• 약학회지
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• 제30권6호
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• pp.306-310
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• 1986

The release of heparin from monolithic devices composed of different ratios of polyethylene oxide(PEO MW 20,000) and polydimethylsiloxane was investigated. Water soluble PEO plended into the polydimethylsiloxane proved a controlled release of heparin. The release rate of heparin could be controlled by varying the content of PEO and loading dose of heparin. The release rate of heparin from the devices increased as the content of PEO and heparin in the devices increased. The release rate of heparin from devices were related to nature of solute(ionic strength) and temperature. The release mechanism may be associated with the creation of pore or domine through the devices the water-uptake and the change in the physical structure of the polydimethysiloxane network.

• Archives of Pharmacal Research
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• 제9권4호
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• pp.193-199
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• 1986

The release of heparin from monolithic devices composed of different ratios of polythylene oxide (PEO MW 20,000) and hydrophobic polydimethylsiloxane or polyurethane was investigated. Water soluble PEO blended into the polymers provided a controlled release of heparin. The release rate of heparin could be controlled by varying the content of PEO. The heparin release rate from the devices increased as the content of PEO in the devices increased. The release mechanism may be associated with the creation of pore of domain through the devices following the swelling and the change in the physical structure of the polymer network. Hydrophobic polydimethylsiloxanes and polyurethanes containing PEO can provide an antith rombogenic material for prologed release of heparin from blended system.

• Journal of Pharmaceutical Investigation
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• 제18권4호
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• pp.169-174
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• 1988

The release of heparin from monolithic devices composed of different ratios of polyethylene oxide-polypropylene oxide (PEO-PPO) and hydrophobic polyurethane was investigated. The release rate of heparin could be controlled by varying the PEO-PPO content. The heparin release rate from the devices increased as the content of PEO-PPO in the devices increased. The release mechanism may be associated with creation of micro-channels and pores through the devices following the change in the physical structure of the polymer network. Hydrophobic polyurethane containing PEO-PPO can provide an antithrombogenic material for prolonged release of heparin from a heparin blended system.

• 약학회지
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• 제29권2호
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• pp.70-75
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• 1985

The influence of polyethylene glycol derivatives on heparin release from cylindrical monolithic type silicone segment devices was examined in physical saline solution. This water-soluble carrier caused the devices to absorb the water in aqueous media. The release rate of heparin from the devices was increased as molecular weight of polyethylene glycol was increased. Water soluble carrier incorporated into silitone segment devices permits controlled release of heparin that otherwise would be released extremly slowly from the polymer. Heparin released from the silicone segment containing polyethylene glycol showed the first-order kinetics. Without changing the release-pattern, the release rate of heparin could be controlled by varing molecular weight of polyethylene glycol, the water-soluble carrier and depleting polyethylene glycol on the outlayer of devices. The mechanism of release probably showed the creation of pore or microdomine through the devices secondary to the swelling.

• Journal of Pharmaceutical Investigation
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• 제17권2호
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• pp.75-78
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• 1987

The release rate of heparin from monolithic devices composed of raffinose, ${\beta}-cyclodextrin$, polyethylene oxide (Mw 20,000, PEO), and hydrophobic polyether urethane (biomer) was investigated. Water soluble raffinose, ${\beta}-cyclodextrin$, and PEO blended into the biomer provided a controlled release of heparin. The release rate of heparin could be controlled by the content of raffinose, ${\beta}-cyclodextrin$, and PEO in the devices. The mechanism of release rate increased by the raffinose, ${\beta}-cyclodextrin$, and PEO may result from the formation of channels and pores in the biomer matrices following the swelling and the change in the physical structure of polymer net work. Hydrophobic polyurethane containing raffinose, ${\beta}-cyclodextrin$, and PEO can provide a hydrophilic antithrombogenic material for prolonged release of heparin.

• 한국식품영양과학회지
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• 제20권1호
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• pp.40-45
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• 1991

The release of hepatic triglyceride lipase from cultured rat hepatocytes and its hormonal regulation were studied. The activity of lipase released into the medium in the presence of heparin was increasing during 24 hours on the 2nd of culture while this was 10% in the absence of heparin as compared with the lipase activity in the presense of heparin. When hepatocytes were cultured with anti-hepatic triglyceride lipase lgG the lipase activity was supp-ressed by 92% The results suggest that the enzyme relaeased into culture medium is identical to hepatic triglyceride lipase which can be released only in the presence of heparin the model of release being similar to that of lipoprotein lipase from adipocytes. The addition of monensin to the medium resulted in The inhibition of lipase secretion by 61% Insulin enhanced lipase activity only 20% whereas dexamethasone suppressed the activity by 44% These data inidica-ted that hepatic triglyceride lipase is secreted and released from hepatocytes in the presence of heparin and its secretion is regulated by hormones.

• BMB Reports
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• 제29권3호
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• pp.205-209
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• 1996

To investigate the role of heparin in keratinocyte growth factor (KGF) and acidic fibroblast growth factor (aFGF) high affinity binding to the KGF receptor (KGFR), a cell free system was established which utilized a secreted chimeric molecule between the KGFR extracellular domain and the immunoglobulin heavy chain Fc domain (KGFR-HFc). KGFR-HFc was purified from NIH 3T3 cells and demonstrated the binding of $[^3H]-heparin$ as well as heparin Sepharose. Scatchard analysis showed that the dissociation constant for heparin binding to KGFR-HFc was 140 nM. High affinity KGF and aFGF binding to KGFR-HFc remained unchanged after treatment with 0.6 M NaCl, which is the concentration sufficient to release any bound heparin to the KGFR-HFc. These results strongly suggest that although the KGFR interacts with heparin, the presence of heparin is not absolutely required for high affinity binding of either KGF or aFGF to the KGFR.

• 전기전자학회논문지
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• 제21권3호
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• pp.320-330
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• 2017

Porous nanosilica (PNS) has been identified as a potential candidate for controlled drug delivery. However, unmodified PNS-based carriers exhibited an initial release of loaded bioactive agents, which may limit their potential clinical applications. In this study, the surface of PNS was functionalized with adamantylamine (ADA) via disulfide bonds (-S-S-), PNS-S-S-ADA, which was then modified with cyclodextrin (CD)-heparin (Hep) (CD-Hep), PNS-S-S-CDH, for redox triggered rhodamine B (RhB) delivery. The obtained samples were then characterized by proton nuclear magnetic resonance ($^{1}H\;NMR$), Fourier transform infrared (FTIR), and transmission electron microscope (TEM). These results showed that PNS-S-S-CDH was successfully formed with spherical shape and average diameter of $45.64{\pm}2.33nm$. In addition, RhB was relatively encapsulated in the PNS-S-S-CDH (RhB@PNS-S-S-CDH) and slowly released up to 3 days. The release of RhB, in particular, was triggered due to the cleavage of -S-S- in the presence of dithiothreitol (DTT). It might be anticipated that the modified PNS can be used as redox-responsive drug delivery system in cancer therapy.

• The Journal of Advanced Prosthodontics
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• 제3권3호
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• pp.145-151
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• 2011

PURPOSE. This study was performed to investigate the ability of recombinant human-bone morphogenic protein-2 immobilized on a heparin-grafted bone substrate to enhance the osteoblastic functions. MATERIALS AND METHODS. The Bio-$Oss^{(R)}$, not coated with any material, was used as a control group. In rhBMP-2-Bio-$Oss^{(R)}$ group, rhBMP-2 was coated with Bio-$Oss^{(R)}$ using only deep and dry methods (50 ng/mL, 24 h). In heparinized rhBMP-2-Bio-$Oss^{(R)}$ group, dopamine was anchored to the surface of Bio-$Oss^{(R)}$, and coated with heparin. rhBMP-2 was immobilized onto the heparinized- Bio-$Oss^{(R)}$ surface. The release kinetics of the rhBMP-2-Bio-$Oss^{(R)}$ and heparinized rhBMP-2-Bio-$Oss^{(R)}$ were analyzed using an enzyme-linked immunosorbent assay. The biological activities of the MG63 cells on the three groups were investigated via cytotoxicity assay, cell proliferation assay, alkaline phosphatase (ALP) measurement, and calcium deposition determination. Statistical comparisons were carried out by one-way ANOVA test. Differences were considered statistically significant at $^*$P<.05 and $^{**}$P<.001. RESULTS. The heparinized rhBMP-2-Bio-$Oss^{(R)}$ showed more sustained release compared to the rhBMP-2-Bio-$Oss^{(R)}$ over an extended time. In the measurement of the ALP activity, the heparinized group showed a significantly higher ALP activity when compared with the non-heparinized groups (P<.05). The MG63 cells cultivated in the group with rhBMP-2 showed increased calcium deposition, and the MG63 cells from the heparinized group increased more than those that were cultivated in the non-heparinized groups. CONCLUSION. Heparin increased the rhBMP-2 release amount and made sustained release possible, and heparinized Bio-$Oss^{(R)}$ with rhBMP-2 successfully improved the osteoblastic functions.

• Korean Chemical Engineering Research
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• 제48권2호
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• pp.178-184
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• 2010

본 논문에서는 생체적합성 고분자들의 자기 조립 특성을 이용하여 마이크론 단위의 캡슐을 제조하여, 캡슐 내부에 단백질을 넣고 시간과 pH에 따른 방출 거동을 고찰하였다. 본 연구에서는 키토산과 헤파린 그리고 알지네이트를 사용하여 동공(hollow) 캡슐을 제조하였다. 멜라민과 포름알데히드를 일정 비율로 혼합하여, 표면에 전하를 가지는 마이크론 단위의 core를 제조한 후, 음전하를 가지는 헤파린 혹은 알지네이트를 core 위에 흡착시키고, 양전하를 띠는 키토산을 흡착시킨 후, core 위에 교대로 흡착시켜 Multilayer를 형성시켰다. 4 층을 쌓은 후에 HCl을 이용하여 pH 2로 조절하면, core는 제거되고 속이 비어 있는 캡슐을 제조할 수 있었다. 동공 캡슐은 투과전자현미경, 표면주사현미경 및 광학현미경으로 관찰하였다. 이러한 캡슐은 pH에 따라서 각기 다른 거동을 보이는데, 본 연구에서는 내부에 FITC-albumin을 넣어 UV분광기로 방출되는 상대적인 양을 관찰한 결과, 키토산-헤파린 캡슐과 키토산-알지네이트 캡슐은 각기 다른 pH에서 개폐됨을 알 수 있었다.