|
|
Formulation and characterization of oxims loaded PLGA nanoparticles
Hafezi, Ramin ; Šnejdrová, Eva (advisor) ; Paraskevopoulos, Georgios (referee)
Thesis title: Formulation and characterization of oxime loaded PLGA nanoparticles Author: Ramin Hafezi Supervisor: PharmDr. Eva Šnejdrová, Ph.D. Advisor: PharmDr. Juraj Martiška, Ph.D. Department: Department of Pharmaceutical Technology The diploma thesis was focused on PLGA nanoparticles (NPs) which could be loaded with oximes, prepared by a double emulsion technique, and characterised by size, polydispersity and zeta potential. The theoretical part deals with the most common methods of the NPs preparation, the polymers and stabilizers employed, and drug delivery to brain. In the experimental part the effect of various formulation factors on NP characteristics were studied: linear or branched PLGA derivative, the concentrations of polymer, the volumes of primary emulsion. Dichloromethane (DCM) or Dimethyl sulfoxide (DMSO) as solvent for polymers were used and Poloxamer 407 or Didodecyldimethylammonium bromide (DDAB) as an outer phase stabilizer were employed. By comparison among the collected results, it seemed 1% A2 in DMSO and stabilization with poloxamer 407 could be best candidate for the oxime loaded drug delivery systems as it was possible to produce nanoparticles with size from 152 to 168 nm with PDI of below 0.15. Electrostatic stability in case of using DDAB was resulted excellent and...
|
|
|
Characterization of PLGA-based film forming systems
Věříš, Andrea ; Šnejdrová, Eva (advisor) ; Paraskevopoulos, Georgios (referee)
Title of thesis: Characterization of PLGA-based film forming systems Author: Mgr. Andrea Věříš Department: Department of Pharmaceutical Technology Supervisor: PharmDr. Eva Šnejdrová, Ph.D. The aim of this thesis is to review available sources on film forming systems (FFSs), to test characteristics of poly(lactic-co-glycolic acid) of low molar mass linear or branched configuration in combination with multifunctional plasticizers and to formulate salicylate loaded film forming system. The theoretical section is focused on general characteristics and excipients used for FFs formulation and testing methods. Besides that, mathematical models commonly used for evaluation of flow behaviour are included. In the experimental section, effects of plasticizers ethyl pyruvate, methyl salicylate and triacetin on the rheological and adhesive properties of the polyesters were tested to select the optimal combination. All tested plasticizers decrease the viscosity of the polymers with ethyl pyruvate being the most effective. The flow curves of plasticized PLGA were analysed to Power law and Newton models revealing the Newton character of the systems. The evaluation of viscoelastic behavior showed liquid-like characteristic of these systems. The adhesive properties were determined by the pull away test providing the...
|
|
|
Effect of the concentration of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil
Chladová, Pavlína ; Paraskevopoulos, Georgios (advisor) ; Holas, Ondřej (referee)
Effect of the concentration of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-Fluorouracil Pavlína Chladová Dendrimers are synthetic, symmetrically tree-like branched molecules. They are composed of repeating units (monomers). They have high density of surface functional groups and spherical shape in solution. Since their molecular weight is highly controllable, they are characterized by monodispersity and this is their main difference from classical polymers. Dendrimers have a wide spectrum of applications in biomedicine. Due to the empty space between the branches of the molecule, they can encapsulate drugs, and by conjugation and complexation to the surface groups, they are able to carry even larger drug molecules. Thus, dendrimers can be used as drug delivery systems. In addition, they have been used for skin application of several active molecules, either as topical or transdermal delivery. Suitable properties for (trans)dermal application have been demonstrated for dendrimers which consist of monomers with amine groups and are connected with amide bonds. The goal of this thesis was the preparation of dendrimers with these characteristics and the evaluation of their concentration influence to the permeability of 5-Fluorouracil (5-FU) to human...
|
|
|
Effect of the generation of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil
Houšková, Denisa ; Paraskevopoulos, Georgios (advisor) ; Holas, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Supervisor: Dr. Georgios Paraskevopoulos, Ph.D. Consultant: Mgr. Anna Nová ková Author: Denisa Houšková Title of thesis: Effect of the generation of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil. Dendrimers can be defined like highly branched, star-shaped macromolecules with nanometer-scale dimensions and unlimited applications in both biological and materials sciences. Polyamidoamine (PAMAM) dendrimers have been used to effectively enhance the (trans)dermal drug delivery of several active substances. Inspired by the structure of PAMAM dendrimers, a new class of dendrimers was designed having amino-functionalized periphery and ethylenediamine core. A repeating motif of bis(2-aminoethyl)glycine was used for generation growth up to the third generation. The new dendritic molecules of zero, first, second and third generation were tested for their ability to enhance the deposition of 5-fluorouracil in the different layers of human skin ex vivo by using Franz diffusion cells. The results suggest that the new dendrimers, at a concentration of 20 mg/mL in 60 % propylene glycol in water as vehicle, are able to deliver 5-fluorouracil at the...
|
|
|
Calcium phosphate bone cements: Synthesis, Characterization and drug release properties
Doubek, Jiří ; Paraskevopoulos, Georgios (advisor) ; Kováčik, Andrej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Author: Jiří Doubek Supervisor: Dr. Georgios Paraskevopoulos, Ph.D. Title of Thesis: Calcium phosphate bone cements: Synthesis, characterization and drug release properties Non-healing bone traumas are currently a complication, which may disable a patient from active life for a long period. Due to the fact that bone mass consists mostly of hydroxyapatite, a derivative of calcium phosphate - calcium phosphate cement (CPC) - is studied as an injectable bone substitute. The cement's characteristics (low setting temperature, injectability, bioactivity, and resorbability) are very promising. Furthermore, the possibility to incorporate a drug in the formulation that would support the healing process opens a way for new therapeutic options. Firstly, the aim of this research was to synthesize a high-quality α-tricalcium phosphate (α-TCP) and characterize its properties. Subsequently, the prepared α-TCP was used for the preparation of an injectable and washout resistant cement paste. Finally, the properties of developed pure or ibuprofen-loaded cement were examined by X-ray diffraction, Raman spectra, compressive strength, scanning electron microscopy, and dissolution studies. The obtained data revealed that...
|
|
|
Study of the effect of cholesterol concentration on monolayer models
Šrámová, Eliška ; Paraskevopoulos, Georgios (advisor) ; Svačinová, Petra (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Author: Eliška Šrámová Supervisor: Dr. Georgios Paraskevopoulos, Ph. D Consultant: Mgr. Anna Nováčková Title of Thesis: Study of the effect of cholesterol concentration on monolayer models Skin is composed of 3 major layers: hypodermis, dermis, and epidermis. The uppermost layer, which is called stratum corneum (SC), has a unique structure resembling a well-built wall. Corneocytes represent bricks and the lipid matrix works like a mortar. Ceramides, free fatty acids, and cholesterol (Chol) are the main lipids creating the human SC matrix. In a healthy SC, the ratio of these lipids is equimolar. This ratio is crucial, not only to maintain the barrier function of the skin, but also for the organization of lipids in SC. Chol appears to be required for the correct lamellar organization, and the ordering of lipids inside of the lamellar formation (lateral organization) in SC. Abnormalities in the ratio of the lipids and depleted amount of Chol can lead to a disruption of the skin barrier function resulting in skin disease or multisystemic diseases (e.g. X-linked ichthyosis, Conradi-Hünermann-Happle syndrome, and CHILD syndrome.) The present work deals with a Chol deficiency study on lipid organization on...
|
|
|
Pharmaceutical applications of polyesters as drug nanocarriers
Staňková, Petra ; Holas, Ondřej (advisor) ; Paraskevopoulos, Georgios (referee)
Charles University Faculty of Pharmacy in Hradci Králové Department of Pharmaceutical Technology Consultant: PharmDr. Ondřej Holas, PhD. Student: Petra Staňková Title of Thesis: Pharmaceutical applications of polyesters as drug nanocarriers Nanoparticles are nowadays intensively studied and perspective type of a drug carrier. Its potential is based on a possibility of targeted drug delivery and controlled drug release. The theoretical part is about nanoparticles types, polymers derived from α-hydroxyacids (PLA, PGA, PLGA). Focus is given on methods of nanoparticles preparation: dispersion of preformed polymers or the polymerization of monomers. The modification of particles surface and practical use of nanomedicine in healthcare are described in other chapters. The research in experimental part is focused on the influence of different types of PLGA and their weighing on the size, polydispersity, nanoparticles zeta potential and encapsulation efficiency of rhodamine B. Nanoparticles were prepared by nanoprecipitation method or by solvent evaporation method. The Zetasiser ZS 90 device was used to measure the size of the nanoparticles and to measure zeta potential. The result of the research shows the most suitable weighing for creation of nanoparticles is 25 mg. The samples of this weighing show a...
|
|
|
Effect of the generation of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil
Houšková, Denisa ; Paraskevopoulos, Georgios (advisor) ; Holas, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Supervisor: Dr. Georgios Paraskevopoulos, Ph.D. Consultant: Mgr. Anna Nová ková Author: Denisa Houšková Title of thesis: Effect of the generation of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil. Dendrimers can be defined like highly branched, star-shaped macromolecules with nanometer-scale dimensions and unlimited applications in both biological and materials sciences. Polyamidoamine (PAMAM) dendrimers have been used to effectively enhance the (trans)dermal drug delivery of several active substances. Inspired by the structure of PAMAM dendrimers, a new class of dendrimers was designed having amino-functionalized periphery and ethylenediamine core. A repeating motif of bis(2-aminoethyl)glycine was used for generation growth up to the third generation. The new dendritic molecules of zero, first, second and third generation were tested for their ability to enhance the deposition of 5-fluorouracil in the different layers of human skin ex vivo by using Franz diffusion cells. The results suggest that the new dendrimers, at a concentration of 20 mg/mL in 60 % propylene glycol in water as vehicle, are able to deliver 5-fluorouracil at the...
|
|
|
Calcium phosphate bone cements: Synthesis, Characterization and drug release properties
Doubek, Jiří ; Paraskevopoulos, Georgios (advisor) ; Kováčik, Andrej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Author: Jiří Doubek Supervisor: Dr. Georgios Paraskevopoulos, Ph.D. Title of Thesis: Calcium phosphate bone cements: Synthesis, characterization and drug release properties Non-healing bone traumas are currently a complication, which may disable a patient from active life for a long period. Due to the fact that bone mass consists mostly of hydroxyapatite, a derivative of calcium phosphate - calcium phosphate cement (CPC) - is studied as an injectable bone substitute. The cement's characteristics (low setting temperature, injectability, bioactivity, and resorbability) are very promising. Furthermore, the possibility to incorporate a drug in the formulation that would support the healing process opens a way for new therapeutic options. Firstly, the aim of this research was to synthesize a high-quality α-tricalcium phosphate (α-TCP) and characterize its properties. Subsequently, the prepared α-TCP was used for the preparation of an injectable and washout resistant cement paste. Finally, the properties of developed pure or ibuprofen-loaded cement were examined by X-ray diffraction, Raman spectra, compressive strength, scanning electron microscopy, and dissolution studies. The obtained data revealed that...
|
|
|
Effect of the concentration of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil
Chladová, Pavlína ; Paraskevopoulos, Georgios (advisor) ; Holas, Ondřej (referee)
Effect of the concentration of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-Fluorouracil Pavlína Chladová Dendrimers are synthetic, symmetrically tree-like branched molecules. They are composed of repeating units (monomers). They have high density of surface functional groups and spherical shape in solution. Since their molecular weight is highly controllable, they are characterized by monodispersity and this is their main difference from classical polymers. Dendrimers have a wide spectrum of applications in biomedicine. Due to the empty space between the branches of the molecule, they can encapsulate drugs, and by conjugation and complexation to the surface groups, they are able to carry even larger drug molecules. Thus, dendrimers can be used as drug delivery systems. In addition, they have been used for skin application of several active molecules, either as topical or transdermal delivery. Suitable properties for (trans)dermal application have been demonstrated for dendrimers which consist of monomers with amine groups and are connected with amide bonds. The goal of this thesis was the preparation of dendrimers with these characteristics and the evaluation of their concentration influence to the permeability of 5-Fluorouracil (5-FU) to human...
|
guest ::
