• Journal of Biomedical Engineering Research
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• v.28 no.4
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• pp.484-493
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• 2007

Two polymeric prodrugs of PGE1 (prodrugs IVg and PNg) were newly synthesized. The drug conjugation proceeded in quantitative yield without decomposition of PGE1 to PGA1. With two types conjugates, PEG-PGE1 and PN-PGE1 with different spacer groups, we first discovered a possibility of slow release of PGE1 in blood circulatory system. PGE1 is conjugated with PEG and PN through the long alkylene spacers, and their availability as polymeric prodrugs is evaluated. Their drug-releasing behavior was examined both in phosphate buffer (pH=7.4) and rat plasma. Each prodrug was known to be highly stabile in the buffer solution. The drug-releasing rate became much faster in rat plasma than in the buffer solution due to the acceleration by the plasma enzymes. The drug-release was found to reach a plateau in rat plasma because the released PGE1 or its derivatives may be captured or decomposed by the plasma proteins. The slower drug-releasing rate of pro drug PNg in rat plasma is reasonably attributed to the molecular aggregation due to the hydrophobic bonding between the PGE1 moieties and spacers.

• Journal of the Korean Chemical Society
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• v.56 no.4
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• pp.473-477
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• 2012

The novel chitosan-based thermosensitive hydrogels were prepared as control-releasing drug carriers. N-carboxyethyl chitosan (ACS) was synthesized by microwave heating for 1 h through Michael addition of CS to acrylic acid in a grafting yield of 52.97%, which was proved to be a faster and more efficient way than ordinary methods. 5-Fu was modified with formaldehyde to synthesize N,N'-Bis(hydroxymethyl)-5-fluorouracil (5-Fu-OH). Then an esterification was performed using ACS and 5-Fu-OH to give 5-Fu-ACS. The new thermosensitive hydrogels were prepared by adding sodium glycerophosphate to the solution of compounds under a certain constant temperature. Simultaneously, the hydrogels' swelling rate, in vitro drug release rate and thermosensitive were studied, and found that the 5-Fu-ACS composite hydrogel had more excellent releasing effect, higher drug loading and better thermosensitive.

• 한국생물공학회:학술대회논문집
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• 2003.10a
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• pp.111-112
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• 2003

• Journal of Pharmaceutical Investigation
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• v.26 no.2
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• pp.119-124
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• 1996

To develop oral controlled release dosage forms, ionic interactions between polymers and drugs were evaluated. Hydroxypropylmethyl cellulose and carboxymethylene were used as model nonionic and ionic polymers, respectively. 5-fluorouracil, propranolol-HCl and sodium salicylate were selected as model nonionic, cationic and anionic, respectively. Polymer-drug mixtures were compressed into tablets and drug release kinetics from these tablets were determined. Drug release from the tablets made of the nonionic polymer was not affected by the charge of drugs, rather, was regulated by the solubility of drugs in different pH releasing media. However, drug release kinetics were significantly affected when drug-polymer ionic interactions exist. Enhanced drug release was observed from anionic drug-anionic polymer tablets due to ionic repulsion, whereas drug release was retarded in cationic drug-anionic polymer tablets owing to ionic attractive force. Therefore, the results suggested that the polymer-drug interactions are important factors in designing controlled release dosage forms.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.301-302
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• 2003

With the aim of obtaining the early bone regeneration efficacy, poly (L-lactide) particulates were developed as a long-term drug carrier system.Biodegradable microparticulates have been used extensively as drug delivery devices. However, problems like poor encapsulation efficiencies of the drugs and complicated fabrication process are still remained to be solved. (omitted)

• Proceedings of the KACD Conference
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• 2003.11a
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• pp.553-553
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• 2003

I. Objectives Endodontic disease is caused primarily by bacteria that interact with periradicular host from the root canal system. Chlorhexidine gluconate is known to effective to eliminate Enterococcus faecalis which resists to other intracanal medicaments. The aim of this in vitro study was to develop a slowly releasing root canal disinfectant using using chlorhexidine gluconate and chitoic acid. II. Materials and Methods Three different group were prepared with different drug release mechanism. In group A, paper points as used core material were loaded with 20% chlorhexidine gluconate.(omitted)

• Biotechnology and Bioprocess Engineering:BBE
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• v.11 no.3
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• pp.262-267
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• 2006

The objective of this study was to develop new self-organized nanogels as a means of drug delivery in patients with cancer. Pullulan (PUL) and deoxycholic acid (DOCA) were conjugated through an ester linkage between the hydroxyl group in PUL and the carboxyl group in DOCA. Three types of PUL/DOCA conjugates were obtained, differing in the number of DOCA substitutions (DS; 5, 8, or 11) per 100 PUL anhydroglucose units. The physicochemical properties of the resulting nanogels were characterized by dynamic light scattering, transmission electron microscopy, and fluorescence spectroscopy. The mean diameter of DS 11 was the smallest (approx. 100 nm), and the size distribution was unimodal. To determine the organizing behavior of these conjugates, we calculated their critical aggregation concentrations (CACs) in a 0.01-M phosphate buffered saline solution. They were $10.5{\times}10^{-4}mg/mL,\;7.2{\times}10^{-4} mg/mL,\;and\;5.6{\times}10^{-4} mg/mL$ for DS 5, 8, and 11, respectively. This indicates that DOCA can serve as a hydrophobic moiety to create self-organized nanogels. To monitor the drug-releasing behavior of these nanogels, we loaded doxorubicin (DOX) onto the conjugates. The DOX-loading efficiency increased with the degree of DOCA substitution. The release rates of DOX from PUL/DOCA nanogels varied inversely with the DS. We concluded that the PUL/DOCA nanogel has some potential for use as an anticancer drug carrier because of its low CAC and satisfactory drug-loading capacity.

• 대한임상약리학회:학술대회논문집
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• 1995.12a
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• pp.63-63
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• 1995

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.217.1-217.1
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• 2000

• BMB Reports
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• v.40 no.6
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• pp.979-985
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• 2007

Induction of growth hormone (GH) by Glycyrrhizae Radix (GR), one of the most popular herbal medicine, and its major ingredients were studied in rat pituitary cells in vitro and in vivo assay. The MeOH extract and the n-hexane (HX) fraction of GR induced rat GH (rGH) release up to 1.89 times ($0.34{\pm}0.04 nM$) and 4.59 times ($0.83{\pm}0.03 nM$), compared to the basal level (p < 0.05). Among many ingredients isolated and purified from GR both glycyrrhetinic acid and glycyrrhizin induced significantly rGH release compared to the control (p < 0.05). After an intravenous injection of rat growth hormone releasing hormone (rGHRH) ($10{\mu}g$/kg) as positive control, in SD rats, $T_{max}$ of plasma rGH level was 10 min, $C_{max}$ was $3.84{\pm}0.01 nM$ (n = 3), and enhanced plasma rGH level returned to the baseline in 90 min. Both $AUC_{0-90}$ (area under the curve) of plasma rGH level after HX fraction and that after rGHRH administration were increased significantly from the basal level, respectively (p < 0.01). In conclusions, HX fraction is the most active fraction of MeOH extract of GR in rGH induction.