0.004 mg/mL on increasing the number of methyl group in the bisacrylate from 4 to 10. Also, the particle size of the block copolymer micelles was determined using dynamic light scattering (DLS). The DLS results revealed the micelles had an average size below 100 nm. These pH-sensitive polymeric micelles may be good carriers for the delivery of an anticancer drug.

• Journal of Pharmaceutical Investigation
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• v.40 no.spc
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• pp.75-82
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• 2010

Specific diseases like cancer and acquired immune deficiency syndrome (AIDS) occur at various organs including lymphatics and spread through lymphatic system. Thus, if therapeutic agents for such diseases are more distributed or targeted to lymphatic system, we can obtain several advantages like reduction of systemic side effect and increase of efficacy. For these reasons, much interest has been focused on the nature of lymphatics and a lot of studies for lymphatic delivery of drugs have been carried out. Because lymphatics consist of single layer endothelium and have high permeability compared with blood capillaries, especially, the studies using nano-sized carriers have been performed. Polymeric nano-particle, liposome, and lipid-based vehicle have been adopted for lymphatic delivery as carriers. According to the administration route and the kind of carrier, the extent of lymphatic delivery efficiency of nano-sized carriers has been changed and influenced by several factors such as size, charge, hydrophobicity and surface feature of carrier. In this review, we summarized the key factors which affect lymphatic uptake and the major features of carriers for achieving the lymphatic delivery. Lymphatic delivery of drug using nano-sized carriers has many fold improved ability of lymphatic delivery compared with that of conventional dosage forms, but it has not shown whole lymph selectivity yet. Even though nano-sized carriers still have the potential and worth to study as lymphatic drug delivery technology as before, full understanding of delivery mechanism and influencing factors, and setting of pharmacokinetic model are required for more ideal lymphatic delivery of drug.

• Journal of Pharmaceutical Investigation
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• v.37 no.4
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• pp.229-235
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• 2007

Multi-layered granules were prepared by a fluidized-bed coater and uniformed granules were obtained with a size range between $950{\sim}1000{\mu}m$ in diameter. The granule system was composed of three layers, i.e. seed layer with sugar sphere bead and a water-swellable polymer, middle layer with a drug, solubilizer and polymer, and the top layer of porous membrane with a polymeric binder. The aim of this work is to find out the dependence of a drug dissolution rate on the amount of a water-soluble binder and a solubilizer in the granule system. The results showed that the higher amount of hydrophilic binder in the porous membrane, gave the bigger pore size and porosity and made faster dissolution rate and also the higher amount of solubilizer in drug layer enhanced the dissolution rate of drug.

• Journal of the Korea Institute of Information and Communication Engineering
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• v.20 no.12
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• pp.2395-2400
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• 2016

Conventional drug carriers such as liposomes, nanoparticles, polymer micelles, polymeric conjugate and lipid microemulsion for cancer chemotherapy shield normal tissues from toxic drugs to treat cancer cells in tumors. However, inaccurate tumor targeting uncontrolled drug release from the carriers and unwanted accumulation in healthy sites can limit treatment efficacy with current conventional drug carriers with insufficient concentrations of drugs in the tumors and unexpected side effects as a result. Sickle red blood cells show natural tumor preferential accumulation without any manipulation due to the adhesive interaction between molecular receptors on the membrane surface and counter-receptor on endothelial cells. In addition, structural changes of microvascular in tumor sites enhances polymerization of sickle red blood cells. In this research, we examined the use of sickle red blood cells as a new drug carrier with novel tumor targeting and controlled release properties to quantify its therapeutic effects.

• Journal of Pharmaceutical Investigation
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• v.40 no.4
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• pp.255-261
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• 2010

Pluronic as pharmaceutical excipients are listed in the US and British Pharmacopoeia. In particular, Pluronics exist as different compositions and display abundant phases as self-assembling into polymeric micelles with various morphologies depending on the aqueous solvent quality, the composition of structure, and hydrophilic-lipophilic balance (HLB). Pluronics were also known as a P-gp modulator, which was exploited as a reversal molecule of multi-drug resistant (MDR) cancers. We selected a lamella forming Pluronic L92 which has high hydrophobicity and relatively long PEO block among L series of Pluronics. The dispersion of L92 showed great size particles and low stability. To increase the stability and to decrease the particle size, secondary Pluronics (F68, F88, F98, F127, P85, P105, and P123) with relatively long PEO chain were added into 0.1 wt% Pluronic L92 dispersion. The stability of binary systems was increased due to incorporated long PEO chain. Their particle sizes slightly decreased to over 200~400 nm and their solubilization capacity of binary systems didn't change except Pluronic L92/P123 mixtures. The L92/P123 systems showed ca. 100 nm sizes and lowest turbidity among the all systems. The solubilization capacity of 0.1 wt% L92/0.1 wt% P123 was slightly increased compared to 0.1 wt% L92 mono system and other binary systems. These nano-sized binary systems may have potential as alternative drug delivery systems with simple preparation method and overcome the drawbacks of mono systems such as low stability and loading capacity.

• Polymer(Korea)
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• v.35 no.5
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• pp.483-487
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• 2011

For the preparation of effective non-vascular drug eluting stent (DES), pullulan acetate (PA) was investigated as a coating material for polytetrafluorethylene (PTFE)-covered stent. PA was coated on PTFE-covered stent (PTFE-stent) by dip coating technique, and then its surface morphology, drug release behavior and cellular toxicity were tested. Field emission-scanning electron microscopy (FE-SEM) result indicated that its surface was smoother after PA coating without any cracking. The sustained release behavior of paclitaxel from PA-coated PTFE membrane was observed for 80 days. Also, the biological stability of paclitaxel in the membrane was confirmed by annexin V binding assays. Furthermore, the antitumor activity was demonstrated by an in vivo test against CT-26 murine colorectal tumors. From the results, we concluded that PA was expected as a useful coating material to design an effective non-vascular DES.

• Polymer(Korea)
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• v.36 no.2
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• pp.182-189
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• 2012

In this study, poloxamer hydrogels were prepared by electron beam irradiation and evaluated for potential application as a buccal mucoadhesive drug delivery system. Poloxamer, one of typical thermoresponsive polymers, was modified to have vinyl end groups for crosslinking reaction, and its hydrogels were fabricated by irradiation crosslinking reaction. Carbopol as a mucoadhesive polymeric additive was introduced to improve the mucoadhesive property of the hydrogels and its effect on the mucoadhesion and drug release properties was investigated. The results showed that the end group modification of poloxamer and the addition of carbopol improved mucoadhesive force and mechanical properties and led to a sustained drug release behavior.

• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.393-400
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• 2009

PHEA (hydroxyethyl-aspartamide)-mPEG (methoy-polyethyleneglycol)-$C_{16}$ (hexadecylamine)-ED (ethylenediamine) was prepared as a drug delivery carrier. The structure and molecular weight of polymers were characterized by $^1H$-NMR and gel permeation chromatography. Micelle size and shape were measured by electro-photometer light scattering and transmission electron microscope. The mean diameter of micelles was 23 nm in aqueous solution. To evaluate the potential of these polymeric micelles as a drug carrier, PSI-mPEG-$C_{16}$-ED was conjugated with Cy5.5 for Near-Infrared Fluorescent (NIRF) based optical imaging. PSI-mPEG-$C_{16}$-ED-Cy5.5 was injected intravenously into mice (n=5) and in vivo NIRF imaging was performed during 48 h after injection. The biodistribution study at 24 h after injection showed the longcirculation property of PSI-mPEG-$C_{16}$-ED-Cy5.5. Therefore, PSI-mPEG-$C_{16}$-ED micelles could be a promising drug carrier and imaging agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.3 s.47
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• pp.295-305
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• 2004

Colloid and surface chemistry have been focused on surface area and surface energy. Local surface properties such as surface density, interaction, molecular orientation and reactivity have been one of interesting subjects. Systems of such surface energy being important would be listed as association colloid, emulsion, particle dispersion, foam, and 2-D surface and film. Such nanoparticle systems would be applied to drug delivery systems and functional cosmetics with biocompatible and degradable materials, while nanoparticles having its size of several nm to micron, and wide surface area, have been accepted as a possible drug carrier because their preparation, characteristics and drug loading have been inves-tigated. The biocompatible carriers were also used for the solubilization of insoluble drugs, the enhancement of skin absorption, the block out of UV radiation, the chemical stabilization and controlled release. Nano/micro emulstion system is classified into nano/microsphere, nano/microcapsule, nano/microemulsion, polymeric micelle, liposome according to its prep-aration method and size. Specially, the preparation method and industrial applications have been introduced for polymeric micelles self-assembled in aqueous solution, nano/microapsules controlling the concentration and activity of high concen-tration and activity materials, and monolayer or multilayer liposomes carrying bioactive ingredients.