• Title/Summary/Keyword: Drug loading

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Brachytherapy in Coronary Artery Disease (관상동맥질환의 방사성동위원소 치료)

  • Song, Ho-Chun
    • Nuclear Medicine and Molecular Imaging
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    • v.40 no.2
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    • pp.113-119
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    • 2006
  • Coronary artery disease is a loading cause of morbidity and mortality across the world. Percutaneous coronary intervention has become the major technique of revascularization. However, restenosis remains a major limitation of this procedure. Recently the need for repeat intervention due to restenosis, the most vexing long-term failure of percutaneous coronary intervention, has been significantly reduced owing to the introduction of two major advances, intracoronary brachytherapy and the drug-eluting stents. Intracoronary brachytherapy has been employed in recent years to prevent restenosis lesions with effective results, principally in in-stent restenosis. Restenosis is generally considered as au excessive form of normal wound healing divided up in precesses: elastic recoil, neointimal hyperplasia, and negative vascular remodeling. Restenosis has previously been regarded as a proliferative process in which neointimal thickening, mediated by a cascade of inflammatory mediators and other factors, is the key factor. Ionizing radiation has been shown to decrease the proliferative response to injury in animal models of restenosis. Subsequently, several randomized, double blind trials have demonstrated that intracoronary brachytherapy can reduce the rates of both angiographic restenosis and clinical event rates in patients undergoing percutaneous coronary intervention for in stent restenosis. Some problems, such as late thrombosis and edge restenosis, have been identified as limiting factors of this technique. Brachytherapy is a promising method of preventing and treating coronary artery restenosis.

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

  • Choi, Byung Moon
    • Journal of The Korean Dental Society of Anesthesiology
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    • v.13 no.4
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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.

Setting Behavior and Drug Release from Brushite Bone Cement prepared with Granulated Hydroxyapatite and β-Tricalcium Phosphate

  • Son, Yeong-Jun;Lee, In-Cheol;Jo, Hyun-Ho;Chung, Tai-Joo;Oh, Kyung-Sik
    • Journal of the Korean Ceramic Society
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    • v.56 no.1
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    • pp.56-64
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    • 2019
  • Calcium phosphate bone cement was prepared to contain antibiotics for release after setting using granulated ${\beta}$-tricalcium phosphate (${\beta}$-TCP) and hydroxyapatite (HA). Gentamicin sulfate (GS) solution was infiltrated within the interconnected pores of the granule to avoid affecting the setting reaction and for protection of GS during the setting. Consequently, the setting time and the temperature increase were not affected, regardless of the loading of GS. The release of the GS from the cement was estimated by measuring the concentration at regular intervals from the cement dipped solution. The ${\beta}$-TCP granule loaded with GS exhibited the saturation of accumulative concentration at 16 h. In contrast, the HA granule with GS exhibited steady increase in accumulative concentration of over $10{\mu}g/ml$ at 144 h. Thus, the granulated cement could release the GS greater than the minimum inhibitory concentration of staphylococcus during the prescription peroid of the oral antibiotics.

Gentamicin/CTMA/Montmorillonite as Slow-Released Antibacterial Agent

  • Fatimah, Is;Hidayat, Habibi;Purwiandono, Gani;Husein, Saddam;Oh, Won-Chun
    • Korean Journal of Materials Research
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    • v.31 no.6
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    • pp.367-374
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    • 2021
  • This paper presents the characteristics of gentamicin-loaded into cetyl trimethyl ammonium intercalated montmorillonite (GtM/CTMA/Mt) as a hybrid composite for a slow-released antibacterial delivery systems. The work describes the successful immobilization of gentamicin into the interlayers of surfactant-modified montmorillonite. Physicochemical characterization of the material is carried out by means of X-ray diffraction, scanning electron microscopy, transmission electron microscopy, and Fourier transform infrared spectroscopy. The kinetics of the gentamicin release is investigated by in vitro study and analyzed based on UV-Vis spectrometry. In addition, antibacterial study is performed towards Klebsiella pneumoniae Staphylococcus aureus, Escherichia coli, and Streptococcus pyogenes. The results show that the gentamicin loading into CTMA/Mt increases the effectiveness of the antibacterial activity, as shown by the higher inhibition zone for all tested bacteria, compared to gentamicin as a positive control. The kinetics study suggests that the gentamicin release obeys the modified Korsmeyer-Peppas model. The physicochemical study and activity test demonstrate the feasibility of the GtM/CTMA/Mt for practical applications.

Development of High Intensity Focused Ultrasound (HIFU) Mediated AuNP-liposomal Nanomedicine and Evaluation with PET Imaging

  • Ji Yoon Kim;Un Chul Shin;Ji Yong Park;Ran Ji Yoo;Soeku Bae;Tae Hyeon Choi;Kyuwan Kim;Young Chan Ann;Jin Sil Kim;Yu Jin Shin;Hokyu Lee;Yong Jin Lee;Kyo Chul Lee;Suhng Wook Kim;Yun-Sang Lee
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.9 no.1
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    • pp.9-16
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    • 2023
  • Liposomes as drug delivery system have proved useful carrier for various disease, including cancer. In addition, perfluorocarbon cored microbubbles are utilized in conjunction with high-intensity focused-ultrasound (HIFU) to enable simultaneous diagnosis and treatment. However, microbubbles generally exhibit lower drug loading efficiency, so the need for the development of a novel liposome-based drug delivery material that can efficiently load and deliver drugs to targeted areas via HIFU. This study aims to develop a liposome-based drug delivery material by introducing a substance that can burst liposomes using ultrasound energy and confirm the ability to target tumors using PET imaging. Liposomes (Lipo-DOX, Lipo-DOX-Au, Lipo-DOX-Au-RGD) were synthesized with gold nanoparticles using an avidin-biotin bond, and doxorubicin was mounted inside by pH gradient method. The size distribution was measured by DLS, and encapsulation efficiency of doxorubicin was analyzed by UV-vis spectrometer. The target specificity and cytotoxicity of liposomes were assessed in vitro by glioblastoma U87mg cells to HIFU treatment and analyzed using CCK-8 assay, and fluorescence microscopy at 6-hour intervals for up to 24 hours. For the in vivo study, U87mg model mouse were injected intravenously with 1.48 MBq of 64Cu-labeled Lipo-DOX-Au and Lipo-DOX-Au-RGD, and PET images were taken at 0, 2, 4, 8, and 24 hours. As a result, the size of liposomes was 108.3 ± 5.0 nm at Lipo-DOX-Au and 94.1 ± 12.2 nm at Lipo-DOX-Au-RGD, and it was observed that doxorubicin was mounted inside the liposome up to 52%. After 6 hours of HIFU treatment, the viability of U87mg cells treated with Lipo-DOX-Au decreased by around 20% compared to Lipo-DOX, and Lipo-DOX-Au-RGD had a higher uptake rate than Lipo-DOX. In vivo study using PET images, it was confirmed that 64Cu-Lipo-DOX-Au-RGD was taken up into the tumor immediately after injection and maintained for up to 4 hours. In this study, drugs released from liposomes-gold nanoparticles via ultrasound and RGD targeting were confirmed by non-invasive imaging. In cell-level experiments, HIFU treatment of gold nanoparticle-coupled liposomes significantly decreased tumor survival, while RGD-liposomes exhibited high tumor targeting and rapid release in vivo imaging. It is expected that the combination of these models with ultrasound is served as an effective drug delivery material with therapeutic outcomes.

Fabrication of PLGA/Dextran Double-Layered Microspheres by Oil-in-Water Solvent Evaporation Method (O/W 용매 증발법을 이용한 PLGA와 덱스트란의 이중층 미립구 제조)

  • Ko Jong Tae;Lee Jae-Ho;Lee Chang-Rae;Shin Hyung Sik;Yuk Soon Hong;Kim Moon Suk;Khang Gilson;Rhee John M.;Lee Hai Bang
    • Polymer(Korea)
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    • v.29 no.6
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    • pp.543-548
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    • 2005
  • Double-layered spheres play an important role in controlling drug delivery for pharmaceutical application, because of the low initial burst compared with single-layered spheres and targetable delivery to specific organ. But it has drawback in loading drug and controlling size. In this study, we developed double-layered spheres using relatively simple oil-in-water (O/W) solvent evaporation method witw/without ultrasonication and investigated the size variation of the double-layered microspheres on the contents of poly(lactide- co-glycolide) (PLGA). Double - layered spheres were char-acterized by scanning elecron microscope (SEM), camscope, and confocal fluorescence laser microscope (CFLM). Double-layered spheres showed smooth surfaces and obvious difference between core and corona by SEM observation and camscope. We observed the fluorescent core in the double-walled spheres composed of FlTC-dextran and PLGA using CFLM. It was found that the core of the microsphere was dextran and the corona of the fabricate microsphere was PLGA. Also, the more PLGA concentration, the more the size of the fabricating double-layered sphere observed.

Preparation and Characteristics of Ipriflavone-Loaded PLGA Microspheres (이프리플라본을 함유한 생분해성 미립구의 제조와 특성분석)

  • 이진수;강길선;이종문;신준현;정제교;이해방
    • Polymer(Korea)
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    • v.27 no.1
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    • pp.9-16
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    • 2003
  • Ipriflavone (IP) stimulates proliferation and differentiation of osteoblast and also enhances calcitonin secretion in the presence of estrogen. Poly(lactide-co-glycolide) (PLCA) due to its controllable biodegradability and relatively good biocompatibility is one of the most significant candidates for the study of drug controlled release system. In this study, IP-loaded PLGA microspheres (MSs) was prepared by using conventional O/W solvent evaporation method. The size of MSs was in the range of 5~200 $mu extrm{m}$. The morphology of MSs was characterized by SEM. And, in vitro release amounts of IP were analyzed by HPLC. The highest encapsulation efficiency were obtained by using gelatin and polyvinyl alcohol (PVA) as emulsifiers. The morphology, size distribution, and in vitro release pattern of MSs were changed by several preparation parameters such as molecular weights (8, 20, 33 and 90 kg/mol), polymer concentrations (2.5, 5, 10 and 20%), emulsifier types (PVA, gelatin and Tween 80), initial drug loading amount (5, 10, 20 and 30%) and stirring speed (250, 500 and 1000 rpm). The release of IP in vitro was more prolonged over 30 days, with close to zero-order pattern by controlling the preparation parameters. The physicochemical properties of IP-loaded PLGA MSs were investigated by XRD and DSC.

Voriconazole Therapeutic Drug Monitoring is Necessary for Children with Invasive Fungal Infection (소아에서 보리코나졸 치료적 약물 농도 모니터링의 임상적 의의)

  • Kang, Hyun Mi;Kang, Soo Young;Cho, Eun Young;Yu, Kyung-Sang;Lee, Ji Won;Kang, Hyoung Jin;Park, Kyung Duk;Shin, Hee Young;Ahn, Hyo Seop;Lee, Hyunju;Choi, Eun Hwa;Lee, Hoan Jong
    • Pediatric Infection and Vaccine
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    • v.21 no.1
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    • pp.9-21
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    • 2014
  • Purpose: To determine the clinical significance of voriconazole therapeutic drug monitoring (TDM) in the pediatric population. Methods: Twenty-eight patients with invasive fungal infections administered with voriconazole from July 2010 to June 2012 were investigated retrospectively. Fourteen received TDM, and 143 trough concentrations were analyzed. All 28 patients were assessed for adverse events and treatment response six weeks into treatment, and at the end. Results: Out of 143 samples, 53.1% were within therapeutic range (1.0-5.5 mg/L). Patients administered with the same loading (6 mg/kg/dose) and maintenance (4 mg/kg/dose) dosages prior to initial TDM showed highly variable drug levels. Adverse events occurred in 9 of 14 patients (64.3%) in both the TDM and non-TDM group. In the TDM group, voriconazole-related encephalopathy (n=2, 14.3%) and aspartate aminotransferase (AST) or alanine aminotransferase (ALT) elevation (n=8, 57.1 %) occurred with serum levels in the toxic range (>5.5 mg/L), whereas blurred-vision (n=2, 14.3%) occurred within the therapeutic range (1.18 mg/L and 3.9 mg/L). The frequency of voriconazole discontinuation due to adverse events was lower in the TDM group (0.0% vs. 18.2%, P =0.481). Overall, 57.2% of the patients in the TDM group versus 14.3% in the non-TDM group showed clinical response after 6 weeks (P =0.055), whereas 21.4% in the TDM group versus 14.3% in the non-TDM group showed response at final outcome (P =0.664). In the TDM group, >67.0% of the serum levels were within therapeutic range for the first 6 weeks; however 45.5% were within therapeutic range for the entire duration. Conclusion: Routine TDM is recommended for optimizing the therapeutic effects of voriconazole.

Heavy Metal and Amino Acid Contents of Soybean by Application of Sewage and Industrial Sludge (생활하수 및 산업폐수 슬러지 처리에 따른 콩의 중금속 및 아미노산 함량)

  • Moon, Kwang-Hyun;Kim, Jae-Young;Chang, Moon-Ik;Kim, Un-Sung;Kim, Seong-Jo;Baek, Seung-Hwa
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.42 no.2
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    • pp.268-277
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    • 2013
  • This study investigates the effects of accumulated levels of heavy metals and nutrients of cultivated soybean plant tissues, after the continuous application of sewage sludge (SS) and industrial sludge (IS). SS and IS were applied to soybean plants at loading of 0, 11.25, 22.50, and 45.00 Mg/ha, and the contents of heavy metals (Cd, Pb, Ni, Cu, and Zn), proteins, and amino acids in the cultivated soybean plants were measured. The Cd content in the soybean was 0.02~0.05 mg/kg, which is within the safety level set in the standard, and that of Pb was 0.02~0.15 mg/kg, which is also within the safety level except for IS 45 Mg/ha. The soybean harvest quantity was higher in the treatment groups than the control group in the first year. However, in the second year, SS had lower harvest and IS had the same level or a decreasing tendency, compared with the control group. In the first year, the content of amino acid which followed handling of SS was increased in the sludge groups more than in the control group in the case of glutamate. However, the influence of continuous application was increased in the sludge groups in the case of amino acids of 12 types. In conclusions, the accumulation in soybean of heavy metals by sludge treatment is not a problem, but the decreased yields needs to be considered. In addition, the most appropriate level of sludge treatment was 11.25 Mg/ha.

Formulation and Characterization of Lipase Loaded Poly(D,L - lactide-co-glycolide) Nanoparticles (리파아제가 함입된 락타이드-글리콜라이드 공중합체 나노입자의 제조 및 특성)

  • Kim, Beom-Su;ZEROUAL, Y;Lee, Kang-Min
    • Polymer(Korea)
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    • v.31 no.1
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    • pp.20-24
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    • 2007
  • The preservation of biological activity of protein drugs in formulation is still a major challenge for successful drug delivery. Lipase was encapsulated in poly (D,L-lactide- co-glycolide) PLGA nano-particles using a w/o/w solvent evaporation technique. The lipase-containing PLGA/poly (vinyl alcohol) (PVA) nanoparticles were characterized with regard to morphology, size, size distribution, lipase-loading efficiency, in vitro lipase release, and stability of lipase activity. The size of nanoparticles increased as polymer concentration was increased. The size of particles was not significantly affected by the PVA concentration; on the other hand, the particle size distribution was the narrowest when 4% of PVA was used. In optimum conditions, we possessed nanoparticles that characterized 72.5% of encapsulation efficiency, $198.3{\pm}13.8 nm$ size diameter. During the initial burst phase, the in vitro release rate was very fast, reaching 83% within 12 days. Until days 6, enzyme activity increased as the amount of lipase released was increased.