• 제목/요약/키워드: sustained release

검색결과 354건 처리시간 0.022초

PLGA 나노파티클의 Plasmid DNA 봉입: 폴록사머와 온도의 영향 (Encapsulation of Plasmid DNA in PLGA Nanoparticles: Effects of Poloxamer and Temperature)

  • 강현숙;류상화;명창선;황성주;박정숙
    • Journal of Pharmaceutical Investigation
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    • 제37권1호
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    • pp.39-43
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    • 2007
  • Previously, we have reported that PLGA nanoparticles were prepared for sustained release of water-soluble blue dextran and the particle size, in vitro release pattern and encapsulation were modulated by varying polymers. This study was designed to encapsulate plasmid DNA in PLGA nanoparticles and to investigate the effect of Polymers and temperatures. PLGA nanoparticles were fabricated with poloxamer 188 (P188) or poloxamer 407 (P407) by using spontaneous emulsification solvent diffusion method. As a model plasmid DNA, pCMV-Taq2B/1L-18 was encapsulated in PLGA nanoparticles. Then, the particle size, zeta potential and encapsulation efficiency of nanoparticles containing plasmid DNA were investigated. Particle sizes of PLGA nanoparticles prepared with P188 and P407 were in the range of 200-330 nm and 250-290 nm, respectively. Zeta potentials of nanoparticles were negative regardless of nanoparticle compositions. Encapsulation efficiency of P407 nanoparticles prepared at $30^{\circ}C$ was higher than those at other preparation condition. From the results, the PLGA nanoparticles prepared with poloxamers at different temperature, could modulate the particles size of nanoparticles, and encapsulation efficiency of plasmid DNA.

Enhanced Transdermal Delivery of Pranoprofen from the Bioadhesive Gels

  • Shin, Sang-Chul;Cho, Cheong-Weon
    • Archives of Pharmacal Research
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    • 제29권10호
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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.

연소실 길이에 따른 이중선회 가스터빈 모델 연소기에서 연소불안정 모드 연구 (A Study of Combustion Instability Mode according to the Variation of Combustor Length in Dual Swirl Gas Turbine Model Combustor)

  • 장문석;이기만
    • 한국연소학회지
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    • 제21권2호
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    • pp.29-37
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    • 2016
  • This study described the experimental investigations of combustion instability in a model gas turbine combustor. Strong coupling between pressure oscillations and unsteady heat release excites a self-sustained acoustic wave, which results in a loud and annoyed sound, and may also lead to a structural damage to the combustion system. In this study, in order to examine the combustion instability phenomenon of a dual swirling combustor configuration, the information of heat release and pressure fluctuation period with respect to the variation in both thermal power and combustor length was collected experimentally. As a result, the fundamental acoustic frequency turned out to increase with the increasing thermal power without respect to the combustor length. The frequency response to the combustor length was found to have two distinct regimes. In a higher power regime the frequency significantly decreases with the combustor length, as it is expected from the resonance of gas column. However, in a lower power regime it is almost insensitive to the combustor length. This insensitive response might be a result of the beating phenomenon between the interacting pilot and main flames with different periods.

Echinacoside, an active constituent of Herba Cistanche, suppresses epileptiform activity in hippocampal CA3 pyramidal neurons

  • Lu, Cheng-Wei;Huang, Shu-Kuei;Lin, Tzu-Yu;Wang, Su-Jane
    • The Korean Journal of Physiology and Pharmacology
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    • 제22권3호
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    • pp.249-255
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    • 2018
  • Echinacoside, an active compound in the herb Herba Cistanche, has been reported to inhibit glutamate release. In this study, we investigated the effects of echinacoside on spontaneous excitatory synaptic transmission changes induced by 4-aminopyridine (4-AP), by using the in vitro rat hippocampal slice technique and whole-cell patch clamp recordings from CA3 pyramidal neurons. Perfusion with echinacoside significantly suppressed the 4-AP-induced epileptiform activity in a concentration-dependent manner. Echinacoside reduced 4-AP-induced increase in frequency of spontaneous excitatory postsynaptic currents (sEPSCs) but it did not affect the amplitude of sEPSCs or glutamate-activated currents, implicating a presynaptic mechanism of action. Echinacoside also potently blocked sustained repetitive firing, which is a basic mechanism of antiepileptic drugs. These results suggest that echinacoside exerts an antiepileptic effect on hippocampal CA3 pyramidal neurons by simultaneously decreasing glutamate release and blocking abnormal firing synchronization. Accordingly, our study provides experimental evidence that echinacoside may represent an effective pharmacological agent for treating epilepsy.

외측 상완 유리 피판을 이용한 양측 제1수지간 중증 화상 반흔 구축의 재건 (Lateral Arm Free Flap Reconstruction in a Patient with Severe Burn Scar Contracture of the Bilateral First Web Space)

  • 윤태근;은석찬
    • 대한화상학회지
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    • 제24권2호
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    • pp.46-49
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    • 2021
  • An anatomically normal first web space is essential for optimal prehensile movements of the thumb and hand. A 28-year-old woman presented with severe scarring and contractures of the first web space of both hands, following a flame burn injury sustained 25 years prior to presentation. First web space contracture may occur secondary to severe injuries, burns (as observed in our patient), or congenital hand anomalies. A significant amount of additional skin is required to release a severe first web space contracture. Reconstruction of wide areas of contractures using only local flaps is challenging. Among other free flaps used in clinical practice, the thinned lateral arm free flap provides flexible vascularized tissue for reconstruction of the skin after severe first web space contracture release. Reconstruction using lateral arm free flaps facilitated thumb abduction and opposition (which were initially difficult) and improved hand function in our patient.

SIS로 개질된 PLGA 담체에서의 단백질의 서방화 (Sustained Release of Proteins Using Small Intestinal Submucosa Modified PLGA Scaffold)

  • 고연경;최명규;김순희;김근아;이해방;이종문;강길선
    • 폴리머
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    • 제32권3호
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    • pp.199-205
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    • 2008
  • 단백질 및 펩타이드의 서방형 약물전달체로서 소장점막하조직(SIS)으로 개질된 PLGA 담체를 제조하고자 하였으며, SIS/PLGA 담체는 용매 캐스팅/염 추출법에 의해 준비된 PLGA 담체에 SIS 용액을 첨가하여 단순 함침방법으로 제조하였다. 본 실험에서 사용된 돼지의 소장 점막층에서 유래된 SIS는 면역거부반응이 적어 생체재료로 널리 사용되고 있다. 제조된 PLGA 및 SIS/PLGA 담체를 SEM을 통한 표면 및 내부 관찰결과 두 담체 모두 열린 다공구조를 이루며, 특히 SIS/PLGA 담체는 PLGA 담체의 다공 내부에 SIS가 침투되어 작은 네트워크를 형성하고 있음을 확인하였다. 또한 단백질의 방출경향을 확인하기 위하여 형광이 결합된 소 혈청 알부민(FITC-BSA)을 PLGA 및 SIS/PLGA 담체에 담지시킨 후, 형광광도계를 통해 이들의 방출거동을 확인하였다. PLGA 담체와 비교할 때 SIS/PLGA 담체에서의 BSA의 방출은 초기방출량이 적고 지속적으로 일정량이 방출되는 거동을 확인할 수 있었으며 함량별 BSA 농도에 따른 SIS/PLGA 담체에서의 방출은 BSA의 양이 증가할수록 빠르고 많은 양이 방출되는 경향성 있는 방출패턴을 보임을 확인하였다. 결론적으로 PLGA 담체에 침투한 SIS 젤이 BSA의 급격한 초기방출을 억제하며, SIS로 개질된 PLGA 담체는 방출조절이 가능한 약물전달체로서 매우 유용할 것으로 사료된다.

약물 방출 시스템으로서 이부프로펜/클레이 유-무기 나노복합체의 층간삽입 거동 연구 (Intercalation behavior study of ibuprofen/clay organic-inorganic nanocomposites as drug release system)

  • 최봉석;김동현;김태완;진형호;박홍채;윤석영
    • 한국결정성장학회지
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    • 제21권6호
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    • pp.240-245
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    • 2011
  • 본 연구는 지속적 약물방출 전달체로서의 클레이 내의 재결정화 된 이부프로펜 층간삽입 거동에 대해 주안점을 두었다. 이부프로펜의 층간삽입 거동은 X-선 회절 및 열 중량 분석을 통해 확인하였다. 클레이의 기저 공간은 이부프로펜 분자에 의해 1.2 nm에서 1.5 nm까지 증가하였다. 또한 클레이 내부 공간 층에 존재하는 이부프로펜의 부분 운동은 이부프로펜/클레이 나노복합체의 열적 안정성을 증가시켰다. 나노복합체의 in vitro 약물방출 결과는 이부프로펜이 클레이로부터 일정하게 방출됨을 보였다.

탈분극과 근장그물 내 $Ca^{2+}$ 고갈-유도 평활근의 수축 및 세포 내 $Ca^{2+}$ 변동에 관여하는 L-형 $Ca^{2+}$ 통로의 상관성 (The Relationship of the L-type $Ca^{2+}$ Channel on the Depolarization-and Depletion of SR $Ca^{2+}$ -induced Smooth Muscle Contraction and Intracellular $Ca^{2+}$ Mobilization)

  • 김중환
    • The Journal of Korean Physical Therapy
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    • 제19권5호
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    • pp.65-76
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    • 2007
  • Purpose: It is generally accepted that smooth muscle contraction is triggered by intracellular $Ca^{2+}$ ($[Ca^{2+}]_i$) released from intracellular $Ca^{2+}$ stores such as sarcoplasmic teticulum (SR) and from the extracellular space. The increased $[Ca^{2+}]^i$ can phosphorylate the 20,000 dalton myosin light chain $(MLC_{20})$ by activating MLC kinase (MLCK), and this initiates smooth muscle contraction. In addition to the $[Ca^{2+}]_i$MACK-tension pathway, a number of intracellular signal molecules, including mitogen-activated protein kinase (MAPK), protein kinase C (PKC) and others, play important roles in the regulation of smooth muscle contraction. However, the mechanisms regulating contraction of depletion of SR $Ca^{2+}$ in mouse gastric smooth muscle strips is not still clear. Methods: To investigate the rotes of $Ca^{2+}$ influx and SR $Ca^{2+}$ release channel on gastric motility, isometric contraction and $[Ca^{2+}]_i$ were examined in mouse gastric smooth muscle strips. Results: High KCl, ryanodine, an activator of $Ca^{2+-}$induced $Ca^{2+}$ release channel, and cyclopiazonic acid (CPA), an inhibitor of SR $Ca^{2+-}$ATPase evoked a sustained increase in muscle contraction and $[Ca^{2+}]_i$. These increases induced by high KCl, ryanodine, and CPA were partially blocked by application of verapamil ($10{\mu}M$), a L-type $Ca^{2+}$ channel inhibitor. Additionally, in $Ca^{2+-}$free solution (1 mM EGTA), ryanodine and CPA had no effect contraction and $[Ca^{2+}]_i$ in fundic muscle strips. Conclusion: These results that extracellular $Ca^{2+}$ influx and depletion of SR trigger $Ca^{2+}$ influx through verapamil-sensitive $Ca^{2+}$ channel, and extracellular and SR $Ca^{2+}$ store may functionally involve in the subcellular $Ca^{2+}$ mobilization in mouse gastric muscle.

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Topical Delivery of Budesonide Emulsion Particles in the Presence of PEO-PCL-PEO Triblock Copolymers

  • Cho, Jin-Hun;Baek, Hyon-Ho;Lee, Jung-Min;Kim, Jung-Hyun;Kim, Dae-Duk;Cho, Heui-Kyoung;Cheong, In-Woo
    • Macromolecular Research
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    • 제17권12호
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    • pp.969-975
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    • 2009
  • This article describes the topical delivery and localization of budesonide through the hairless mouse skin. Two poly(ethylene oxide)-block-poly($\varepsilon$-caprolactone)-block-poly(ethylene oxide) (PEO-PCL-PEO) triblock copolymers (T 222 and T 252) having different CL:EO ratios were added in the preparation of budesonide particles stabilized with poly(vinyl alcohol) (PVA) and Tween 80 under ultrasonication. For comparison, a commercial PEO-PPO-PEO triblock copolymer (F68) was studied under the same condition. To demonstrate the effects of the triblock copolymer, the particle size of budesonide emulsion, entrapment efficiency, and in vitro release were measured and compared. The budesonide particles stabilized by the triblock copolymers had a diameter of ca. 350 nm with entrapment efficiencies of 66-76%. The In vitro release profiles of all samples showed an initial burst followed by sustained release. The skin penetration and permeation of budesonide were analyzed by using a Frantz diffusion cell. T 222 and T 252 exhibited higher total permeation amounts, but lower budesonide penetration amounts, than F68. The results suggest that the partitioning of budesonide in each skin layer can be adjusted in order to avoid skin thinning and negative immune response arising from the penetration of budesonide in blood vessels.

Preparation and Stability Evaluation of Docetaxel-Loaded Oral Liposome

  • Chon, Chong-Run;Kim, Hyun-Mi;Lee, Pung-Sok;Oh, Eui-Chaul;Lee, Ma-Se
    • Journal of Pharmaceutical Investigation
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    • 제40권2호
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    • pp.85-90
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    • 2010
  • Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.