• Title/Summary/Keyword: drug-release

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Controlled Release Behavior of Bioactive Molecules from Photo-Reactive Hyaluronic Acid-Alginate Scaffolds

  • Nam, Hye-Sung;An, Jeong-Ho;Chung, Dong-June;Kim, Ji-Heung;Chung, Chong-Pyoung
    • Macromolecular Research
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    • v.14 no.5
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    • pp.530-538
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    • 2006
  • There are three important components in tissue engineering: the cells, signaling factors (cytokines and growth factors), and scaffolds. To obtain finely engineered tissue, all three components should perform their individual functions and be fully integrated with each other. For the past few years, we have studied the characteristics of photodimerizable HA (CHA)/alginate (CA) composite materials. CHA/CA complex hydrogels, which were irradiated under UV light and, then treated with calcium ions, were found to have good biocompatibility, mechanical properties and water resistance for implantable tissue scaffolds. In this study, we introduced a cell growth factor (basic fibroblast growth factor; bFGF) into the CHA/CA scaffolds and studied its release behavior. We also introduced tetracycline hydrochloride and flurbiprofen into the same scaffolds as model activation factors and evaluated their release behaviors from the scaffolds. The drug release rate from the materials was influenced by various parameters, such as the degree of crosslinking, the cross linker type, the physico-chemical properties of the drug, and the amount of the drug in the polymer. The results indicated that the negatively charged CHA/CA composite materials showed sustained release behavior and that HA has a particularly strong negative charge, making it attractive toward tetracycline hydrochloride and bFGF, but repulsive toward flurbiprofen.

Therapeutic efficacy of the photoactivated sickle cells as novel drug delivery vehicle (약물전달 시스템 개발을 위한 여기된 광감응제의 응용)

  • Choe, Se-woon
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • 2015.10a
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    • pp.958-960
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    • 2015
  • Sickle cells possess a unique combination of traits that may enable their use as models for novel synthetic tumor targeting controlled release drug carriers with the ability to treat disseminated tumors in advanced metastatic disease. In this study, we assess the ability of light-activated release sickle cells to enhance tumor delivery of the fluorescent dye calcein by delayed photolysis controlled release compared to free systemic administration of calcein. Sickle cells from mouse models of the disease were shown to preferentially accumulate in tumors compared to adjacent tissue, in 4T1 tumors in mice on a time scale about 12 hours. Sickle cells photosensitized with protoporphyrin IX achieved delayed release of 50% of contents 8-16 hours after photoactivation, which was deemed useful for in vivo delivery of cargo to tumors given the tumor accumulation time of the sickle cells. Sickle cells may be useful as a model for new synthetic drug carrier particles with delayed photolysis controlled release properties.

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Adsorption and Release Characteristics of Sulindac on Chitosan-based Molecularly Imprinted Functional Polymer Films (키토산 기반 분자 각인 고분자 필름의 슐린닥 흡착 및 방출 특성)

  • Yoon, Yeon-Hum;Yoon, Soon-Do;Nah, Jae Woon;Shim, Wang Geun
    • Applied Chemistry for Engineering
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    • v.30 no.2
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    • pp.233-240
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    • 2019
  • Molecular recognition technology has attracted considerable attention for improving the selectivity of a specific molecule by imprinting it on a polymer matrix. In this study, adsorption and release characteristics of chitosan based drug delivery films imprinted with sulindac (SLD) were investigated in terms of the plasticizer, temperature and pH and the results were also interpreted by the related mathematical models. The adsorption characteristics of target molecules on SLD-imprinted polymer films were better explained by the Freundlich and Sips equation than that of the Langmuir equation. The binding site energy distribution function was also useful for understanding the adsorption relationship between target molecules and polymer films. The drug release of SLD-imprinted polymer films followed the Fickian diffusion mechanism, whereas the drug release using artificial skin followed the non-Fickian diffusion behavior.

Colon Delivery of Prednisolone Based on Chitosan Coated Polysaccharide Tablets

  • Park, Hyun-Sun;Lee, Jue-Yeon;Cho, Sun-Hye;Baek, Hyon-Jin;Lee, Seung-Jin
    • Archives of Pharmacal Research
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    • v.25 no.6
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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.

Characterization of alginate/carboxymethyl scleroglucan hydrogels as a delivery system for protein drug

  • Lee, Chang-Moon;Park, Jeong-Eun;Kim, Dong-Woon;Rhee, Joon-Haeng;Kim, Gwang-Yun;Lee, Ki-Young
    • 한국생물공학회:학술대회논문집
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    • 2005.04a
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    • pp.580-583
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    • 2005
  • The aim of this study was to prepare a hydrogels composed of alginate blended with a carboxymethyl scleroglucan (CMSC) and evaluate the feasibility of the hydrogels as a drug delivery system for a protein. The main advantage of the alginate/CMSC hydrogels is to improve a restricted drug release from alginate hydrogels. The CMSC was chemically synthesized with chloroacetic acid and confirmed using a FT-IR. The alginate/CMSC hydrogels were prepared at distinct compositions by crosslinking with calcium ions. The swelling ratios of these hydrogels increased significantly with increasing the content of CMSC. At pH 7.4, the swelling ratios of the hydrogels increased remarkably as compared to those at pH 1.2. In ovalbumin (OVA) release test, the amount of OVA released from the hydrogels showed higher as compared to those released at pH 1.2. In addition, the release of OVA was improved with increasing the content of CMSC. Thus, the alginate/CMSC hydrogels may be used as a potential system for oral delivery of protein drugs.

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The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies (이트라코나졸 마이크로스폰지의 약물 전달 시스템: 제조, 특성 및 방출 연구)

  • Cho, Young-Ho;Lee, Jong-Hwa;Kim, Hak-Hyung;Lee, Gye-Won
    • KSBB Journal
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    • v.26 no.3
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    • pp.217-222
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    • 2011
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of $Eudragit^{(R)}$ E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.

Biostable Poly(ethylene oxide)-b-poly(methacrylic acid) Micelles forpH-triggered Release of Doxorubicin

  • Choi, Young-Keun;Lee, Dong-Won;Yong, Chul-Soon;Choi, Han-Gon;Bronich, Tatiana K.;Kim, Jong-Oh
    • Journal of Pharmaceutical Investigation
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    • v.41 no.2
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    • pp.111-115
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    • 2011
  • pH-sensitive cross-linked polymeric micelles were synthesized by using block ionomer complexes of poly(ethylene oxide)-b-poly(methacrylic acid) (PEO-b-PMA) with calcium ions as micellar templates. An anticancer drug, doxorubicin (DOX) was conjugated on the cross-linked ionic cores of micelles via acid-labile hydrozone bonds. The resulting DOX-conjugated, pH-sensitive micelles are stable at physiological conditions, whereas the release of DOX was significantly increased at the acidic pH. Such micelles were internalized to lysosomes, and acidic pH in lysosomes triggers the release of DOX upon internalization in MCF-7 breast cancer cells. The released DOX entered the cell nucleus and eventually killed cancer cells. Therefore, these data demonstrate that the pH-sensitive micelles could be a promising nanocarrier for delivery of anticancer drug, DOX.

Development of Automated Diffusion Cell for Determining In Vitro Drug Release from Transdermal Device (경피흡수제형의 in vitro 약물방출실험을 위한 연속확산 장치의 개발)

  • Byun, Young-Rho;Choi, Young-Kweon;Jeong, Seo-Young;Kim, Young-Ha
    • YAKHAK HOEJI
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    • v.34 no.3
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    • pp.161-165
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    • 1990
  • An automated, simple, and reliable method was developed for determining in vitro drug release rate from transdermal delivery dosage forms. The patch is held in position in the heating block by sandwiching it between the middle plate and the bottom plate of diffusion cell. The dissolution profile of the commercially available transdermal scopolamine patch was determined over a 72-h period, and the results were compared with those obtained with other methods; paddle-over-disk method, reciprocating method, and diffusion cell method. It was demonstrated that the flow-through method is equivalent in terms of release rate profile and accumulated released drug amount over the lifetime of the dosage form tested. Also this method is simple, reliable and reproducible. Therefore, this technique can be used in a quality control for assuring product uniformity.

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Rectal Absorption of Acetaminophen from Polyethylene Glycol and Witepsol Suppositories (아세트아미노펜의 Polyethylene glycol 및 Witepsol 좌제의 직장흡수 - 병원제제를 목적으로 한 아세트아미노펜좌제의 조제 및 유용성 검토-)

  • Lee, Hye Suk;Jin, Sun Kyung;Choi, Jung Hwa;Ku, Young Soon
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.143-146
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    • 1998
  • Acetaminophen (APAP) suppositories with active ingredients, i.e., polyethylene glycol (PEG), Witepsol H-15 (WH), were prepared for hospital use and investigated on their drug release characteristics and pharmacokinetics. WH was employed as oil-soluble base with an aim of reducing fragility and mucosa irritancy that are common drawbacks found in PEG suppositories. Also hollow type suppository was tried as compared with conventional type suppository. Drug release tests revealed that in most formulations, more than $80\%$ of loaded APAP were released within 20 minutes, except for APAP-WH hollow type suppositories. Significant differences in the plasma concentration profile were observed among four type suppositories. $T_{max}$ of APAP-PEG and APAP-WH suppositories were 90 and 60 minutes, respectively, in hollow types. APAP-WH hollow type suppositories demonstrated fast absorption rates of APAP as compared with those of APAP-PEG suppositories. No burst effect was observed from APAP-WH suppository in contrast to APAP conventional type suppository, whereas AUCs of all the suppositories were similar. APAP-WH hollow type suppository may be an useful dosage form for hospital use.

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Evaluation of In-Vitro Dissolution and In-Vivo Absorption for Two Different Film-Coated Pellets of Clarithromycin

  • Zhang Xiang-rong;Chen Xiao-yan;Hu Lian-Dong;Tang Xing;Li San-Ming;Zhong Da-fang
    • Archives of Pharmacal Research
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    • v.28 no.8
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    • pp.977-982
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    • 2005
  • The aim of this study was to compare two formulations of film-coated pellets containing c1arithromycin after single oral dose study in healthy male volunteers. Two formulations with different coating polymers were prepared: formulation-1 (F-1) was prepared by incorporating three kinds of pH-dependent gradient-release coated pellets into capsules and formulation-2 (F-2) was prepared by coated with an insoluble semiosmotic film. Release profiles of filmcoated pellets were evaluated using paddle method under different conditions. Pharmacokinetic profiles of these formulations were obtained in three healthy male volunteers and compared to commercially available immediate release (IR) tablets. The relative bioavailability based on the $AUC_{0-24h}$ was found to be $96.2\%\;and\;58.7\%$ for F-1 and F-2 compared with IR, and the $T_{max}$ was delayed.