Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 18 of 18 for “"pharmacokinetic profiles"”.
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Design, Synthesis, and Evaluation of Novel Antimycobacterial Agents With Enhanced Pharmacokinetic Profiles
… were assessed along with in vitro cytotoxicity profiles, pharmacokinetic and physicochemical parameters, including aqueous solubility, permeability, and human plasma protein binding. Based on the preliminary data, of the 39 compounds tested, compounds 192 and 200 were identified as the best …
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Pharmacokinetic Profiles of Oxytetracycline in Yellow Perch (Perca flavescens) as Determined by Plasma Concentration Following Different Routes of Administration
… used in the aquaculture industry. Previous pharmacokinetic studies of OTC have been conducted in cold water and warm water species of fish. However, no pharmacokinetic studies have been conducted on a cool water species such as yellow perch (Perca flavescens). The yellow perch is a cool …
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PHARMACOKINETICS AND ORAL DELIVERY OF POLYMETHOXYLATED FLAVONES
… and luteolin tetramethyl ether (LTE), their pharmacokinetic profiles were assessed in Sprague-Dawley rats. Aqueous solubility has been identified a major barrier to their oral bioavailability. Subsequently, self-microemulsifying drug delivery system (SMEDDS) was developed and characterized. …
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Characterization of novel small molecule inhibitors of FOXM1 as potential therapeutic agents for breast cancer
… specificity and potency, and importantly, poor pharmacokinetic profiles in animals. To this end, we have identified and characterized novel inhibitors of FOXM1 that effectively suppress breast cancer cell growth and survival in vitro and in vivo. Our potential FOXM1 inhibitors displayed …
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Preclinical pharmacokinetic evaluation of novel antimalarial and antituberculosis drug leads
Preclinical pharmacokinetics relies on efficient and accurate screening to select clinical candidates from early leads. Poor pharmacokinetic interpretation can disadvantage drug discovery by promoting inadequate compounds and expelling potential drug candidates. Objectives of this project included …
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Development of orthogonal nanotherapeutics for colorectal cancer treatment
… in vivo can be challenging due to the dissimilar pharmacokinetic profiles that can hugely affect their therapeutic effects. Moreover, RG7388 and Entinostat suffer from severe systemic toxicities such as leukopenia and thrombocytopenia.<br/><br/>The emerging clinical success of nanomaterials over …
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Synthesis, characterization and biological investigation of self-delivering and modified short interfering RNAs (siRNAs)
… must be chemically modified to improve their pharmacokinetic profiles. This dissertation reports the use of two bioconjugates, cholesterol and folic acid, to improve the cellular uptake and delivery of siRNAs and explores the incorporation of a novel sugar moiety within siRNAs to assess its …
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Combination of STING and TLR 7/8 agonists as vaccine adjuvants for cancer immunotherapy
… cytokine. Small molecules display poor pharmacokinetic profiles in vivo, therefore, we fabricated nanoparticles to improve their in vivo disposition. PLGA NPs displayed similar DC activation to free drugs and hence will be used for further in vivo studies.
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Melatonin-Tamoxifen Drug Conjugates as Breast Cancer Drugs: Pharmacological Evaluation in Phenotypically Diverse Breast Cancer Models and Pharmacokinetic Assessment in Liver Microsome and Female Mouse Models
… C4 and C5 also exhibited unique binding profiles (affinity for ESR1 and MT1R) compared to the other conjugates. C4 and C5 were further assessed for their actions against tamoxifen-resistant (TamR) MCF-7 cells and patient-derived xenograft triple-negative BC cells (TU-BcX-4IC) as well as …
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Stimuli-Responsive Polymer Systems that Respond to Redox Potential and pH for Controlled Drug Release
… Stimuli-responsive nanocarriers exhibit better pharmacokinetic profiles with reduced premature cargo leakage during circulation time and improved tumor targeting efficacies. pH is the most commonly explored stimuli for designing nanocarriers, however there has been a recent interest in redox …
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Pharmacological characterisation of selected pyrrolobenzodiazepines as anti-cancer agents. Pharmacokinetic and pharmacodynamic characterisation of the pyrrolobenzodiazepine dimer SJG-136 and the monomers D709119, MMY-SJG and SJG-303
… type selective cytotoxicity in in vitro assays. Pharmacokinetic studies in mice via both the i.p. and i.v. route (dosed at the maximum tolerated dose (MTD)) showed that SJG-136 reaches concentrations in plasma well in excess of the in vitro IC50 values for 1 h exposure, and was detected in tumour …
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Non-Neuroleptic Antitubercular and Anticancer Therapeutics through Rational Drug Remodelling of Phenothiazines and Related Antipsychotics
… Prior to chemical synthesis, drug metabolism and pharmacokinetic related properties were predicted in silico to assess drug-likeness of the new chemical entities derived from phenothiazines and related antipsychotics. The in silico profiling also included prediction of blood/brain partition …
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Population pharmacokinetic modelling to address the gaps in knowledge of commonly used HIV and TB drugs in children
… adjustment of doses. This thesis assessed the pharmacokinetics of abacavir and ethambutol and evaluated the influence of covariates such as age and concomitant medication on the PK parameters across different studies using nonlinear mixed-effects modelling. The models developed were used to …
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Synthesis and Evaluation of Carbohydrate Based Cationic Polymers for siRNA Delivery and Tracking
… as well as other RNA molecules have poor pharmacokinetic profiles, can easily be hydrolyzed or degraded, cause serious immunogenic response and can be toxic to particular cell types and organs. To fulfill the demands, a variety of polymeric vehicles have been synthesized and investigated, …
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In vitro and in silico profiling to assist pharmaceutical development
… On the other hand studies demonstrated that poor pharmacokinetic behaviour was responsible for the majority of drug candidate failures. Therefore the challenge is to be able to keep up with the rate of production to study the in vivo behaviour of so many drugs more rapidly and efficiently. The …
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Characterization of a new miniaturized hollow-fiber bioreactor for cultivation of cell lines and primary cells to improve cytostatic drug testing in vitro
… compartment. Thus, time dependent concentration profiles (e.g. pharmacokinetic profiles of drugs) can be realized as illustrated using glucose as a model compound. Depending on the molecular size cut-off of the membranes used, added growth factors like GM-CSF and IL-3 as well as factors secreted …
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Enhancing Cisplatin Delivery and Anti-tumor Efficacy Using Hyperthermia
… under hyperthermic conditions would improve the pharmacokinetic profiles of cisplatin, increase drug delivery to the tumor, decrease normal tissue toxicity, and enhance the anti-tumor activity of cisplatin. We successfully prepared temperature-sensitive liposomes loaded with cisplatin and …
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Characterizing the epidemiology of ophidiomycosis in North American snakes through field studies, modeling, pathogen genomic analysis, and treatment trials
… disease and characterize the pharmacodynamic and pharmacokinetic profiles for a single medication and delivery system in diseased snakes. Ophidiomycosis surveillance was conducted in a variety of snake species in southeast Georgia, USA and in Lake Erie watersnakes (Nerodia sipedon insularum, LEWS) …