• Title/Summary/Keyword: 약물 표적

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간암 치료 신약 개발 및 이의 제제화 연구 (II. 제제화 연구)

  • 정홍석;최명준;장진수;황유경;안교한;이석종
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.251-251
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    • 1994
  • 1차년도에서 이미 확립한 다양한리포좀의 제조 방법에 따라간세포를표 적하기 위해 이들 리포좀의 조성에 galactocercbroside를 함유시켜 targeted liposomes을 제조하였다. 표적리포좀의 제조 방법에 따른 봉합율 (cncapsulation)과 안정성을 조사했을 때, freezing-thawing 과정을 거친 리포좀이 encapsulation 과 stability가 가장 뛰어남을 알 수 있었다. In vitro 간세포 표적능력을 in vitro cell culture system에서 간세포 cell line (Hep G2, 2.2.15과 다른 cell line (Vero E6, J82)에 대한 표적리포좀과 control liposomes의 uptake를 FTTC 또는 CF 형광으로 측정했을 때, 표적리포좀이 간세포 cell line에 더 많이 uptake하는 것을 알았다. In vivo 실험에서는 6 - 8 주령의 mouse tail vain에 표적리포좀과 control liposomes을 주사하여 각 장기에 존재하는 리포좀의 양을 형광으로 측정했을 때, 표적리포좀 (targetcd liposomes)이 다른 장기에 비해 liver에 선택적으로 많이 분포함을 알수있었다. 또한 간암의 효과적인 치료를 위해 간세포와 암세포를 동시에 표적할 수는 double targeting liposomes을 design 하였다.

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Pairwise Neural Networks for Predicting Compound-Protein Interaction (약물-표적 단백질 연관관계 예측모델을 위한 쌍 기반 뉴럴네트워크)

  • Lee, Munhwan;Kim, Eunghee;Kim, Hong-Gee
    • Korean Journal of Cognitive Science
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    • v.28 no.4
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    • pp.299-314
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    • 2017
  • Predicting compound-protein interactions in-silico is significant for the drug discovery. In this paper, we propose an scalable machine learning model to predict compound-protein interaction. The key idea of this scalable machine learning model is the architecture of pairwise neural network model and feature embedding method from the raw data, especially for protein. This method automatically extracts the features without additional knowledge of compound and protein. Also, the pairwise architecture elevate the expressiveness and compact dimension of feature by preventing biased learning from occurring due to the dimension and type of features. Through the 5-fold cross validation results on large scale database show that pairwise neural network improves the performance of predicting compound-protein interaction compared to previous prediction models.

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

  • Cho, Sung Keun;Wee, Tae In;Ha, Jeung;Cho, Sun Hang;Han, Kun;Han, Hee Dong;Shin, Byung Cheol
    • Journal of the Korean Chemical Society
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    • v.57 no.4
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    • pp.493-498
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    • 2013
  • Liposomes, which can deliver payload at target site, have been studied as drug carrier. However, conventional liposomes have limitation for drug release at target site. Therefore, we developed hydroxyapatite (HA) coated ultrasound sensitive liposomes to increase drug release at target site and to enhance stability in blood stream. Control liposome was prepared using hydrogenated soy phosphatidylcholine (HSPC) and cholesterol, and then we assessed HA coating on the surface of control liposomes using calcium acetate, phosphoric acid, and 25% ammonium solution. Doxorubicin was used as a model drug. Size of HA coated liposomes was 120 nm and encapsulation efficiency of doxorubicin in liposomes was up to 95%. Size of HA coated liposomes are not changed in 30% serum solution, however, the control liposomes was 1.4 fold increased. After ultrasound triggered drug release from liposomes, intracellular efficiency of drug released from HA coated liposomes was 3 fold increased compared to control liposomes. In this study, we developed ultrasound sensitive liposomes to enhance drug release, which will be applied in controlled drug release at disease site.

Targeted Drug Delivery Carriers Using Folate Conjugated Poly((R)-3-hydroxy butyrate)-Poly(ethylene glycol) Nanoparticles (Folate가 수식된 Poly((R)-3-hydroxy butyrate)-Poly(ethylene glycol) 나노입자를 이용한 표적지향형 약물전달체)

  • Kwon, Seung-Ho;Kim, Young-Jin
    • Polymer(Korea)
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    • v.33 no.6
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    • pp.515-519
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    • 2009
  • Biodegradable poly((R)-3-hydroxy butyrate) and poly(ethylene glycol) was conjugated to make amphiphilic di-block copolymer. Folate was conjugated at di-block copolymer to target the cancer cells. Copolymer was ready to form the self-assembled micelle whose size was 125~156 nm in aqueous solution. Griseofulvin as a hydrophobic drug was loaded in nanoparticles. Their loading efficiencies were 35~56%. Hydrophobic drug was continuously released for 24 h. Cell viability test showed that folate attached particles were 10% more efficient than the particles without targeting ligands.

Therapeutic efficacy of the photoactivated sickle cells as novel drug delivery vehicle (약물전달 시스템 개발을 위한 여기된 광감응제의 응용)

  • Choe, Se-woon
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • 2015.10a
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    • pp.958-960
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    • 2015
  • Sickle cells possess a unique combination of traits that may enable their use as models for novel synthetic tumor targeting controlled release drug carriers with the ability to treat disseminated tumors in advanced metastatic disease. In this study, we assess the ability of light-activated release sickle cells to enhance tumor delivery of the fluorescent dye calcein by delayed photolysis controlled release compared to free systemic administration of calcein. Sickle cells from mouse models of the disease were shown to preferentially accumulate in tumors compared to adjacent tissue, in 4T1 tumors in mice on a time scale about 12 hours. Sickle cells photosensitized with protoporphyrin IX achieved delayed release of 50% of contents 8-16 hours after photoactivation, which was deemed useful for in vivo delivery of cargo to tumors given the tumor accumulation time of the sickle cells. Sickle cells may be useful as a model for new synthetic drug carrier particles with delayed photolysis controlled release properties.

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Overview of Helicobacter pylori and Treatment Options (헬리코박터 파일로리(Helicobacter pylori) 감염 및 치료법 개요)

  • Song, Young Goo
    • Economic and Environmental Geology
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    • v.48 no.3
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    • pp.241-246
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    • 2015
  • Helicobacter pylori is an important transmissible human pathogen found on the luminal surface of the gastric epithelium. The organism can persist in the stomach indefinitely and causes gastroduodenal inflammation that may proceed to atrophic gastritis, peptic ulcer, gastric MALT lymphoma, and gastric cancer. Standard triple therapy which consists of proton pump inhibitor (PPI) plus two antibiotics (amoxicillin and clarithromycin) is now generally used in Korea, however, eradication rates of H. pylori has been decreasing due to increasing antibiotic resistance. In this review, current second-line treatment regimens, difficult problems on treatment, necessity of local target therapy, applicability of clay minerals as a drug delivery system (DDS), and a new therapeutic strategy and its study plans will be discussed.

Application of Stimuli-responsive Chitosan Micelles for Improved Therapeutic Efficiency of Anticancer Agents (항암제의 치료 효율성을 높이기 위한 다양한 자극 응답성 물질이 개질된 키토산 마이셀의 응용성 고찰)

  • Jeong, Gyeong-Won;Park, Jun-Kyu;Nah, Jae-Woon
    • Applied Chemistry for Engineering
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    • v.29 no.2
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    • pp.147-154
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    • 2018
  • Currently, to overcome low therapeutic efficiencies and side effects of anticancer agents, the study of drug carrier based on polymers have been consistently investigated. Although the traditional drug carrier based on polymers displayed an excellent result and significant progress, there has been a problem with the side effect and low therapeutic efficiency because of the premature drug release before reached to the targeted region by the low stability in blood stream and sustained drug release. In this review article, to improve the problem of inefficient drug release, methods were suggested, which can maximize the therapeutic efficiency by increasing the stability in the blood stream and triggering drug release at the target site by introducing a stimuli-responsive substance to the non-toxic and biocompatible natural polymer chitosan.

Current Status and Consensus on Esophageal Cancer Management (식도암의 치료, 어디까지 와 있는가?)

  • Joon Han Jeon;Dae Young Cheung
    • Journal of Digestive Cancer Research
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    • v.1 no.1
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    • pp.17-23
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    • 2013
  • Over the decades, the treatment of the esophageal cancer has been debated. Multimodal therapy is a important keystone in advanced esophageal cancer. Neoadjuvant chemoradiation therapy is now known to provide advantages for treating stage II and stage III esophageal squamous cell cancer and can also be considered for the esophageal adenocarcinoma. Definitive chemoradiation therapy results in long-term survival compared with surgery alone. This review aims to provide recent consensus recommendations based on the data and literatures.

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Off-pump Coronary Artery Bypass Surgery Versus Drug Eluting Stent for Multi-vessel Coronary Artery Disease (다혈관 관상동맥질환에서의 심폐바이패스를 사용하지 않은 관상동맥우회술과 약물용출 스텐트시술)

  • Lee, Jae-Hang;Kim, Ki-Bong;Cho, Kwang-Ree;Park, Jin-Shik;Kang, Hyun-Jae;Koo, Bon-Kwon;Kim, Hyo-Soo;Sohn, Dae-Won;Oh, Byung-Hee;Park, Young-Bae
    • Journal of Chest Surgery
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    • v.41 no.2
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    • pp.202-209
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    • 2008
  • Background: The introduction of Drug Eluting Stents (DES) decreased the number of patients referred for coronary artery bypass grafting (CABG). The impact of DES on CABG (Step 1) was studied and compared with the 1-year outcome after CABG with DES (Step 2). Material and Method: Surgical results for patients who underwent off-pump CABG (OPCAB) before the introduction of DES(n=298) were compared with those who underwent OPCAB after the introduction of DES (n=288) (Step 1). Postoperative 30-day and 1-year results were also compared between the patients who underwent percutaneous coronary intervention (PCI) using DES (n=220) and those who underwent OPCAB (n=255) (Step 2). Result: Since the introduction of DES, the ratio of CABG versus PCI decreased. In the CABG group, the number of high risk patients such as elderly patients (age 62 vs. 64, p=0.023), those with chronic renal failure (4% vs. 9%, p=0.021), calcification of the ascending aorta (9% vs. 15%, p=0.043), or frequency of urgent or emergent operations (12% vs. 22%, p=0.002) increased. However, there were no differences in the cardiac death and graft patency rates between the two groups (step 1). During the one-year follow up period, the rate of target vessel revascularization (12.3% vs. 2.4%, p<0.001) and major adverse cardiac events (MACE: death, myocardial infarct, TVR) were higher in the DES than the CABG group (13.6% vs 4.3%) (stage 2). Conclusion: Introduction of DES decreased the number of patients referred for surgery, and increased the comorbidity in patients who underwent CABG. DES increased the rate of target vessel revascularization, and the occurrence of MACE during the 1-year follow-up. However, there was no difference in the incidence of myocardial infarction and cardiac death between the two groups.