• Title/Summary/Keyword: Drug loading

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Effect of pH-dependent Solubility on Release Behavior of Alginate-Chitosan Blend Containing Activated Carbon

  • Oh, Ae-Ri;Jin, Dong-Hwee;Yun, Ju-Mi;Lee, Young-Seak;Kim, Hyung-Il
    • Carbon letters
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    • v.10 no.3
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    • pp.208-212
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    • 2009
  • Alginate-chitosan blend containing coconut-based activated carbon was prepared as a drug delivery carrier in order to improve the loading and releasing capacity of the drug. The activated carbon was incorporated as effective adsorbent for drug due to the extremely high surface area and pore volume, high adsorption capacity, micro porous structure and specific surface activity. Alginate-chitosan blend containing coconut-based activated carbon showed the sustained release for a longer period. Alginate-chitosan blend showed higher release of drug as the pH increased and higher release of drug as the content of chitosan decreased due to the pH-dependent solubility of blend components.

Preparation and Drug-releasing Properties of Chitosan-based Thermosensitive Composite Hydrogel

  • Li, Heping;Yu, Tao;Li, Shan;Qin, Long;Ning, Jingheng
    • 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.

Preparation and In Vivo Evaluation of Huperzine A-Loaded PLGA Microspheres

  • FU XU-DONG;GAO YONG-LIANG;PING QI-LENG;Ren Tang
    • Archives of Pharmacal Research
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    • v.28 no.9
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    • pp.1092-1096
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    • 2005
  • Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/w emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with $10\%$ released per day. Thereafter drug release rate became slow gradually and about $90\%$ drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4mg/kg and microspheres were intra­muscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration $(C_{max})$ after i.m. microspheres was only $32\%$ of that after i.m. solution. Drug in plasma could be detectd until day 14 and about $5\%$ of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was $94.7\%$. Inhibition of acyecholinesterase activity (AchE) in rat's cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

Enhanced Transdermal Delivery of Pranoprofen from the Bioadhesive Gels

  • Shin, Sang-Chul;Cho, Cheong-Weon
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.928-933
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    • 2006
  • Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at $32^{\circ}C$, $37^{\circ}C$ and $42^{\circ}C$ according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.

pH-Sensitive Curdlan Acetate Microspheres를 이용한 Indomethacin의 방출 특성

  • Lee, Chang-Mun;Lee, Yeong-Jin;Lee, Gi-Yeong;Choe, Chun-Sun
    • 한국생물공학회:학술대회논문집
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    • 2003.04a
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    • pp.739-742
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    • 2003
  • Curdlan acetate was prepared from hydrophilic curdlan by chemical modification and it was used for pH-sensitive drug delivery system. Curdlan acetate microspheres were prepared by the solvent evaporation method. The size of the curdlan acetate microspheres was below $200\;{\mu}m$. The drug loading efficiency of microspheres was approximately 58.44%. In the swelling test, curdlan acetate microspheres were showed pH-sensitive behavior. The swelling capacity of microspheres at pH 7.4 was much greater than at pH 1.4. Also, Release rate of indomethacin (IND) at pH 7.4 from curdlan acetate microspheres was faster than that at pH 1.4. A pH-sensitive drug release pattern was due to the disintegrating after swelling.

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Preparation and Drug Release Profiles of Solid Lipid Nanoparticles(SLN) (의약품의 Solid Lipid Nanoparticle의 제조 및 용출특성)

  • Yoo, Hye-Jong;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.26 no.2
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    • pp.125-135
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    • 1996
  • Solid lipid nanoparticles(SLN) are particulate systems for parenteral drug administration and suitable for controlled release. SLN were prepared by homogenization process. Dispersion at increased temperature (molten lipid) was performed to yield SLN loaded with lipophilic drugs. Tetracaine base, lidocaine base, prednisolone, methyltestosterone and ethinylestradiol were used as model drugs to access the loading capacity and to study the release behavior. To investigate production parameters(lipids, surfactant concentration, homogenizing rpm) in the formation of SLN, particle size was performed by laser diffraction analysis. The mean particle size of SLN with stearic acid or trilaurin was below 1 micron. By decreasing the particle size and increasing the surfactant concentration, the release rate was increased especially in the case of highly lipophilic drug loaded SLN. Methyltestosterone or ethinylestradiol loaded SLN showed a distinctly prolonged release over a few days.

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Controlled Release Behavior of Temperature Responsive Composite Hydrogel Containing Activated Carbon

  • Yun, Ju-Mi;Im, Ji-Sun;Jin, Dong-Hwee;Lee, Young-Seak;Kim, Hyung-Il
    • Carbon letters
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    • v.9 no.4
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    • pp.283-288
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    • 2008
  • The composites of temperature-sensitive hydrogel and activated carbons were prepared in order to improve both the mechanical strength of hydrogel matrix and the loading capacity of drug in a hydrogel drug delivery system. The swelling of composite hydrogel was varied depending on the temperature. Both the swelling and the release behavior of the composite hydrogel were varied depending on the kind of activated carbon. The release behavior showed the high efficiency which is important for practical applications.

Preparation and Characterization of Poly(D,L-lactic acid) Microspheres Containing Alprazolam (Alprazolam함유 poly(D,L-lactic acid) Microsphere의 제조 및 평가)

  • Yong, Chul-Soon;Kwon, Mi-Ra;Park, Sae-Hae;Oh, Doo-Man
    • Journal of Pharmaceutical Investigation
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    • v.26 no.1
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    • pp.13-22
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    • 1996
  • Poly(D,L-lactic acid) (PLA) microspheres containing alprazolam(APZ) were prepared by a solvent-emulsion evaporation method and their release patterns were investigated in vitro. Various batches of microspheres with different size and drug content were obtained by changing the ratio of APZ to PLA, PLA concentration in the dispersed phase and stirring rate. Rod-like APZ crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. The release rate of APZ for long-acting injectable delivery system in vitro, which would aid in predicting in vitro release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres.

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Drug Release Characteristics of Crosslinked Poly(alkylene oxide) Hydrogels (가교된 폴리 알킬렌 옥사이드 하이드로겔의 약물방출 특성)

  • Kim, Shin-Jeong;Lee, Seung-Jin
    • Journal of Pharmaceutical Investigation
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    • v.21 no.2
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    • pp.91-95
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    • 1991
  • Polyethylene glycol, polypropylene glycol and block copolymer of ethylene glycol and propylene glycol were crosslinked by triisocyanate to form water swellable, rubbery polymer. The equilibrium swelling of the hydrogels ranged from 3% to 60% according to the hydrophobic-hydrophilic properties of the prepolymers. Model drugs, sodium salicylate and prednisolone were incorporated in the polymer matrices by swelling loading. Physical properties of the drugs affected the drug release mechanisms due to the change in the swelling behaviors of the polymeric devices. Zero order release was observed in the case of relatively hydrophobic polymer matrices.

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