• Journal of Pharmaceutical Investigation
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• 제36권6호
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• pp.355-361
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• 2006

Intraarticular corticosteroid injections for therapy of rheumatic arthritis are administered with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of corticosteroidal drug, dexamethasone(DEX), administered at hish dose limited the therapeutic efficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. As a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate(DEX-PAL) was prepared via esterification of palmitoyl chloride and dexamethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated with variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter $83{\sim}95$ nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of aliphatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanospheres containing DEX-PAL may be a promising novel drug carrier for the controlled release of the poorly water-soluble drugs.

• Biotechnology and Bioprocess Engineering:BBE
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• 제11권3호
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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.

• Bulletin of the Korean Chemical Society
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• 제22권5호
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• pp.467-475
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• 2001

A triblock copolymer based on $poly(\varepsilon-caprolactone)$ (PCL) as the hydrophobic part and poly(ethylene glycol) (PEG) as the hydrophilic portion was synthesized by a ring-opening mechanism of ${\varepsilon}-caprolactone$ with PEG containing a hydroxyl group at bot h ends as an initiator. The synthesized block copolymers of PCL/PEG/PCL (CEC) were confirmed and characterized using various analysis equipment such as 1H NMR, DSC, FT-IR, and WAXD. Core-shell type nanoparticles of CEC triblock copolymers were prepared using a dialysis technique to estimate their potential as a colloidal drug carrier using a hydrophobic drug. From the results of particle size analysis and transmission electron microscopy, the particle size of CEC core-shell type nanoparticles was determined to be about 20-60 nm with a spherical shape. Since CEC block copolymer nanoparticles have a core-shell type micellar structure and small particle size similar to polymeric micelles, CEC block copolymer can self-associate at certain concentrations and the critical association concentration (CAC) was able to be determined by fluorescence probe techniques. The CAC values of the CEC block copolymers were dependent on the PCL block length. In addition, drug loading contents were dependent on the PCL block length: the larger the PCL block length, the higher the drug loading content. Drug release from CEC core-shell type nanoparticles showed an initial burst release for the first 12 hrs followed by pseudo-zero order release kinetics for 2 or 3 days. CEC-2 block copolymer core-shell type nanoparticles were degraded very slowly, suggesting that the drug release kinetics were governed by a diffusion mechanism rather than a degradation mechanism irrelevant to the CEC block copolymer composition.

• Archives of Pharmacal Research
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• 제23권4호
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• pp.385-390
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• 2000

To demonstrate the effect of formulation conditions on the controlled release of protein from poly(lactide-co-glycolide) (PLGA) microspheres for use as a parenteral drug carrier, ovalbumin (OVA) microspheres were prepared using the W/O/W multiple emulsion solvent evaporation and extraction method. Methylene chloride or ethyl acetate was applied as an organic phase and poly(vinyl alcohol) as a secondary emulsion stabilizer. Low loading efficiencies of less than 20％ were observed and the in vitro release of OVA showed a burst effect in all batches of different microspheres, followed by a gradual release over the next 6 weeks. Formulation processes affected the size and morphology, drug content, and the controlled release of OVA from PLGA microspheres.

• 대한화학회지
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• 제55권6호
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• pp.978-982
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• 2011

In order to enhance the target action of chitosan-based drug, this paper firstly prepared phenylalanyl-glycylchitosan (Phe-Gly-CS) by grafting the key intermediate, bromoacetyl-phenylalanine (BA-Phe) onto chitosan. Then the target sugar molecule, lactobionic acid (LA), was grafted to Phe-Gly-CS and the topic compound lactobionic acid grafted phenylalanyl-glycyl-chitosan (Phe-Gly-CS-LA) was finally obtained in a yield of 78.8%. The product were characterized by FTIR, MS and 1H NMR. The preparing condition of BA-Phe was optimized as follows: the best pH was 10-11, the optimum temperature was $-4^{\circ}C$, the reaction time was 1.5 h.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.408.1-408.1
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• 2002

A interpolymer complexes composed of poly(acrylic acid)(PAA) and po!y(vinyl alcohol)(PVA) were prepared by template polymerization of acrylic acid in the presence of PVA for mucoadhesive drug delivery. FT -IR results showed that the PAA/PVA interpolymer complex was formed by hydrogen bonding between the carboxyl groups of PAA and the hydroxyl group of PVA. The dissolution rate or the swelling ratio of the PAA/PVA interpolymer complexes was dependent on the pH and molecular weight of PVA that was used as a template. (omitted)

• 한국산학기술학회논문지
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• 제16권1호
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• pp.585-592
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• 2015

이 연구의 목적은 척추 추간판 융해제인 카이모파파인을 나노캐리어 시스템에 충진시켜 주입시, 추간판내 약제의 확산범위가 감소하는지 평가하기 위한 것이다. 총 3주간 시행된 실험의 재료로는 두 개의 카데바에서 채취된 열다섯 개의 척추 추간판이 쓰였고, 이들은 주입되는 카이모파파인의 종류에 따라 일반 카이모파파인 그룹과 나노캐리어 시스템 그룹으로 나뉘었다. 나노캐리어 시스템 그룹은 다시 그 기반재료가 되는 플루로닉의 종류에 따라 플루로닉 F 127(DA-PF 127) 나노캐리어 그룹과 플루로닉 F 68(DA-PF 68) 나노캐리어 그룹으로 나뉘었다. 실험결과 나노캐리어 시스템을 사용한 그룹은 일반 카이모파파인 그룹에 비해, 척추 추간판 내부로 주입되었을 때, 주입지점에서 멀리 확산되지 않고 국소적으로 작용하는 특성을 보였다(p<0.01). 이러한 특성은 향후 추간판 내 병소만을 선택적으로 제거하는 최소침습적 척추시술의 기반약제로 응용될 가능성을 제시해준다.

• 한국섬유공학회:학술대회논문집
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• 한국섬유공학회 2003년도 봄 학술발표회 논문집
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• pp.297-298
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• 2003

Chitin is a natural biopolymer that, with its derivative chitosan, has been represented as a biomaterial with considerable potential in wide ranging medical applications. But there are some limitations in using chitosan as attained, for instance, the problem of water solubility$^1$. In order to use chitosan in various applications (e.g. drug carrier), chemical modifications are often necessary$^2$. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.358.3-358.3
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• 2002

We recently synthesized new platinum(II) complex analogs containing trans-1 and cis-l.2-diaminocyclohexane (DACH) as carrier ligands and L -3-phenyllactic acid(PLA) as a leaving group. Our platinum-based drug discovery program has been aimed at developing drugs capable of diminishing toxicity and improving selective cytotoxicity. (omitted)

• Archives of Pharmacal Research
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• 제25권6호
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• pp.964-968
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• 2002

Colon drug delivery is advantageous in the treatment of colonic disease and oral delivery of drugs unstable or suceptible to enzymatic degradation in upper GI tract. In this study, multilayer coated system that is resistant to gastric and small intestinal conditions but can be easily degraded by colonic bacterial enzymes was designed to achieve effective colon delivery of prednisolone. Variously coated tablets containing prednisolone were fabricated using chitosan and cellulose acetate phthalate (CAP) as coating materials. Release aspects of prednisolone in simulated gastrointestinal fluid and rat colonic extracts (CERM) were investigated. Also, colonic bacterial degradation study of chitosan was performed in CERM. From these results, a three layer (CAP/Chitosan/CAP) coated system exhibited gastric and small intestinal resistance to the release of prednisolone in vitro most effectively. The rapid increase of prednisolone in CERM was revealed as due to the degradation of the chitosan membrane by bacterial enzymes. The designed system could be used potentially used as a carrier for colon delivery of prednisolone by regulating drug release in stomach and the small intestine.