• 제목/요약/키워드: controlled drug release

검색결과 261건 처리시간 0.023초

별아교세포 선택적 유전자 치료전달을 위한 PLGA 나노입자 개발 (Development of PLGA Nanoparticles for Astrocyte-specific Delivery of Gene Therapy: A Review)

  • 신효정;이가영;권기상;권오유;김동운
    • 생명과학회지
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    • 제31권9호
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    • pp.849-855
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    • 2021
  • 최근에는 나노기술이 다양한 분야에 도입되고 활용되면서 신약개발이 가속화되고 있다. 나노입자는 약물의 단일 투여로 장기간 동안 혈중 약물 농도를 유지하고, 병리학적 부위에만 선택적으로 방출되는 장점이 있어 비병리 주위에 대한 부작용을 줄일 수 있다. Poly (D,L-lactic-co-glycolic acid) (PLGA)는 가장 광범위하게 개발된 생분해성 고분자 중 하나이다. PLGA는 다양한 응용분야의 약물전달에 널리 사용된다. 또한 FAD에 의해 약물전달 시스템으로 승인되었으며, 유전자 치료제와 같은 제어방출제형에 널리 적용된다. PLGA 나노입자는 수동 및 능동 표적화 방법을 사용하여 특정 세포 유형에 고효율의 전달 시스템으로 개발되었다. 이러한 PLGA 나노입자를 이용한 약물전달체 개발 후 표적 부위에 선택적으로 약물을 전달하고 질병에 따라 장기간 유효 혈중 농도를 최적화한다. 이 리뷰논문에서 우리는 유전자 치료를 위한 PLGA 나노 물질을 기반으로 하는 성상 세포 선택적 나노입자의 개발을 조사하여 세포 특이적으로 치료결과를 향상시키는 방법에 중점을 두고자 한다.

분무건조 방법으로 제조된 미립구에서 Sibutramine의 방출거동 (Sibutramine Release Behavior from Microspheres Prepared by Spray-Dry Method)

  • 박정수;오정수;오재민;김윤태;이준희;모종현;이해방;강길선
    • 폴리머
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    • 제32권3호
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    • pp.193-198
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    • 2008
  • 시부트라민은 비만을 치료하기 위한 식욕억제제로서 높은 결정성을 갖는 난용성 약물이다. 이러한 난용성 약물의 용해도를 증가시키기 위하여 고체분산법을 바탕으로 한 분무건조기를 이용하여 미립구를 제조할 수 있었다. 제조된 미립구는 주사전자현미경을 이용하여 제조시 사용한 용매에 따른 미립구 형태차이를 확인할 수 있었으며 용매증발 속도가 빠를수록 구형을 이루는 것을 확인할 수 있었다. X선 회절기를 이용하여 제조된 미립구에서 시부트라민의 결정성이 10%이하로 감소되었음을 확인하였다. 제조된 미립구는 pH 1.2와 pH 6.8에서 방출을 실시하였으며 시부트라민이 pH에 따라서 용해도 차이가 크다는 것을 확인하였다. 또한, 경필 캡슐을 이용한 것이 정제형태보다 방출이 약 4배 정도 빠르다는 것을 확인할 수 있었다. 이러한 결과를 바탕으로 제형의 형태에 따라 방출거동이 조절될 수 있음을 확인하였다.

Remifentanil-Propofol Sedation as an Ambulatory Anesthesia for Carpal Tunnel Release

  • Lee, Jae-Jun;Hwang, Sung-Mi;Jang, Ji-Su;Lim, So-Young;Heo, Dong-Hwa;Cho, Yong-Jun
    • Journal of Korean Neurosurgical Society
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    • 제48권5호
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    • pp.429-433
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    • 2010
  • Objective : This prospective study evaluated the use of continuous sedation using propofol and remifentanil when carpal tunnel release (CTR) was performed under local anesthesia. Methods : We sedated 60 patients undergoing CTR using local anesthesia with remifentanil at loading and continuous doses of $0.5\;{\mu}g\;kg^{-1}$ and $0.05\;{\mu}g\;kg^{-1}min^{-1}$, respectively, and propofol, using a target controlled infusion (TCI) pump set to a target of $2\;{\mu}g\;mL^{-1}$ (group A), or with the same drug doses except that the continuous remifentanil dose was $0.07\;{\mu}g\;kg^{-1}min^{-1}$ (group B) or $0.1\;{\mu}g\;kg^{-1}min^{-1}$ (group C). Results : In group B, the levels of pain when local anesthetics were administered (p = 0.001), intraoperative pain (p < 0.001) and anxiety (p = 0.001) were significantly lower than those of group A. Furthermore, the incidence of adverse events, including desaturation (p < 0.001) and vomiting (p = 0.043), was significantly lower in group B than in group C. Conclusion : Continuous sedation using an appropriate dose of remifentanil and propofol can be used as safe, efficacious ambulatory anesthesia in cases of CTR under local anesthesia, performed using only 2 mL of local anesthetic, with a high degree of patient satisfaction.

필로디핀이 함유된 미립구의 생체이용률 (Bioavailability of Microspheres Containing Felodipine)

  • 양재헌;나성범;김영일;김남순
    • 약학회지
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    • 제44권5호
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    • pp.440-447
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    • 2000
  • Microspheres of felodipine, which is one of the calcium channel blocker using a mixture of Eudragi $t^{R}$ RL, L, E, and cellulose on the base of Eudragi $t^{R}$ RS were investigated. Cremopho $r^{R}$ was added to each preparation of polymers in order to increase the release of felodipine from microspheres. Felodipine-loaded microspheres were prepared by a solvent evaporation method, which is based on dispersion of methylene chloride containing felodipine and polymers in 0.5 w/v % polyvinyl alcohol solution. The average diameter based on the size distribution of the felodipine-loaded microspheres was observed to be ca. 40-55 ${\mu}{\textrm}{m}$. A good and smooth surface were showed in all types of the microspheres. The amount of felodipine loaded was over 90 w/w % in all types of microspheres. The dissolution profiles of felodipine from microspheres were similar with each type of polymer, and about a 60 w/w % of the total amount of felodipine loaded to microsphere was released within 7 hours. Dissolution rate of felodipine from the microsphere was increased by addition of Cremophor. After oral administration of the felodipine-loaded microspheres in PVA solution and felodipine alone in PEG solution to rats, respectively, the pharmacokinetic study revealed that the Tmax values of the microspheres were observed in the range of 0.67~l.0 hr while that of the felodipine solution was obtained 0.33 hr. In addition, the AUC of the microspheres at 0 to 7 hr was remarkably increased in comparison to that of felodipine solution. These results revealed that the microspheres based on Eudragit RS could be a good candidate for the controlled release drug delivery system for felodipine.e.e.e.

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Docetaxel-loaded PLGA nanoparticles to increase pharmacological sensitivity in MDA-MB-231 and MCF-7 breast cancer cells

  • Tran, Phuong;Nguyen, Thu Nhan;Lee, Yeseul;Tran, Phan Nhan;Park, Jeong-Sook
    • The Korean Journal of Physiology and Pharmacology
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    • 제25권5호
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    • pp.479-488
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    • 2021
  • This study aimed to develop docetaxel (DTX) loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized. In vitro anticancer effect and cellular uptake were evaluated in breast cancer cells. The particle size and zeta potential of the DTX-NPs were 160.5 ± 3.0 nm and -26.7 ± 0.46 mV, respectively. The encapsulation efficiency and drug loading were 81.3 ± 1.85% and 10.6 ± 0.24%, respectively. The in vitro release of DTX from the DTX-NPs was sustained at pH 7.4 containing 0.5% Tween 80. The viability of MDA-MB-231 and MCF-7 cells with DTX-NPs was 37.5 ± 0.5% and 30.3 ± 1.13%, respectively. The IC50 values of DTX-NPs were 3.92- and 6.75-fold lower than that of DTX for MDA-MB-231 cells and MCF-7 cells, respectively. The cellular uptake of coumarin-6-loaded PLGA-NPs in MCF-7 cells was significantly higher than that in MDA-MB-231 cells. The pharmacological sensitivity in breast cancer cells was higher on MCF-7 cells than on MDA-MB-231 cells. In conclusion, we successfully developed DTX-NPs that showed a great potential for the controlled release of DTX. DTX-NPs are an effective formulation for improving anticancer effect in breast cancer cells.

Synthesis and Characterization of Thermosensitive Nanoparticles Based on PNIPAAm Core and Chitosan Shell Structure

  • Jung, Hyun;Jang, Mi-Kyeong;Nah, Jae-Woon;Kim, Yang-Bae
    • Macromolecular Research
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    • 제17권4호
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    • pp.265-270
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    • 2009
  • Noble thermosensitive nanoparticles, based on a PNIPAAm-co-AA core and a chitosan shell structure, were designed and synthesized for the controlled release of the loaded drug. PNIPAAm nanoparticles containing a carboxylic group on their surface were synthesized using emulsion polymerization. The carboxylic groups were conjugated with the amino group of a low molecular weight, water soluble chitosan. The particle size of the synthesized nanoparticles was decreased from 380 to 25 nm as the temperature of the dispersed medium was increased. Chitosan-conjugated nanoparticles with $2{\sim}5$ wt% MBA, a crosslinking monomer, induced a stable aqueous dispersion at a concentration of 1mg/1mL. The chitosan-conjugated nanoparticles showed thermo sensitive behaviors such as LCST and size shrinkage that were affected by the PNIPAAm core and induced some particle aggregation around LCST, which was not shown in the NIPAAm-co-AA nanoparticles. These chitosan-conjugated nanoparticles are also expected to be more biocompatible than the PNIPAAm core itself through the chitosan shell structures.

Synthesis of Microaglae-Capturing Magnetic Microcapsule Using CaCO3 Microparticles and Layer-by-Layer Coating

  • Lee, Young-Hee;Seo, Jung-Cheol;Oh, You-Kwan;Lee, Kyubock
    • 한국재료학회지
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    • 제28권7호
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    • pp.376-380
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    • 2018
  • Microalgae produce not only lipids for biodiesel production but also valuable biochemicals which are often accumulated under cellular stress mediated by certain chemicals. While the microcarriers for the application of drug delivery systems for animal cells are widely studied, their applications into microalgal research or biorefinery are rarely investigated. Here we develope dual-functional magnetic microcapsules which work not only as flocculants for microalgal harvesting but also potentially as microcarriers for the controlled release of target chemicals stimulating microalgae to enhance the accumulation of valuable chemicals. Magnetic microcapsules are synthesized by layer-by-layer(LbL) coating of PSS-PDDA on $Fe_3O_4$ nanoparticle-embedded $CaCO_3$ microparticles followed by removing $CaCO_3$ sacrificial templates. The positively charged magnetic microcapsules flocculate microalgae by electrostatic interaction which are sequentially collected by the magnetophoretic separation. The microcapsules with a polycationic outer layer provide efficient binding sites for negatively charged microalgae and by that means are further utilized as a chemical-delivery and flocculation system for microalgal research and biorefineries.

다중 전극에 전기 중합한 전도성 고분자를 이용한 선택적 약물방출 특성 (Characteristics of controlled drug release using conductive polymer electrochemically polymerized on multi-electrodes)

  • 송태은;장종현;손지회;양상식;박정호
    • 대한전기학회:학술대회논문집
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    • 대한전기학회 2004년도 추계학술대회 논문집 전기물성,응용부문
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    • pp.278-280
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    • 2004
  • 본 논문의 내용은 다중전극에 전기 중합한 전도성 고분자를 이용하여 약물을 결합한 후 전압 인가에 의한 선택적인 약물방출을 구현하는 것이다. Glass wafer에 anode와 cathode 전극을 제작하고 4개의 anode 전극면에 각각 전기중합으로 전도성 고분자막을 합성하였다. 양이온성 약물인 lidocaine을 결합할 수 있도록 피롤과 함께 도펀트로써 분자량이 큰 DBS를 사용하였으며 고분자막의 이온출입원리를 이용하여 약물을 결합하고 방출하였다. Cyclic voltammogram로부터 PPy(DBS) Polypyrrole (dodecylbenzene sulfonate) 전극의 산화 환원특성 및 전극면에 PPy(DBS) 막이 생성되기 위한 조건을 확인하였고, 그 결과를 토대로 PPy(DBS)막을 3전극 시스템과 Coulometry를 이용하여 전압을 인가하여 합성하였고, 합성전하량으로 부터 PPy(DBS)막의 두께를 알 수 있었다. Lidocaine의 결합 및 방출 시에도 정전압을 이용하였으며 약물의 방출 유무를 확인하기 위하여 UV spectrometer를 사용하였다. 다중전극에 PPy(DBS)막을 1.5um 두께로 합성한 후 lidocaine을 결합시키고 선택적으로 약물을 방출한 결과 각각의 PPy(DBS)막으로부터 $1.4{\sim}1.7mg$의 약물이 방출됨을 확인 할 수 있었다.

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술후 통증조절을 위한 새로운 대안으로서의 Oxycodone (Oxycodone: A New Therapeutic Option in Postoperative Pain Management)

  • 최병문
    • 대한치과마취과학회지
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    • 제13권4호
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    • pp.167-178
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    • 2013
  • Oxycodone is a semi-synthetic opioid synthesized from poppy-derived thebaine. It is a narcotic analgesic generally indicated for relief of moderate to severe pain. Although developed in an attempt to improve on the existing opioids, the adverse effects of oxycodone are those that are typically found in opioids. In recent years, the use of the opioid oxycodone has increased markedly and replacing morphine as the first line choice of opioid in several countries. There are formulations for oral immediate, oral extended release and intravenous use. In 2013, intravenous oxycodone was approved for marketing by Ministry of Food and Drug Safety (MFDS), with the indication of postoperative intravenous patient-controlled analgesia (IV PAC). Simulation study of oxycodone demonstrated that minimum effective analgesic concentration (MEAC) of oxycodone was most quickly reached with higher loading dose and IV PCA with background infusion, which may reduce the necessity of rescue analgesics during immediate postoperative period. Previous studies for postoperative pain management with intravenous oxycodone are limited in sample size, mostly less than 100 patients, which may not be large enough to assess safety of intravenous oxycodone. The effectiveness and tolerability of IV PCA with oxycodone should, therefore, be evaluated in large scale clinical trials in Korean populations.

Interleukin-6-producing paraganglioma as a rare cause of systemic inflammatory response syndrome: a case report

  • Yin Young Lee;Seung Min Chung
    • Journal of Yeungnam Medical Science
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    • 제40권4호
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    • pp.435-441
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    • 2023
  • Pheochromocytomas and paragangliomas (PPGLs) may secrete hormones or bioactive neuropeptides such as interleukin-6 (IL-6), which can mask the clinical manifestations of catecholamine hypersecretion. We report the case of a patient with delayed diagnosis of paraganglioma due to the development of IL-6-mediated systemic inflammatory response syndrome (SIRS). A 58-year-old woman presented with dyspnea and flank pain accompanied by SIRS and acute cardiac, kidney, and liver injuries. A left paravertebral mass was incidentally observed on abdominal computed tomography (CT). Biochemical tests revealed increased 24-hour urinary metanephrine (2.12 mg/day), plasma norepinephrine (1,588 pg/mL), plasma normetanephrine (2.27 nmol/L), and IL-6 (16.5 pg/mL) levels. 18F-fluorodeoxyglucose (FDG) positron emission tomography/CT showed increased uptake of FDG in the left paravertebral mass without metastases. The patient was finally diagnosed with functional paraganglioma crisis. The precipitating factor was unclear, but phendimetrazine tartrate, a norepinephrine-dopamine release drug that the patient regularly took, might have stimulated the paraganglioma. The patient's body temperature and blood pressure were well controlled after alpha-blocker administration, and the retroperitoneal mass was surgically resected successfully. After surgery, the patient's inflammatory, cardiac, renal, and hepatic biomarkers and catecholamine levels improved. In conclusion, our report emphasizes the importance of IL-6-producing PPGLs in the differential diagnosis of SIRS.