• Title/Summary/Keyword: controlled drug release

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Alginate/Carboxymethyl Scleroglucan Hydrogels for Controlled Release of Protein Drugs

  • Lee, Chang-Moon;Jeong, Hwan-Jeong;Kim, Dong-Woon;Lee, Ki-Young
    • Macromolecular Research
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    • v.16 no.5
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    • pp.429-433
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    • 2008
  • Alginate/carboxymethyl scleroglucan (CMSG) hydrogels were suggested as a novel carrier for the controlled release of protein drugs. The drug release characteristics of alginate hydrogels were improved by CMSG addition. Scleroglucan (Sclg) was carboxymethylated using monochloroacetic acid in aqueous alkaline medium. Alginate/CMSG hydrogels were prepared by dropping the mixture solution of alginate/CMSG into calcium chloride solution. The swelling behaviors and drug release characteristics of the hydrogels were investigated in the buffers of pH 1.2 or 7.4. As the CMSG content increased in the hydrogels, the swelling ratio of the alginate/CMSG hydrogel increased rapidly in the buffer of pH 7.4. At pH 1.2, however, the swelling ratio significantly decreased compared to that at pH 7.4. According to in vitro release tests, only 15% of ovalbumin, investigated as a model protein drug, was released from the alginate/CMSG hydrogels at pH 1.2 within 6 h. At pH 7.4, however, the drug release significantly increased due to the rapid swelling of the hydrogels. The release and swelling behaviors of the hydrogels could be controlled by changing the CMSG content in the hydrogels. These results supported the use of alginate/CMSG hydrogels as a suitable carrier for the controlled release of protein drugs in a pH responsive manner.

Fabrication and Characterization of Flurbiprofen loaded Chitosan Beads for Periodontal Regeneration (치주조직 재생용 플루르비프로펜 함유 키토산 비드의 제조 및 용출특성)

  • Rhee, Su-Jin;Park, Yoon-Jeong;Lee, Seung-Jin;Chung, Chong-Pyoung
    • Journal of Pharmaceutical Investigation
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    • v.27 no.1
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    • pp.71-77
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    • 1997
  • With the aim of improving periodontal regeneration efficacy, as a biodegradable local drug delivery device, drug releasing chitosan beads were prepared. Chitosan beads were prepared through the formation of intermolecular or intramolecular ionic interaction bewteen chitosan and sodium tripolyphosphate and were loaded with flurbiprofen. The mean diameter of the beads was $250\;{\mu}m$. Drug loading efficiency was improved by regulating the pH of tripolyphosphate solution. The drug release kinetics mainly depended upon the hydrophobic properties of the flurbiprofen, that is, the release of flurbiprofen showed initial burst with rapid release for the first day followed by a levelling off of the release rate. However, the release rate could be controlled by the formulation factor including the pH, concentration of the tripolyphosphate solution, gelation time, drug contents. From these results, flurbiprofen loaded chitosan beads were anticipated as biodegradable local drug delivery devices for periodontal regeneneration.

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Preparation and Dissolution Profiles of Controled Release Formulations Containing Tamsulosin Hydrochloride (염산 탐스로신을 함유하는 방출제어형 제제의 제조 및 용출거동)

  • Yun, Jae-Nam;Kim, Jeong-Soo;Kim, Dong-Woo;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.35 no.6
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    • pp.445-451
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    • 2005
  • As a selective ${\alpha}_{1A}-adrenoreceptor$ antagonist, tamsulosin has been used clinically for urinary obstructed patients with benign prostatic hyperplasia. The single and multi-layered pellets containing tamsulosin hydrochloride were prepared in an effort to control the drug release, avoiding dose-dependent side effects of tamsulosin hydrochloride upon oral administration. The drug release from multi-layered pellets was substantially controlled, compared with single layered pellets. The drug release from coated pellets with single or multi layer was affected by the nature of coating agent, the percentage of coating level and the presence of hydrophilic material in coating layer. In conclusion, the controlled release oral delivery system using multi-layered pellet is very useful for tamsulosin hydrochloride, resulting in improvement of patient compliance and therapeutic drug levels for a longer period of time.

Evaluation of Methyl Methacrylate-Butyl Methacrylate Copolymer Films and Kinetics of Nitrofurazone Release (메칠메타크릴레이트-부틸메타크릴레이트 공중합체 필름의 평가 및 니트로푸라존 방출의 속도론적 연구)

  • Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.17 no.3
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    • pp.111-126
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    • 1987
  • Methyl methacrylate-butyl methacrylate copolymer (MMBM)-dibutyl phthalate (DBP) films were investigated as a potential topical drug delivery system for the controlled release of nitrofurazone. The kinetic analysis of release data indicated that drug release followed a diffusion-controlled granular matrix model, where the quantity released per unit area is proportional to the square root of time. DBP of several hydrophobic plasticizers selected was found to give the highest release of nitrofurazone. However, hydrophilic plasticizers such as propylene glycol and polyethylene glycol 400 had no controlled release properties and acceptable film formation. The effects of changes in film composition, drug concentration, film thickness, pH of release medium, and temperature on the in vitro release of nitrofurazone were analyzed both theoretically and experimentally. The release rate constant (k') was found to be proportional to DBP content, pH, and the temperature of release medium, but independent of film thickness, and drug concentration in a range of 0.1-0.4% by weight. The linear relationship was found to exist between the log k' and DBP content. The release of nitrofurazone from MMBM-DBP (8:2) films was found to be an energy-linked process. Two energy terms were calculated ; the activation energy for matrix diffusion was 13.45 kcal/mole, and the heat of drug crystal solvation was 27.26-29.34 kcal/mole. Observation of scanning electron micrographs and microscopic photographs showed that the incorporation of DBP in films increased markedly the particle size of nitrofurazone dispersed in the film matrix, comparing with the fine dispersion of nitrofurazone in pure MMBM film alone.

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Controlled Release of Propranolol Hydrochloride and Indomethacin from Hollow Type Suppository Using Witepsol H-15 (Witepsol 중공좌제로부터의 염산프로프라놀롤 및 인도메타신의 방출제어)

  • Jin, Suk-Yeong;Gu, Yeong-Sun
    • YAKHAK HOEJI
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    • v.40 no.4
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    • pp.400-410
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    • 1996
  • In oder to develop the controlled release of drugs from the suppositories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppo sitory forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The oleaginous Witepsol H-15 (WH-15) as a base, and indomethacin (IDM) of a very slightly soluble drug and propranolol-HCL (PPH) of a very soluble drug were employed as model drugs. The in vitro drug release showed that the cumulative release amount of PPH from PPH-(methylcellulose) MC-SDS and PPH-(ethylcellulose) EC-SDS hollow type suppositories reached 40% and 12% in 6 hrs,respectively. On the other hand, the drug release for a conventional suppository was 80% in 6 hrs. For the IDM suppositories,the cumulative drug release from IDM-(polyvinylpyrrolidone) PVP-SDS hollow type suppositories reached 99% in 24 hrs, whereas that from a conventional suppository reached 85%. An in vivo experiment with rabbits showed that IDM-PVP-SDS hollow type suppository delayed the absorption of IDM, significantly. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of IDM-PVP-SDS suppository were 60 min, 12.12${\mu}g$/ml and 2657${\mu}g$/ml/min, respectively. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of controlled group were 20 min, 15.49${\mu}g$/ml and 2190${\mu}g$/ml/min, respectively.

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Controlled Release of Fluorouracil from Sodium Alginate Matrices (알긴산나트륨 마트릭스로부터 플루오로우라실의 제어 방출)

  • Kim, Sung-Ho;Jung, Yong-Jae;Ha, Chung-Hun
    • Journal of Pharmaceutical Investigation
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    • v.22 no.2
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    • pp.149-153
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    • 1992
  • The applicability of sodium alginate as a carrier of 5-fluorouracil as an oral delivery system was investigated. Hydrophobicity of sodium alginate was controlled by introducing cetyl group to this polymer. The effects of degree of esterification for n-cetyl partial ester on the rate of release of 5-fluorouracil in artificial gastric juice and artificial intestinal juice were examined. The release rete of the drug in the gastric juice was mainly affected by the diffusion of the drug. The release rate of the drug in the intestinal juice could be controlled by the degree of esterification. The alginate matrices may be a valuable addition as the carrier of 5-fluorouracil for an oral delivery system.

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Regulation of Mitogen-activated Protein Kinases by Translatoinally Controlled Tumor Protein in PC12 Cells (PC12 세포주에서 Translationally Controlled Tumor Protein에 의한 Mitogen-activated Protein Kinases 활성 조절)

  • Kim, Mi-Yeon;Kim, Mi-Young
    • YAKHAK HOEJI
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    • v.54 no.5
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    • pp.323-327
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    • 2010
  • Translationally controlled tumor protein (TCTP) activates basophils to release histamine and causes chronic inflammation. It was also reported that TCTP significantly reduced in brain of Alzheimer's Disease and Down Syndrome as compared to normal person, suggesting that TCTP might be involved in cognitive function. We wondered whether TCTP could act as a general inducer in neurotransmitters release in brain. We, therefore, investigated the role of TCTP in PC12 cell line which expressed neuronal properties. We found that TCTP could activate JNK, and the activity was inhibited by pretreatment of dicoumarol, a JNK inhibitor. However, TCTP could not activate ERK that has known to be involved in neurotransmitter release. These suggest TCTP did not participate in neurotransmitter release from PC12 cells, and TCTP might not be a general inducer in neurotransmitter release.

Nanocellulose Applications for Drug Delivery: A Review

  • Lee, Seung-Hwan;Kim, Hyun-Ji;Kim, Jin-Chul
    • Journal of Forest and Environmental Science
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    • v.35 no.3
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    • pp.141-149
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    • 2019
  • Nanocellulose, which can exist as either cellulose nanocrystals or cellulose nanofibrils, has been used as a biomaterial for drug delivery owing to its non-immunogenicity, biocompatibility, high specific area, good mechanical properties, and variability for chemical modification. Various water-soluble drugs can be bound to and released from nanocelluloses through electrostatic interactions. The high specific surface area of nanocellulose allows for high specific drug loading. Additionally, a broad spectrum of drugs can bind to nanocellulose after facile chemical modifications of its surface. Controlled release can be achieved for various pharmaceuticals when the nanocellulose surface is chemically modified or physically formulated in an adequate manner. This review summarizes the potential applications of nanocelluloses in drug delivery according to published studies on drug delivery systems.

Dissolution of Chlorpheniramine Mallate (CMP) from Sustained-Release Tablets Containing CPM in the Coated Film Layer (핵정(核鐘)에 코팅된 필름층 중에 함유되어 있는 말레인산클로르페니라민의 방출특성)

  • Yu, Jei-Man;Shim, Chang-Koo;Lee, Min-Hwa;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.20 no.2
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    • pp.89-95
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    • 1990
  • Ethylcellulose-PEG 4000 film coated on core tablets was investigated as a potential drug delivery system for the controlled release of chlorpheniramine maleate (CPM). The kinetic analysis of the release data indicated that CPM release followed a diffusion-controlled model, where the quantity released per unit area is proportional to the square root of time. The effect of the film composition, CPM concentration, plasticizer concentration and CPM solubility on the release characteristics were examined. The release rate constant increased as CPM concentration increased. It also increased as the PEG 4000 content in the film increased above 10%(w/w), however, it decreased as the PEG 4000 content increased in the concentration range below 10%(w/w). The release rate constant was not affected by the coated weight on the core tablet. The film-coated tablets which contain CPM only in the coated film layer seemed to be a potential oral drug delivery system for the controlled release of CPM.

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Drug Release Characteristics of Biodegradable Polymers for Stent Coating (스텐트 코팅용 생분해성 고분자의 약물 방출 특성)

  • 강혜수;김진설;김동운;강병철;이봉희;김범수
    • KSBB Journal
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    • v.18 no.2
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    • pp.107-110
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    • 2003
  • Biodegradable polymers, poly(lactic-co-glycolic acid) (PLGA), poly(3-hydroxybutyrate) (PHB), and medium chain length polyhydroxyalkanoates (MCL-PHA) containing rose bengal (model drug) were coated onto the surface of stainless steel (stent materials) and their in vitro release characteristics were investigated. Drug release increased with; decreasing PLGA concentration, increasing rose bengal concentration, and Increasing dip-coating duration. The order of drug release from the polymer coating was: PHB > PLGA > MCL-PHA. These results suggest that drug release can be controlled by: changing the concentration and type of polymer, the drug concentration, and the dip-coating duration.