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 20 of 131 for “"aqueous solubility"”.
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Synthesis and biological activity of ajoenes with increased aqueous solubility
… active than Z-ajoene with an IC50 of 1.7 M. An aqueous solubility assay reveals that aqueous solubility increased with subsituition and the analogues with amido or acetate substituents were the most soluble ones. The analogues were also shown to enhance the apoptotic effects of two …
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Predicting aqueous solubility of pharmaceutical agents by solid dispersion prepared by solvent evaporation method
<p>Solubility of active pharmaceutical agents is a crucial process that determines drug absorption and ultimately its bioavailability. Many of the new therapeutically beneficial compounds discovered are lipophilic requiring various solubility enhancement strategies to improve their solubility. …
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Correlation of Aqueous Solubility and Anti-Cancer Activity of Novel Triazolium and Imidazolium Salts
… cancer therapeutics. This thesis describes the aqueous solubility and the differential activity of N,AT-bis-substituted-l,2,4-triazolium bromide salts and N/N'-bis(naphthylmethyl)imidazolium bromide salts against MDA-MB-468 breast cancer cells and PC-3 prostate carcinomas. Using a microscale …
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Low temperature aqueous solubility of fluorite at temperatures of 5, 25, and 50°C and ionic strengths up to 0.72M
Historical fluorite solubility research found that fluorite solubilities varied over three orders-of-magnitude and appear to be inconsistent with several recently determined fluorite solubilities. This research involved a comprehensive series of solubility experiments run over a period of three …
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Synthesis, characterisation, structure-activity and structure-property relationship studies of quinazolinones as antimycobacterial agents
… work in our research group. However, low aqueous solubility was associated with this series of compounds as a major liability, which needed to be addressed given its likely negative impact on the oral bioavailability of the compounds should they progress further. In an effort to address …
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The supramolecular derivatisation of pharmaceutically relevant compounds via co-crystallization and cyclodextrin inclusion complexation
… (FT-IR and 1H NMR) techniques. Preliminary solubility studies indicated that for five of the forms, aqueous solubility increases for the drug leads in the range 2- to 20-fold were achieved. In addition, amorphous forms of the three pyrido[1,2-a]benzimidazole derivatives were prepared via …
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Syntheses, Characterization, Physical and Biological Properties of Long-chain, Water-soluble, Dendritic Amphiphiles
… R= CnH2n+1] to alleviate the low aqueous solubility of fatty acids. The dendritictricarboxlyato headgroup improves aqueous solubility and allows us to measure the intrinsic biological activity of our amphiphiles without the potential hindrance of low aqueous solubility. The aqueous …
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The preparation and characterization of multi-component systems in drug pre-formulation
… and single crystal X-ray diffraction. Phase solubility studies with a variety of CDs showed that the poor aqueous solubility of allopurinol and 6-thioguanine was not significantly modified in the presence of CD solutions. However, a more accurate aqueous solubility value for 6-thioguanine was …
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Formation, Characterization and Stability of Natural Antimicrobial-Cyclodextrin Complexes
… activity were evaluated to quantify their solubility. Twenty three of the compounds evaluated are components of plant essential oils and the remaining five compounds are alkyl esters of para-hydroxybenzoic acid. The test compounds were evaluated for aqueous solubility as well as their …
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Design, Synthesis, and Evaluation of Novel Antimycobacterial Agents With Enhanced Pharmacokinetic Profiles
… a panel of mycobacteria. However, they have poor aqueous solubility limiting their translational potential. Our efforts to improve the aqueous solubility of the indole-based compounds has yielded the acetamide series. The design is based on the hypothesis that ‘Medicinal chemistry ligand-based …
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Preparação e caracterização de complexos multicomponentes contendo ciclodextrinas e benznidazol
… disease treatment in Brazil. This drug has low solubility, which restricts its dissolution rate. Thus, the present work aimed to study the BNZ interactions in binary systems with beta cyclodextrin (β-CD) and hydroxypropyl-beta cyclodextrin (HP-β-CD), in order to increase the apparent aqueous …
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Optimization of N-(1-Adamantyl)-3-Aryl Acetamides as Novel Antimycobacterial Agents
… sub-μg/mL MIC values, but both series have poor aqueous solubility, limiting their advancement through the drug development pipeline. Novel acetamide-based MmpL3 inhibitors were discovered in our lab with high antimycobacterial potency and improved aqueous solubility by approximately 30-fold over …
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Stereoisomeric Prodrugs to Improve Ocular And Oral Absorption of Prednisolone
… for their physico-chemical properties such as aqueous solubility and chemical stability. In vivo oral absorption studies in rats have been conducted to study the efficacy of prodrugs in improving prednisolone absorption post oral delivery. LDP and DLP demonstrated higher aqueous solubility …
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The Development of Sulfatase-Cleavable Linkers for Antibody-Drug Conjugates
… such as instability in rodent blood and poor aqueous solubility. First, this thesis describes the design, synthesis and evaluation of arylsulfates as enzymecleavable ADC linkers. These arylsulfates were designed to be cleaved by lysosomal sulfatases, thus revealing a phenolate, primed for …
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Development and Evaluation of Nano‑scale Systems for Targeted Delivery to Treat Liver Fibrosis
… consequence of HSCs activation. However, the low aqueous solubility affects its in vivo application. Therefore, poly(ethylene glycol)‑b‑poly(carbonate‑co‑lactide) copolymers were used to make micellar formulation to enhance solubility. PEG‑PCcL micelles were applied to increase the aqueous …
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Application of machine learning methods for design of crystallisation processes
… outcomes, including crystal habit and non-aqueous solubility of pharmaceutical drugs in a diverse range of solvents.;High throughput screening for analysing crystallisation outcomes and crystal habit of paracetamol in a diverse range of solvents was developed using Technobis Crystalline. …
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Modeling and Prediction of Amorphous Solid Dispersion Formation Using a Molecular Descriptor
<p>Poor aqueous solubility of an active pharmaceutical ingredient (API) is a significant hurdle during drug development. Delivering a drug in its amorphous solid-state is a potential method to overcome this issue, since the amorphous form has increased apparent aqueous solubility. However, the …
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Improved Properties of Natamycin Upon Formation of Cyclodextrin Inclusion Complexes
Natamycin is an antimycotic with very low water solubility and extremely high photosensitivity, which is used to extend the shelf life of shredded cheese products. The objectives of this research are: (a) to find a new delivery system for natamycin, which increases its aqueous solubility and (b) to …
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Physicochemical studies of the inclusion of selected agrochemicals in cyclodextrins
… display adverse properties such as low aqueous solubility, low stability, and high toxicity that limit their applications and render them environmentally hazardous. The possibility of improving these physical properties was attempted by complexing four pesticides with native and …
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Unresolved complex mixtures of aromatic hydrocarbons in the marine environment : toxicity, solubility and photodegradation studies
… particular emphasis on assessment of toxicity, aqueous solubility and photodegradation behaviour. A previously established link between the reduced Scope for Growth (SFG) of mussels with the concentration of 2-3 ringed aromatic hydrocarbons in mussels from petroleum impacted sites was found also …
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