• 제목/요약/키워드: Site release

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하이드록시아파타이트 코팅 리포솜의 초음파에 의한 약물방출 (Ultrasound-Triggered Drug Release of Hydroxyapatite Coated Liposomes)

  • 조성근;위태인;하정;조선행;한건;한희동;신병철
    • 대한화학회지
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    • 제57권4호
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    • pp.493-498
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    • 2013
  • 리포솜은 표적 약물을 봉입하여 병소에 안전하게 전달할 수 있는 약물전달체로서 연구되고 있다. 그러나 일반적인 리포솜은 표적부위에서 약물방출이 제한적인 문제점이 있다. 따라서 본 연구에서는 리포솜의 안정성을 향상시키고 표적부위에서 외부 초음파로부터 약물의 방출을 극대화시키기 위하여 하이드록시아파타이트(hydroxyapatite, HA)가 코팅된 리포솜을 개발하였다. 대조군 리포솜은 인지질과 콜레스테롤을 이용하여 제조하였고, 대조군 리포솜의 표면에 칼슘 아세테이트, 포스포릭에시드, 그리고 25% 암모니아용액을 이용하여 HA를 코팅하였다. 모델 약물로는 독소루비신을 사용하였다. HA코팅 리포솜의 크기는 120 nm 이었고, 약물봉입효율은 95% 이상이었다. 30% 혈장용액 내에서 HA코팅 리포솜의 입자크기는 일정한 상태를 유지하였으며, 대조군 리포솜은 크기가 1.4배 증가하였다. 외부 초음파 자극에 의한 리포솜으로부터 약물 방출을 유도한 후, 방출된 약물의 세포 이입율은 HA 코팅된 리포솜이 3배 이상 대조군 리포솜에 비하여 증가하였다. 본 연구에서는 외부 초음파 자극에 의하여 리포솜으로부터 약물의 방출을 극대화시키기 위한 초음파 민감형 리포솜을 개발하였고, 본 제형은 표적부위에서 약물의 방출을 효과적으로 제어하기 위한 분야에 활용이 가능할 것이다.

A STUDY ON METHODOLOGY FOR IDENTIFYING CORRELATIONS BETWEEN LERF AND EARLY FATALITY

  • Kang, Kyungmin;Jae, Moosung;Ahn, Kwang-Il
    • Nuclear Engineering and Technology
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    • 제44권7호
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    • pp.745-754
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    • 2012
  • The correlations between Large Early Release Frequency (LERF) and Early Fatality need to be investigated for risk-informed application and regulation. In Regulatory Guide (RG) -1.174, while there are decision-making criteria using the measures of Core Damage Frequency (CDF) and LERF, there are no specific criteria on LERF. Since there are both huge uncertainties and large costs needed in off-site consequence calculation, a LERF assessment methodology needs to be developed, and its correlation factor needs to be identified, for risk-informed decision-making. A new method for estimating off-site consequence has been presented and performed for assessing health effects caused by radioisotopes released from severe accidents of nuclear power plants in this study. The MACCS2 code is used for validating the source term quantitatively regarding health effects, depending on the release characteristics of radioisotopes during severe accidents. This study developed a method for identifying correlations between LERF and Early Fatality and validates the results of the model using the MACCS2 code. The results of this study may contribute to defining LERF and finding a measure for risk-informed regulations and risk-informed decision-making.

Identification of binding motifs for skeletal ryanodine receptor and triadin

  • Lee, Jae-Man;Kim, Do-Han
    • 한국생물물리학회:학술대회논문집
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    • 한국생물물리학회 2003년도 정기총회 및 학술발표회
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    • pp.66-66
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    • 2003
  • In skeletal muscle cells, depolarization of the transverse tubules (T-tubules) results in Ca$\^$2+/ release from the sarcoplasmic reticulum (SR), leading to elevated cytoplasmic Ca$\^$2+/ and muscle contraction. This process has been known as excitation-contraction coupling (E-C coupling). Several proteins, such as the ryanodine receptor (RyR), triadin, junctin, and calsequestrin (CSQ), have been identified to be involved in the Ca$\^$2+/ release process. However, the molecular interactions between the SR proteins have not been resolved. In the present study, the mechanisms of interaction between RyRl and triadin have been studied by in vitro protein binding and $\^$45/Ca$\^$2+/ overlay assays. Our data demonstrate that the intraluminal loop II of RyR1 binds to triadin in Ca$\^$2+/-independent manner. Moreover, we could not find any Ca$\^$2+/ binding sites in the loop II region. GST-pull down assay revealed that a KEKE motif of triadin, which was previously identified as a CSQ binding site (Kobayasi et al.,2000 JBC) was also a binding site for RyR1. Our results suggest that the intraluminal loop II of RyR could participate in the RyR-mediated Ca$\^$2+/ release process by offering a direct binding site to luminal triadin.

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Modeling of the Environmental Behavior of Tritium Around the Nuclear Power Plants

  • Park, Heui-Joo;Lee, Hansoo;Kang, Hee-Suk;Park, Yong-Ho;Lee, Chang-Woo
    • Nuclear Engineering and Technology
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    • 제34권3호
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    • pp.242-249
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    • 2002
  • The relationship between the tritium release rate from the nuclear power plant and tritium concentration in the environment around the Kori site was modeled. The tritium concentration in the atmosphere was calculated by multiplying the release rates and $\chi$/Q values, and the d3V deposition rate at each sector according to the direction and the distance was obtained using a dry deposition velocity. The area around Kori site was divided into 6 zones according to the deposition rate. The six zones were divided into 14 compartments for the numerical simulation. Transfer coefficients between the compartments were derived using site characterization data. Source terms were calculated from the dry deposition rates. Tritium concentration in surface soil water and groundwater was calculated based upon a compartment model. The semi-analytical solution of the compartment model was obtained with a computer program, AMBER. The results showed that most of tritium deposited onto the land released into the atmosphere and the sea. Also, the estimated concentration in the top soil agreed well to that measured. Using the model, tritium concentration was predicted in the case that the tritium release rates were doubled.

Novel approach to predicting the release probability when applying the MARSSIM statistical test to a survey unit with a specific residual radioactivity distribution based on Monte Carlo simulation

  • Chun, Ga Hyun;Cheong, Jae Hak
    • Nuclear Engineering and Technology
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    • 제54권5호
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    • pp.1606-1615
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    • 2022
  • For investigating whether the MARSSIM nonparametric test has sufficient statistical power when a site has a specific contamination distribution before conducting a final status survey (FSS), a novel approach was proposed to predict the release probability of the site. Five distributions were assumed: lognormal distribution, normal distribution, maximum extreme value distribution, minimum extreme value distribution, and uniform distribution. Hypothetical radioactivity populations were generated for each distribution, and Sign tests were performed to predict the release probabilities after extracting samples using Monte Carlo simulations. The designed Type I error (0.01, 0.05, and 0.1) was always satisfied for all distributions, while the designed Type II error (0.01, 0.05, and 0.1) was not always met for the uniform, maximum extreme value, and lognormal distributions. Through detailed analyses for lognormal and normal distributions which are often found for contaminants in actual environmental or soil samples, it was found that a greater statistical power was obtained from survey units with normal distribution than with lognormal distribution. This study is expected to contribute to achieving the designed decision error when the contamination distribution of a survey unit is identified, by predicting whether the survey unit passes the statistical test before undertaking the FSS according to MARSSIM.

Experimental Study on Sustained-release 5-Fluorouracil Implantation in Canine Peritoneum and Para-aortic Abdominalis

  • Wei, Guo;Nie, Ming-Ming;Shen, Xiao-Jun;Xue, Xu-Chao;Ma, Li-Ye;Du, Cheng-Hui;Wang, Shi-Liang;Bi, Jian-Wei
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권1호
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    • pp.407-411
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    • 2014
  • Objective: To observe local and systemic toxicity after sustained-release 5-fluorouracil (5-Fu) implantation in canine peritoneum and para-aortic abdominalis and the changes of drug concentration in the local implanted tissue with time. Methods: 300 mg sustained-release 5-Fu was implanted into canine peritoneum and para-aorta abdominalis. Samples were taken 3, 5, 7 and 10 days after implantation for assessment of changes and systemic reactions. High performance liquid chromatography was applied to detect the drug concentrations of peritoneal tissue at different distances from the implanted site, lymphatic tissue of para-aortic abdominalis, peripheral blood and portal venous blood. Results: 10 days after implantation, the drug concentrations in the peritoneum, lymphatic tissue and portal vein remained relatively high within 5 cm of the implanted site. There appeared inflammatory reaction in the local implanted tissue, but no visible pathological changes such as cell degeneration and necrosis, and systemic reaction like anorexia, nausea, vomiting and fever. Conclusions: Sustained-release 5-Fu implantation in canine peritoneum and para-aortic abdominalis can maintain a relatively high tumour-inhibiting concentration for a longer time in the local implanted area and portal vein, and has mild local and systemic reactions. Besides, it is safe and effective to prevent or treat recurrence of gastrointestinal tumours and liver metastasis.

삼차신경 감각핵의 신경전달물질 유리에 대한 수 종 약물의 효과 (EFFECTS OF A VARIOUS DRUGS ON THE RELEASE OF NEUROTRANSMITTERS FROM TRIGEMINAL SENSORY NUCLEUS)

  • 윤정혜;이명종
    • Restorative Dentistry and Endodontics
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    • 제20권2호
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    • pp.423-431
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    • 1995
  • Trigeminal spinal sensory nucleus is a main relay site in transmission of orofacial pain. Glutamate and aspartate playa role in transmission of primary afferents. This experiment was performed to study the role of capsaicin, KR-25018 and shogaol on the release of glutamate and aspartate from trigeminal spinal sensory nucleus. Release of excitatory amino acids(EAAs) was induced by electrical stimulation of oral mucosa with innocuous or noxious stimuli. Capsaicin($10{\mu}M$), KR-25018($10{\mu}M$), shogaol($10{\mu}M$), ruthenium red and capsazapine were added to perfusion solution to observe the changes in EAA release, and glutamate and aspartate were determined by HPLC. Release of glutamate and aspartate from trigeminal sensory nucleus was increased by noxious stimulation of oral mucosa, but innocuous stimulation did not affect on the release of EAA Capsaicin and KR-25018 increased the release of glutamate and aspartate, and effect of KR-25018 on release of EAA was more potent than capsaicin. But shogaol had a weak effect on release of EAA. Effect of capsaicin and KR-25018 was partially blocked by capsaicin antagonists, ruthenium red and capsazepine.

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Accumulation and Release of Heavy Metals (Cu, Zn, Cd and Pb) in the Mussel, Mytilus galloprovincialis; Reciprocal Transplantation Experiment

  • Kim, Chan kook;Choi, Man Sik;Lee, Chang-Bok
    • Journal of the korean society of oceanography
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    • 제39권3호
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    • pp.197-206
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    • 2004
  • Mussel, Mytilus galloprovincialis, was transplanted reciprocally between contaminated site (St. STP) and relatively less contaminated site (St. UB) in Onsan Bay, Korea in order to estimate heavy metal accumulation and release. Transplanted and indigenous mussels were collected 8 times over 108 days deployment at both sites and analyzed for Cd, Cu, Pb and Zn using ICP/MS. Cu and Zn concentration did not show any significant differences between transplanted and indigenous mussels throughout the experiment period, although dissolved Cu and Zn concentrations in seawater were significantly higher at contaminated site. Pb accumulated rapidly, while Cd did not show any accumulation in the mussels transplanted from St. UB to St. STP. These accumulation patterns might reflect the variation of dissolved metal concentration; dissolved Pb concentration was significantly higher in St. STP than St. UB, while dissolved Cd concentration was similar between both sites throughout this experiment. Release of Cd and Pb in the mussels transplanted from St. STP to St. UB was not significant during the transplantation period. The levels and variation of Pb and Cd concentrations in mussels transplanted from St. STP to St. UB were similar to those in the indigenous mussels at St. STP throughout the period. Therefore, Cd and Pb accumulated in indigenous mussels may indicate the integrated metals throughout their lives, not responding to the present status of seawater because the release of accumulated metals in mussels occurs very slowly when the seawater metal levels are lowered. On the other hand, since the transplanted mussels can respond immediately to the levels of metals in seawater, it may be suggested that the present status of heavy metals in seawater can be only acquired from the metal levels of mussels transplanted from clean environments.

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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    • 제28권9호
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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.

Monte Carlo 방법을 이용한 대기오염 배출률 예측의 불확실성 평가 (Uncertainty Evaluation of the Estimated Release Rate for the Atmospheric Pollutant Using Monte Carlo Method)

  • 정효준;김은한;서경석;황원태;한문희
    • 한국환경과학회지
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    • 제15권4호
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    • pp.319-324
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    • 2006
  • Release rate is one of the important items for the environmental impact assessment caused by radioactive materials in case of an accidental release from the nuclear facilities. In this study, the uncertainty of the estimated release rate is evaluated using Monte Carlo method. Gaussian plume model and linear programming are used for estimating the release rate of a source material. Tracer experiment is performed at the Yeoung-Kwang nuclear site to understand the dispersion characteristics. The optimized release rate was 1.56 times rather than the released source as a result of the linear programming to minimize the sum of square errors between the observed concentrations of the experiment and the calculated ones using Gaussian plume model. In the mean time, 95% confidence interval of the estimated release rate was from 1.41 to 2.53 times compared with the released rate as a result of the Monte Carlo simulation considering input variations of the Gaussian plume model. We confirm that this kind of the uncertainty evaluation for the source rate can support decision making appropriately in case of the radiological emergencies.