• Polymer(Korea)
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• v.28 no.4
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• pp.335-343
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• 2004

Carmustine (l,3-bis(2-chloroethyI)-1-nitrosourea, BICNU) used as antineoplastic drug for the treatment of brain tumor is not appropriate for the long term delivery, because it has short biological half life. Therefore, poly(D,L-lactide-co-glycolide) (PLGA) is useful as drug carrier for the long term delivery due to bulk erosion property. Glycolide monomer is applied to release of BICNU owing to non-toxic and monomeric components after biodegradation of PLGA. In this study, BICNU-loaded PLGA wafers with or without glycolide monomer were fabricated by conventional direct compression method for the sustained release of BICNU. These wafers were observed for their release profiles of BICNU and degradation rates by SEM, NMR, and GPC. Furthermore, we make multi-layer wafers and compare them with release profiles of conventional wafer. From these results, drug release of BICNU-loaded PLGA wafers was increased with increasing the glycolid monomer contents. We confirmed that glycolide monomer and BICNU contents in barrier-layer influenced the drug release profiles and degradation rate.

• Macromolecular Research
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• v.17 no.12
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• pp.1010-1014
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• 2009

Monodispersed microparticles with a poly(D,L-lactide-co-glycolide) (PLGA) core and a poly(ethyl 2-cyanoacrylate) (PE2CA) shell were prepared by Shirasu porous glass (SPG) membrane emulsification to reduce the initial burst release of doxorubicin (DOX). Solution mixtures with different weight ratios of PLGA polymer and E2CA monomer were permeated under pressure through an SPG membrane with $1.9\;{\mu}m$ pore size into a continuous water phase with sodium lauryl sulfate as a surfactant. Core-shell structured microparticles were formed by the mechanism of anionic interfacial polymerization of E2CA and precipitation of both polymers. The average diameter of the resulting microparticles with various PLGA:E2CA ratios ranged from 1.42 to $2.73\;{\mu}m$. The morphology and core-shell structure of the microparticles were observed by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The DOX release profiles revealed that the microparticles with an equivalent PLGA:E2CA weight ratio of 1:1 exhibited the optimal condition to reduce the initial burst of DOX. The initial release rate of DOX was dependent on the PLGA:E2CA ratio, and was minimized at a 1:1 ratio.

• Textile Coloration and Finishing
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• v.10 no.5
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• pp.32-38
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• 1998

Glycolides were polymerized by PPG or Pluronic(PN) to give A-B-A block copolyesters consisting of polyglycolide(A) and polypropylene glycol(B) or polyglycolide(A) and PN (B). Lactones were easily copolymerized with polyethers by ester interchange reaction even in the absence of catalyst. It is because PPG and PN are telechelic polyethers having hydroxy groups on their both ends. When the feed ratio of PPG(M$_{n}$=4,000) and PN(M$_{n}$=11,500) were over 5 and 10 wt% .elative to glycolide, respectively, the polymerization of glycolide took place from the terminus hydroxy groups of PPG or PN to produce the desired A-B-A block copolymers in high yields. The molecular weights of the copolymers, which estimated from the monomer conversions and the feed ratios of PPG and PN, could be controlled by changing the kind of terminus hydroxy of polyether and the feed molar ratio of PPG and PN. PN.

• Journal of Biomedical Engineering Research
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• v.13 no.2
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• pp.147-154
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• 1992

Poly (glycolic aclu-co-glycine-L-lactic aclu) has been prepared by rlng opening polymerlzation. The monomer 6-methyl morpholine-2, 5-dlone was synthe-slzed by bromoproplonylation of 2 bromopropionyl bromide with glycine. Glycolide and 6-methyl morpholine-2, 5-dione have been used as starling materials for polydepsipeptides. The synthesized copolymers have been Identlrled by NMR and FT-lR spectrophotometer. The Tg value of poly(glycollc aclu-co glycine-L-tactic acld ) Is In creased with increasing mole fraction of 6-methylmorpholine-2, 5-dlone(60-$84^{\circ}C$). The glass trasltion temperature of poly(glycolic acid-co-glycine-L-lactic-acid) (62-$86^{\circ}C$) is lower than that of poly (L-lactic acrid-co-glycine-L-lactic acid ). The thermal degradation of poly( L-lactic acid-co- glycine-L-lactic acid ) Is decreased with increasing mole fraction of L-lactide. The thermal degrada pion of poly(glycolic acrid-co-91ycine-L-lactic aclu ) is increased with increasing mole Fraction of glycolide.

• Korean Chemical Engineering Research
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• v.46 no.2
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• pp.205-210
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• 2008

Poly(D,L-lactide-co-glycolide) (PLGA) has been widely used as carriers in controlled release delivery systems due to its biodegradability and relatively good biocompatibility. However, Release pattern of carriers fabricated using PLGA have disadvantage an initial burst within a few days, lag time several days and then sudden release changes. To solve these problems of PLGA, we fabricated PLGA wafer including monomer. Also, drug release behavior restraint sudden burst effect using recrystallization of PLGA. Recrystallized PLGA was characterized the morphological difference by SEM and in vitro release behavior measured by HPLC. The PLGA molecular weight analyzed to recognize monomer influence during degradation process of polymer using GPC. In this study, drug release duration cut short up to three days and was eliminated the lag time based on the bulk erosion.

• Polymer(Korea)
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• v.30 no.6
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• pp.464-470
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• 2006

Diblock copolymers consisting of methoxy Poly (ethylene glycol) (MPEG) and poly (${\epsilon}-ca$ prolactone) (PCL), poly(${\delta}-valerolactone$) (PVL), poly(L-lactide) (PLLA), or poly(L-lactide-co-glycolide) (PLGA) were prepared to compare the characterization of diblock copolymers as a drug carrier. MPEG-PCL, MPEG-PVL, MPEG-PLLA, and MPEG-PLGA diblock copolymers were synthesized by the ring-opening polymerization of ${\epsilon}$-caprolactone or ${\delta}$-valerolactone in the presence of $HCl{\cdot}Et_2O$ as a monomer activator at room temperature and by the ring-opening polymerization of L-lactide or a mixture of L-lactide and glycolide in the presence of stannous octoate at $130^{\circ}C$, respectively. The synthesized diblock copolymers were characterized with $^1H-NMR$, GPC, DSC, and XRD. The micellar characterization of MPEG-polyester diblock copolymers in an aqueous phase was carried out by using NMR, dynamic light scattering, AFM, and fluorescence techniques. Most micelles exhibited a spherical shape in AFM. Thus, ore confirmed that the micelles formed with MPEG-polyester diblock copolymers have possibility as a potential hydrophobic drug delivery vehicle because a hydrophobic drug could be preferentially distributed in the micelle core.

• Macromolecular Research
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• v.11 no.4
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• pp.207-223
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• 2003

For last five years, we are developing the novel local drug delivery devices using biodegradable polymers, especially polylactide (PLA) and poly(D,L-lactide-co-glycolide) (PLGA) due to its relatively good biocompatibility, easily controlled biodegradability, good processability and only FDA approved synthetic degradable polymers. The relationship between various kinds of drug [water soluble small molecule drugs: gentamicin sulfate (GS), fentanyl citrate (FC), BCNU, azidothymidine (AZT), pamidronate (ADP), $1,25(OH)_2$ vitamin $D_3$, water insoluble small molecule drugs: fentanyl, ipriflavone (IP) and nifedipine, and water soluble large peptide molecule drug: nerve growth factor (NGF), and Japanese encephalitis virus (JEV)], different types of geometrical devices [microspheres (MSs), microcapsule, nanoparticle, wafers, pellet, beads, multiple-layered beads, implants, fiber, scaffolds, and films], and pharmacological activity are proposed and discussed for the application of pharmaceutics and tissue engineering. Also, local drug delivery devices proposed in this work are introduced in view of preparation method, drug release behavior, biocompatibility, pharmacological effect, and animal studies. In conclusion, we can control the drug release profiles varying with the preparation, formulation and geometrical parameters. Moreover, any types of drug were successfully applicable to achieve linear sustained release from short period ($1{\sim}3$ days) to long period (over 2 months). It is very important to design a suitable formulation for the wanting period of bioactive molecules loaded in biodegradable polymers for the local delivery of drug. The drug release is affected by many factors such as hydrophilicity of drug, electric charge of drug, drug loading amount, polymer molecular weight, the monomer composition, the size of implants, the applied fabrication techniques, and so on. It is well known that the commercialization of new drug needs a lot of cost of money (average: over 10 million US dollar per one drug) and time (average: above 9 years) whereas the development of DDS and high effective generic drug might be need relatively low investment with a short time period. Also, one core technology of DDS can be applicable to many drugs for the market needs. From these reasons, the DDS research on potent generic drugs might be suitable for less risk and high return.