• 한국수산과학회지
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• 제16권3호
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• pp.239-245
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• 1983

Electrochemical adsorption always was accompanied with solvent displacement and relative size factor(x) of adsorbate and solvent and hydrogen coverage(${\theta}$) on the lead anodic film electrode formed in phosphoric acid in NaCl solution and the sea water at $15{\sim}35^{\circ}C$ were studied by means of constant current-potential method and potentiodynamic cathodic polarization method. In this experiment, various constants and thermodynamic quantities calculated from the hydrogen coverage were also described to explain the reactivities of di-iso-butylnitrosoamine(DBNA) and proton ($H^+$) according to the changes of interactions between solute and solvent in the bulk phase and interphase. It was investigated that the average values of relative size factor and the coverage of hydrogen atoms studied with the electrode of lead anodic film formed in phosphoric acid solution in 60mM DBNA+0.5M NaCl and in 60mM DBNA+$6\%0$ sea water were about 11.0 and 0.2 respectively. Hydrogen evolution was electrochemical mechanism because of substitutional adsorption of aromatic substance with their delocalization of electrons, but in the case of non-charge transfer adsorption of aliphatic substance(DBNA) interacting relatively little with the electrode, it was combination mechanism.

• Asian Pacific Journal of Cancer Prevention
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• 제15권23호
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• pp.10281-10287
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• 2015

Background: Development of a nanosized polymeric delivery system for erlotinib was the main objective of this research. Materials and Methods: Poly caprolactone-polyethylene glycol-polycaprolactone (PCEC) copolymers with different compositions were synthesized via ring opening polymerization. Formation of triblock copolymers was confirmed by HNMR as well as FT-IR. Erlotinib loaded nanoparticles were prepared by means of synthesized copolymers with solvent displacement method. Results: Physicochemical properties of obtained polymeric nanoparticles were dependent on composition of used copolymers. Size of particles was decreased with decreasing the PCL/PEG molar ratio in used copolymers. Encapsulation efficiency of prepared formulations was declined by decreasing their particle size. Drug release behavior from the prepared nanoparticles exhibited a sustained pattern without a burst release. From the release profiles, it can be found that erlotinib release rate from polymeric nanoparticles is decreased by increase of CL/PEG molar ratio of prepared block copolymers. Based on MTT assay results, cell growth inhibition of erlotinib has a dose and time dependent pattern. After 72 hours of exposure, the 50% inhibitory concentration (IC50) of erlotinib hydrochloride was appeared to be $14.8{\mu}M$. Conclusions: From the obtained results, it can be concluded that the prepared PCEC nanoparticles in this study might have the potential to be considered as delivery system for erlotinib.

• 대한화학회지
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• 제27권3호
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• pp.167-177
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• 1983

물-메탄올, 물-에탄올, 물-아세톤 및 물-아세토니트릴의 2-성분 혼합용매 속에서 2-염화안트라센 술포닐의 가용매 분해반응을 전기전도도법을 써서 속도론적으로 고찰하였다. 물의 몰분률이 같은 혼합용매속에서는 쌍극자성 반양성자 용매에서 보다 양성자성 용매에서 속도가 컸으며, 물-메탄올 혼합용매에서는 실험 농도의 전체 범위에 걸쳐 물-에탄올에서 보다 항상 속도가 컸으나 아세톤과 아세토니트링의 경우에는 몰분율 0.9에서 속도의 크기가 뒤바뀌었다. 용매의 이온화 능력에 대한 반응의 감도를 나타내는 m와 전이상태에서의 물의 관여차수 n값은 모두 쌍극자성 반양성자용매에서 컸다. 이들 값과, 속도상수에서 결정한 활성화 파라미터로부터 2-염화안트라센 술포닐의 가용매분해반응은$ S_N2$ 메카니즘으로 진행된다는 것을 알았다.

• 폴리머
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• 제34권6호
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• pp.547-552
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• 2010

생분해성 고분자는 제약 및 생명공학 분야에서 많은 관심을 받고 있는 물질로 특히 나노미립구의 형태로 약물전달체의 개발에 널리 이용되고 있다. 본 연구에서는 cyclohexanedimethanol과 oxalyl chloride를 pyridine의 존재 하에서 반응하여 고분자량의 생분해성 퍼옥살레이트 고분자를 합성하고 그 물리화학적 및 생물학적 특성을 조사하였다. 폴리옥살레이트는 분자량이 약 75000 Da 정도인 반결정성 고분자이며 물에서 가수분해가 일어남을 GPC와 NMR로 확인하였다. 소수성의 폴리옥살레이트는 단일유화법으로 나노미립구로 제조될 수 있으며 약물을 포접할 수 있고 아주 우수한 세포안정성을 가졌다. 용이한 합성과 우수한 물리화학적 및 생물학적 특성을 바탕으로 폴리옥살레이트 나노미립구는 약물전달체 개발에 아주 높은 잠재력이 있음을 확인하였다.

• 대한약침학회지
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• 제19권1호
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• pp.37-44
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• 2016

Objectives: This study examined the relative efficacies of a derivative of betulinic acid (dBA) and its poly (lactide-co-glycolide) (PLGA) nano-encapsulated form in A549 lung cancer cells in vivo and in co-mutagen [sodium arsenite (SA) + benzo[a]pyrene (BaP)]-induced lung cancer in mice in vivo. Methods: dBA was loaded with PLGA nanoparticles by using the standard solvent displacement method. The sizes and morphologies of nano-dBA (NdBA) were determined by using transmission electron microscopy (TEM), and their intracellular localization was verified by using confocal microscopy. The binding and interaction of NdBA with calf thymus deoxyribonucleic acid (CT-DNA) as a target were analyzed by using conventional circular dichroism (CD) and melting temperature (Tm) profile data. Apoptotic signalling cascades in vitro and in vivo were studied by using an enzyme-linked immunosorbent assay (ELISA); the ability of NdBA to cross the blood-brain barrier (BBB) was also examined. The stage of cell cycle arrest was confirmed by using a fluorescence-activated cell-sorting (FACS) data analysis. Results: The average size of the nanoparticles was ~ 110 nm. Confocal microscopy images confirmed the presence of NdBA in the cellular cytoplasm. The bio-physical properties of dBA and NdBA ascertained from the CD and the Tm profiles revealed that NdBA had greater interaction with the target DNA than dBA did. Both dBA and NdBA arrested cell proliferation at G0/G1, NdBA showing the greater effect. NdBA also induced a greater degree of cytotoxicity in A549 cells, but it had an insignificant cytotoxic effect in normal L6 cells. The results of flow cytometric, cytogenetial and histopathological studies in mice revealed that NdBA caused less nuclear condensation and DNA damage than dBA did. TEM images showed the presence of NdBA in brain samples of NdBA fed mice, indicating its ability to cross the BBB. Conclusion: Thus, compared to dBA, NdBA appears to have greater chemoprotective potential against lung cancer.

• 대한약침학회지
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• 제27권1호
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• pp.1-13
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• 2024

Background: Diabetic nephropathy (DN) is one of the major complications of chronic hyperglycaemia affecting normal kidney functioning. The ayurvedic medicine curcumin (CUR) is pharmaceutically accepted for its vast biological effects. Objectives: The Curcuma-derived diferuloylmethane compound CUR, loaded on Poly (lactide-co-glycolic) acid (PLGA) nanoparticles was utilized to combat DN-induced renal apoptosis by selectively targeting and modulating Bcl2. Methods: Upon in silico molecular docking and screening study CUR was selected as the core phytocompound for nanoparticle formulation. PLGA-nano-encapsulated-curcumin (NCUR) were synthesized following standard solvent displacement method. The NCUR were characterized for shape, size and other physico-chemical properties by Atomic Force Microscopy (AFM), Dynamic Light Scattering (DLS) and Fourier-Transform Infrared (FTIR) Spectroscopy studies. For in vivo validation of nephro-protective effects, Mus musculus were pre-treated with CUR at a dose of 50 mg/kg b.w. and NCUR at a dose of 25 mg/kg b.w. (dose 1), 12.5 mg/kg b.w (dose 2) followed by alloxan administration (100 mg/kg b.w) and serum glucose levels, histopathology and immunofluorescence study were conducted. Results: The in silico study revealed a strong affinity of CUR towards Bcl2 (dock score -10.94 Kcal/mol). The synthesized NCUR were of even shape, devoid of cracks and holes with mean size of ~80 nm having -7.53 mV zeta potential. Dose 1 efficiently improved serum glucose levels, tissue-specific expression of Bcl2 and reduced glomerular space and glomerular sclerosis in comparison to hyperglycaemic group. Conclusion: This study essentially validates the potential of NCUR to inhibit DN by reducing blood glucose level and mitigating glomerular apoptosis by selectively promoting Bcl2 protein expression in kidney tissue.