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Relevant bibliographies by topics / Intrinsic solubility

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Academic literature on the topic 'Intrinsic solubility'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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Journal articles on the topic "Intrinsic solubility"

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Dezani, André Bersani, Thaisa Marinho Pereira, Arthur Massabki Caffaro, Juliana Mazza Reis, and Cristina Helena dos Reis Serra. "Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification." Brazilian Journal of Pharmaceutical Sciences 49, no. 4 (December 2013): 853–63. http://dx.doi.org/10.1590/s1984-82502013000400026.

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Solubility and dissolution rate of drugs are of major importance in pre-formulation studies of pharmaceutical dosage forms. The solubility improvement allows the drugs to be potential biowaiver candidates and may be a good way to develop more dose-efficient formulations. Solubility behaviour of lamivudine, stavudine and zidovudine in individual solvents (under pH range of 1.2 to 7.5) was studied by equilibrium solubility and intrinsic dissolution methods. In solubility study by equilibrium method (shake-flask technique), known amounts of drug were added in each media until to reach saturation and the mixture was subjected to agitation of 150 rpm for 72 hours at 37 ºC. In intrinsic dissolution test, known amount of each drug was compressed in the matrix of Wood's apparatus and subjected to dissolution in each media with agitation of 50 rpm at 37 ºC. In solubility by equilibrium method, lamivudine and zidovudine can be considered as highly soluble drugs. Although stavudine present high solubility in pH 4.5, 6.8, 7.5 and water, the solubility determination in pH 1.2 was not possible due stability problems. Regarding to intrinsic dissolution, lamivudine and stavudine present high speed of dissolution. Considering a boundary value presented by Yu and colleagues (2004), all drugs studied present high solubility characteristics in intrinsic dissolution method. Based on the obtained results, intrinsic dissolution seems to be superior for solubility studies as an alternative method for biopharmaceutical classification purposes.

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Istratov, A. A., P. Zhang, R. J. McDonald, A. R. Smith, M. Seacrist, J. Moreland, J. Shen, R. Wahlich, and E. R. Weber. "Nickel solubility in intrinsic and doped silicon." Journal of Applied Physics 97, no. 2 (January 15, 2005): 023505. http://dx.doi.org/10.1063/1.1836852.

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Han, Kyong Ho, Gil Song Jeon, In Kwon Hong, and Seung Bum Lee. "Prediction of solubility parameter from intrinsic viscosity." Journal of Industrial and Engineering Chemistry 19, no. 4 (July 2013): 1130–36. http://dx.doi.org/10.1016/j.jiec.2012.12.009.

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4

Llinàs, Antonio, Jonathan C. Burley, Karl J. Box, Robert C. Glen, and Jonathan M. Goodman. "Diclofenac Solubility: Independent Determination of the Intrinsic Solubility of Three Crystal Forms." Journal of Medicinal Chemistry 50, no. 5 (March 2007): 979–83. http://dx.doi.org/10.1021/jm0612970.

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Palmer, David S., Antonio Llinàs, Iñaki Morao, Graeme M. Day, Jonathan M. Goodman, Robert C. Glen, and John B. O. Mitchell. "Predicting Intrinsic Aqueous Solubility by a Thermodynamic Cycle." Molecular Pharmaceutics 5, no. 2 (February 22, 2008): 266–79. http://dx.doi.org/10.1021/mp7000878.

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Raevsky, Oleg A., Veniamin Y. Grigorev, Daniel E. Polianczyk, Olga E. Raevskaja, and John C. Dearden. "Aqueous Drug Solubility: What Do We Measure, Calculate and QSPR Predict?" Mini-Reviews in Medicinal Chemistry 19, no. 5 (February 21, 2019): 362–72. http://dx.doi.org/10.2174/1389557518666180727164417.

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Detailed critical analysis of publications devoted to QSPR of aqueous solubility is presented in the review with discussion of four types of aqueous solubility (three different thermodynamic solubilities with unknown solute structure, intrinsic solubility, solubility in physiological media at pH=7.4 and kinetic solubility), variety of molecular descriptors (from topological to quantum chemical), traditional statistical and machine learning methods as well as original QSPR models.

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Laihanen, Niina, Esa Muttonen, and Matti Laaksonen. "Solubility and Intrinsic Dissolution Rate of Alprazolam Crystal Modifications." Pharmaceutical Development and Technology 1, no. 4 (January 1996): 373–80. http://dx.doi.org/10.3109/10837459609031432.

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Zhou, Haoli, and Wanqin Jin. "Membranes with Intrinsic Micro-Porosity: Structure, Solubility, and Applications." Membranes 9, no. 1 (December 26, 2018): 3. http://dx.doi.org/10.3390/membranes9010003.

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Microporous polymer membranes have been widely studied because of their excellent separation performance. Among them, polymers of intrinsic micro-porosity (PIMs) have been regarded as a potential next-generation membrane material for their ultra-permeable characteristics and their solution-processing ability. Therefore, many reviews have been reported on gas separation and monomers for the preparation of PIMs. This review aims to provide an overview of the structure-solubility property. Different structures such as non-network and network macromolecular structure made of different monomers have been reviewed. Then their solubility with different structures and different separation applications such as nanofiltration, pervaporation, and gas/vapor separation are summarized. Lastly, we also provide our perspectives on the challenges and future directions of the microporous polymer membrane for the structure-property relationship, anti-physical aging, and more.

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Nainwal, Nidhi, Ranjit Singh, Sunil Jawla, and Vikas Anand Saharan. "The Solubility-Permeability Interplay for Solubility-Enabling Oral Formulations." Current Drug Targets 20, no. 14 (October 14, 2019): 1434–46. http://dx.doi.org/10.2174/1389450120666190717114521.

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The Biopharmaceutical classification system (BCS) classifies the drugs based on their intrinsic solubility and intestinal permeability. The drugs with good solubility and intestinal permeability have good bioavailability. The drugs with poor solubility and poor permeability have solubility dependent and permeability dependent bioavailability, respectively. In the current pharmaceutical field, most of the drugs have poor solubility. To solve the problem of poor solubility, various solubility enhancement approaches have been successfully used. The effects of these solubility enhancing approaches on the intestinal permeability of the drugs are a matter of concern, and must not be overlooked. The current review article focuses on the effect of various solubility enhancing approaches viz. cyclodextrin, surfactant, cosolvent, hydrotropes, and amorphous solid dispersion, on the intestinal permeability of drugs. This article will help in the designing of the optimized formulations having balanced solubility enhancement without affecting the permeability of drugs.

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Stanciu, Ioana. "Methods for Determining the Solubility Parameter of Additives for Lubricating Oils." Oriental Journal Of Chemistry 35, no. 4 (July 22, 2019): 1297–301. http://dx.doi.org/10.13005/ojc/350407.

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In this article I have been looking at the determination of the solubility parameter by two methods for an additive KELTAN 4200 used in lubricating oils. To determine the solubility parameter, it is necessary to know the intrinsic viscosities of the polymer in as many solvents with different solubility parameters. Determination of the partial and global solubility parameters was done, first, using the Hansen method, then by an improved method.

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Dissertations / Theses on the topic "Intrinsic solubility"

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McCracken, Colin Gary. "The intrinsic and extrinsic solubility of hydrogen in aluminium-lithium based alloys." Thesis, Brunel University, 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.385654.

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McDonagh, James L. "Computing the aqueous solubility of organic drug-like molecules and understanding hydrophobicity." Thesis, University of St Andrews, 2015. http://hdl.handle.net/10023/6534.

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This thesis covers a range of methodologies to provide an account of the current (2010-2014) state of the art and to develop new methods for solubility prediction. We focus on predictions of intrinsic aqueous solubility, as this is a measure commonly used in many important industries including the pharmaceutical and agrochemical industries. These industries require fast and accurate methods, two objectives which are rarely complementary. We apply machine learning in chapters 4 and 5 suggesting methodologies to meet these objectives. In chapter 4 we look to combine machine learning, cheminformatics and chemical theory. Whilst in chapter 5 we look to predict related properties to solubility and apply them to a previously derived empirical equation. We also look at ab initio (from first principles) methods of solubility prediction. This is shown in chapter 3. In this chapter we present a proof of concept work that shows intrinsic aqueous solubility predictions, of sufficient accuracy to be used in industry, are now possible from theoretical chemistry using a small but diverse dataset. Chapter 6 provides a summary of our most recent research. We have begun to investigate predictions of sublimation thermodynamics. We apply quantum chemical, lattice minimisation and machine learning techniques in this chapter. In summary, this body of work concludes that currently, QSPR/QSAR methods remain the current state of the art for solubility prediction, although it is becoming possible for purely theoretical methods to achieve useful predictions of solubility. Theoretical chemistry can offer little useful additional input to informatics models for solubility predictions. However, theoretical chemistry will be crucial for enriching our understanding of the solvation process, and can have a beneficial impact when applied to informatics predictions of properties related to solubility.

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Wassvik, Carola. "Computational Analysis of Aqueous Drug Solubility – Influence of the Solid State." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis (AUU), 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-7334.

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Sugandhi, Eko Winny. "Synthesis, Characterization, and Antimicrobial Activity of Water-soluble, Tri-carboxylato Amphiphiles." Diss., Virginia Tech, 2007. http://hdl.handle.net/10919/26106.

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Many previous studies of biological activity in a homologous series of amphiphiles have shown a cut-off effect, where the biological activity increases with an increase in chain length, after which the activity plateaus or weakens. One factor suspected to cause this problem is solubility issues. We have designed several series of very hydrophobic, water-soluble amphiphiles to overcome this problem. Three homologous series containing mobile hydrophobic moieties and two series of epimers containing rigid cholestane moieties have been synthesized; the hydrophobic moiety is connected to the first-generation, Newkome-type dendron via a ureido linker. We have demonstrated that as tris(triethanolammonium) salts, these amphiphiles show excellent solubility in water. The solubilities in aqueous triethanolamine solution of the three series containing mobile hydrophobic moieties are 19,500 to 25,700 μM depending on the formula weight of the homolog, while those containing rigid cholestane moieties are 18,900 and 17,400 μM. Having eliminated the solubility issue, the antimicrobial activity against a broad spectrum of microorganisms has been screened. We have demonstrated that the antimicrobial activity depends on the amphiphile-series, species, chain-length, or epimer specificities, as well as hydrophobicity. The one-tailed, tri-carboxylato amphiphiles are generally better than the other series, with two exceptions. First, the two-tailed tri-carboxylato amphiphiles, 3CUr1(11)₂ and 3CUr1(12)₂, are more active against Cryptococcus neoformans; in fact, both amphiphiles (MICs are 6.9 and 7.2 μM, respectively) are considered to display good antifungal activity. Second, amphiphile 3CUr-β-cholestane, whose MIC is 27 μM, is more active against Staphylococcus aureus. Overall, these new tri-carboxylato amphiphiles only exhibit moderate activity with two promising leads. Furthermore, we have demonstrated the intrinsic activity (MIC₀) of the one-tailed, tri-carboxylato amphiphile series (3CUrn) against Mycobacterium smegmatis. All the MIC₀s observed are at least 8-fold lower than the corresponding CMCs. Amphiphile 3CUr16 is the most active; the MIC₀ is 100-fold smaller than the CMC. With this consideration, we have suggested that the mechanism of action of the antimycobacterial activity in amphiphile 3CUr16 is not related to detergency.
Ph. D.

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5

Issa, Michéle Georges. "Avaliação do impacto de diferentes variáveis no ensaio de dissolução intrínseca de metronidazol." Universidade de São Paulo, 2011. http://www.teses.usp.br/teses/disponiveis/9/9139/tde-15072011-104145/.

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O objetivo do presente trabalho foi avaliar o impacto de diferentes variáveis no ensaio de dissolução intrínseca de metronidazol. Inicialmente, as amostras, com diferentes graus de micronização, foram submetidas à caracterização físico-química, sendo realizados ensaios de solubilidade, tamanho de partícula, análise térmica (DSC/ TG), infravermelho por transformada de Fourier (FTIR), difratometria de raios X (DRX), análise de área superficial pelo método BET, microscopia óptica, densidade verdadeira e densidade compactada. Na sequência, foram realizados os ensaios de dissolução intrínseca segundo um planejamento experimental do tipo fatorial fracionado, sendo cada fator avaliado em três níveis. Para o delineamento, utilizou-se o programa Statistica 8.0. e os fatores estudados foram: velocidade de rotação, pressão utilizada na formação do compactado do fármaco, meio de dissolução e grau de micronização. Os resultados mostraram alteração nas propriedades reológicas do material conforme o aumento do grau de micronização, enquanto as demais propriedades não foram afetadas. Entre os fatores estudados no delineamento, a velocidade de rotação e o meio de dissolução, foram aqueles que exerceram influência significativa na dissolução intrínseca do metronidazol. Embora a solubilidade do fármaco não sofra influência do tamanho de partícula, valores superiores foram observados em HCl 0,1 M, meio em que também foram obtidas as mais elevadas velocidades de dissolução intrínseca (VDIs).
The purpose of this study is to evaluate the impact of different variables in the intrinsic dissolution test of metronidazol. Initially, the samples, with different levels of micronization, underwent physicochemical characterization, whereby they were tested for solubility, particle size, thermal analysis (DSC/TG), Fourier transform infrared (FTIR) spectroscopy, X-ray diffractometry (DRX), surface area analysis by the BET method, optical microscopy, true density and tapped density. Then, intrinsic dissolution tests were carried out according to fractional factorial experimental planning, with each factor being evaluated on three levels. The Statistica 8.0 software program was used for design, and the factors studied were: rotational velocity, pressure used in the formation of the compressed drug, dissolution medium and level of micronization. The results indicated alterations in the rheological properties of the material, as the level of micronization increased, while the remaining properties were unaffected. Among the factors studied in the design, the rotation speed and the dissolution medium were the factors that exercised the most significant influence on the intrinsic dissolution of metronidazol. Although the solubility of the drug is not influenced by particle size, higher values were observed in HCl 0.1 M, the medium in which the highest intrinsic dissolution rates (IDRs) were also obtained.

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Costa, Iguatinã de Melo. "Estudo de propriedades físico-químicas de metalofármacos de dirutênio com anti-inflamatórios não esteroides." Universidade de São Paulo, 2014. http://www.teses.usp.br/teses/disponiveis/46/46136/tde-30092014-105337/.

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Complexos de rutênio, em razão da menor toxicidade e por poderem exibir atividade citotóxica ou antimetastática, tem sido considerados como alternativas potencialmente promissoras aos complexos de platina para tratamento de câncer. Nosso grupo de pesquisa tem investigado a interação de íons metálicos com fármacos anti-inflamatórios não esteroides (FAINEs) e já obteve sucesso na preparação de metalofármacos de dirutênio(II,III)-FAINEs, os quais se mostraram promissores com relação à atividade frente a modelos de glioma. Com a finalidade de contribuir para o entendimento das propriedades físico-químicas desses complexos, o presente trabalho teve como principal objetivo analisar propriedades consideradas particularmente essenciais a um potencial candidato a fármaco, tais como, estabilidade no estado sólido, lipofilicidade, solubilidade aquosa e dissolução intrínseca. Um complexo inédito de fórmula [Ru2Cl(feno)4], em que feno = fenoprofenato, foi sintetizado e caracterizado por meio de análise elementar, espectroscopia eletrônica, espectroscopia vibracional, difratometria de raios X, análise térmica e espectrometria de massas. Os complexos já testados anteriormente para atividade biológica, [Ru2Cl(ibp)4], ibp = ibuprofenato, e [Ru2(cet)4Cl], cet = cetoprofenato, foram analisados quanto à estabilidade no estado sólido por meio da determinação isotérmica de variação de massa. As lipofilicidades desses dois complexos, juntamente com a dos fármacos de origem e a do precursor sintético [Ru2(O2CH3)4Cl], foram avaliadas pelo método shake flask, e suas solubilidade aquosas foram investigadas em presença de co-solventes alcoólicos. Investigou-se ainda a velocidade de dissolução intrínseca do [Ru2Cl(ibp)4] que se encontra em estágio avançado de estudos biológicos. Os resultados obtidos trazem novas informações sobre o comportamento térmico dos complexos e sobre suas características biofarmacêutica.
Ruthenium complexes, mainly due to the lower toxicity and the cytotoxic and anti-metastatic activities, have been considered as potentially promising alternatives to platinum drugs for cancer treatment. Our research group has investigated the interactions of diruthenium metal cores with anti-inflammatory non-steroidal drugs (NSAIDs) and succeeded in preparing diruthenium(II,III)-NSAIDs metallodrugs which show promising activity against glioma models. With the aim of elucidating the physico-chemical properties of these complexes, the major objective of the present work was to investigate properties which are considered as essential for a potential candidate to drug, e.g., stability in the solid state, lipophilicity, aqueous solubility and intrinsic dissolution. A new complex of formula [Ru2Cl(feno)4], where feno = fenoprofen, was synthesized and characterized by elemental analysis, electronic spectroscopy, vibrational spectroscopy, X-rays difractommetry, thermal analysis and mass spectrometry. The complexes previously tested for biological properties, [Ru2Cl(ibp)4], ibp = ibuprofenate, and [Ru2(cet)4Cl], cet = cetoprofenate, were inv estigated for the stability in the solid state by isothermal thermogravimetry. The lipophilicity of the se complexes, as well as those of the parent drugs and of the precursor [Ru2(O2CH3)4Cl], was evaluated by the shake flask method, and their aqueous solubility in the presence of alcohol co-solvents was investigated. In addition, the intrinsic dissolution rate was determined for [Ru2Cl(ibp)4], which is undergoing advanced biological studies. The results provide important new information on the thermal behavior of the complexes and also on their biopharmaceutical propertie.

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Books on the topic "Intrinsic solubility"

1

McCracken, C. G. The intrinsic and extrinsic solubility of hydrogen in aluminium-lithium based alloys. Uxbridge: Brunel University, 1994.

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Book chapters on the topic "Intrinsic solubility"

1

Burgot, Jean-Louis. "Intrinsic, Ionic, and Total Solubilities; Solubility Product and Precipitation." In Ionic Equilibria in Analytical Chemistry, 609–17. New York, NY: Springer New York, 2012. http://dx.doi.org/10.1007/978-1-4419-8382-4_32.

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Palmer, David S., and Maxim V. Fedorov. "Molecular Simulation Methods to Compute Intrinsic Aqueous Solubility of Crystalline Drug-Like Molecules." In Computational Pharmaceutical Solid State Chemistry, 263–86. Hoboken, NJ: John Wiley & Sons, Inc, 2016. http://dx.doi.org/10.1002/9781118700686.ch11.

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3

Bejaoui, Marouene, Hanen Oueslati, and Haykel Galai. "Ternary Solid Dispersion Strategy for Solubility Enhancement of Poorly Soluble Drugs by Co-Milling Technique." In Chitin and Chitosan - Physicochemical Properties and Industrial Applications [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.95518.

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Amorphous ternary solid dispersion has become one of the strategies commonly used for improving the solubility and bioavailability of poorly water soluble drugs. Such multicomponent solid dispersion can be obtained by different techniques, this chapter provides an overview of ternary solid dispersion by co-milling method from the perspectives of physico-chemical characteristics in vitro and in vivo performance. A considerable improvement of solubility was obtained for many active pharmaceutical ingredients (e.g., Ibuprofen, Probucol, Gliclazid, Fenofibrate, Ibrutinib and Naproxen) and this was correlated to the synergy of multiple factors (hydrophilicity enhancement, particle size reduction, drug-carrier interactions, anti-plasticizing effect and complexation efficiency). This enhanced pharmacokinetic properties and bioavailability of these drug molecules (1.49 to 15-folds increase in plasma drug concentration). A particular focus was accorded to compare the ternary and binary system including Ibuprofen and highlighting the contribution of thermal and spectral characterization techniques. The addition of polyvinylpyrrolidone (PVP K30), a low molecular weight molecule, into the binary solid dispersion (Ibuprofen/β-cyclodextrin), leads to a 1.5–2 folds increase in the drug intrinsic dissolution rate only after 10 min. This resulted from physical stabilization of amorphous Ibuprofen by reducing its molecular mobility and inhibiting its recristallization even under stress conditions (75% RH and T = 40°C for six months).

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Venkateswara Raju, Chikkili, Mathavan Sornambigai, and Shanmugam Senthil Kumar. "Ruthenium-Tris-Bipyridine Derivatives as a Divine Complex for Electrochemiluminescence Based Biosensor Applications." In Ruthenium - an Element Loved by Researchers [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.96819.

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In electrochemiluminescence (ECL) studies, Tris (bipyridine)ruthenium(II) chloride (Ru(bpy)3 2+) and its derivatives have been used as primary luminophores since 1972. The flexible solubility in both aqueous and non-aqueous medium and the remarkable intrinsic properties like chemical, optical and desirable electrochemical behavior drives the researcher to use Ru(bpy)3 2+ and its derivatives as highly active ECL probes in modern analytical science. Novel surface modification of Ru(bpy)3 2+ based ECL platforms are highly useful in the selective and sensitive detection of biomolecules, DNA analysis, immunoassays detection, and imaging of the biologically important molecules in cells and tissue of living organisms. This chapter discusses and highlights the most significant works in Ru(bpy)3 2+ based ECL properties of reaction mechanisms and their applications.

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