Preparation and self-assembly of amphiphilic polylysine dendrons

Polylysine dendrons with lipid tails prepared by divergent solid-phase synthesis showed self-assembling properties in aqueous solutions.</p

Zebrafish embryos allow prediction of nanoparticle circulation times in mice and facilitate quantification of nanoparticle-cell interactions

The zebrafish embryo is a vertebrate well suited for visualizing nanoparticles at high resolution in live animals. Its optical transparency and genetic versatility allow noninvasive, real-time observations of vascular flow of nanoparticles and their interactions with cells throughout the body. As a consequence, this system enables the acquisition of quantitative data that are difficult to obtain in rodents. Until now, a few studies using the zebrafish model have only described semiquantitative results on key nanoparticle parameters. Here, a MACRO dedicated to automated quantitative methods is described for analyzing important parameters of nanoparticle behavior, such as circulation time and interactions with key target cells, macrophages, and endothelial cells. Direct comparison of four nanoparticle (NP) formulations in zebrafish embryos and mice reveals that data obtained in zebrafish can be used to predict NPs' behavior in the mouse model. NPs having long or short blood circulation in rodents behave similarly in the zebrafish embryo, with low circulation times being a consequence of NP uptake into macrophages or endothelial cells. It is proposed that the zebrafish embryo has the potential to become an important intermediate screening system for nanoparticle research to bridge the gap between cell culture studies and preclinical rodent models such as the mouse

pH duyarlı anti kanser ilaç taşıyıcı nanosistemler.

In the recent years, development of various organic and inorganic nano-sized systems has gained great interests especially for cancer diagnosis and treatment and intense researches are carried out in this area. Regarding to the recent trends for drug delivery system design, the novel approaches for drug carriers are mainly based on development of smart and nano-size drug carriers which are targeted to cancer cells. Hence, for an effective tumor-targeted delivery device, besides its chemical structure further criteria such as detection of tumor site and sensitivity to the higher temperature and lower pH of the tumor compare to rest of the body gains importance. The aim of this study is to design and prepare polysebacic anhydride (PSA) based nanocapsules (NCs) loaded with Doxorubicin (DOX) which is an anti cancer drug. In order to obtain an intelligent delivery system, drug-loaded nanocapsules were coated with pH sensitive poly (L-histidine). PSA nano-carriers were firstly loaded with DOX and then in order to introduce pH sensitivity, they were coated with poly (L-histidine). PLH-coated NCs were modified with polyethylene glycol (PEG) to prevent their macrophage uptake. Drug release profile from this system was examined in two different buffer solutions prepared as acidic (pH 4) and physiological (pH 7.4) media. The physical and chemical properties of the nano particles were characterized by Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS), ultraviolet and visible absorption spectroscopy (UV-VIS), and scanning electron microscopy (SEM). In vitro studies of the prepared nanocapsules were performed on MDA-MB-231 breast cancer cells by using WST Kit 8 cell viability test. In order to obtained results, pH sensitive nanocapsules with size 230 nm exhibited cellular uptake and promising intracellular release of drug.Ph.D. - Doctoral Progra

Fenollü ve bisfenollü polibenzoksazinlerin ısısal olarak karakterizasyonu.

Although, several researches on synthesis and characterization of benzoxazines and polybenzoxazines have appeared in the literature, detailed studies on thermal characterization are still limited. In this study, polymerization and thermal degradation mechanisms of benzoxazines were investigated via direct pyrolysis mass spectrometry. Benzoxazine monomers prepared by reactions of phenol or bisphenol- A with aniline or methyl amine were analyzed to investigate the effects of the structures of phenyl and amine groups on both polymerization and thermal degradation behaviours. It has been proposed in the literature that polymerization of benzoxazines occurs by ring opening polymerization of oxazine ring; cleavage of O-CH2 bond of the oxazine ring and attack of n-CH2 group to phenol or bisphenol-A ring. However, the direct pyrolysis mass spectrometry analyses of polymerization and thermal degradation of benzoxazines pointed out that after the cleavage of O-CH2 bond of the oxazine ring, polymerization proceeded through opposing pathways. Strong evidences confirming coupling of (CH3)NCH2 or (C6H5)NCH2 groups yielding dimers involving diamine linkages were detected. Polymerization of the dimer by the reactions with the corresponding monomers was proposed. In case of benzoxazines based on bisphenol-A, the results indicated polymerization of the dimer ii by coupling of both of the oxazine rings. On the other hand, polymerization of the dimer through the ethylene units (vinyl polymerization) in case of benzoxazine monomer based on phenol and methyl amine was also noted. For polybenzoxazines based on aniline another polymerization pathway involved attack of radicals generated by cleavage of the oxazine ring to aniline ring. Multi-step thermal decomposition was observed for all the polybenzoxazines under investigation confirming the presence of units with different structures and stabilities.M.S. - Master of Scienc

The use of pyrolysis mass spectrometry to investigate polymerization and degradation processes of methyl amine-based benzoxazine

In this study, direct pyrolysis mass spectrometry, DP-MS, was applied to investigate curing and polymerization mechanisms of phenol and methyl amine-based benzoxazine monomer, and thermal decomposition and crosslinking characteristics of the corresponding polybenzoxazine. The results indicated opposing polymerization reaction routes besides the generally accepted one. The cleavage of C-O bonds of the oxazine rings either followed by transformation into a polymer constituting ortho or para substituted phenol units or by coupling of -NCH2. Polymerization of the dimer generated by coupling of -NCH2, by either further reactions with benzoxazine monomers or by radicalic vinyl polymerization, yields different polymeric structures. The evolution of alkyl amines and diamines involving more than three carbon atoms at early stages of pyrolysis and the multi-step thermal decomposition detected confirmed this proposal. The formation of char residues were associated with crosslinking of fragments and/or polymer backbone generated by the loss of diamine units and side chains

Thermal degradation of polysiloxane and polyetherester containing benzoxazine moieties in the main chain

In this study investigation of thermal characteristics of polysiloxane and polyetherester containing benzoxazine moieties in the main chain was performed via pyrolysis mass spectrometry. Pyrolysis mass spectrometry analyses revealed that the thermal stability and the extent of cross-linking enhanced when the benzoxazine moieties were separated by thermally more stable units such as siloxanes. However, when the siloxane chain units were long, possibility of polybenzoxazine growth decreased significantly and benzoxazine moieties were evolved in the temperature range where polysiloxane degradation took place. (C) 2010 Elsevier B.V. All rights reserved. Keyword

Poly(sebacic anhydride) nanocapsules as carriers: effects of preparation parameters on properties and release of doxorubicin

Poly(sebacic anhydride) (PSA) is a promising polymer for the production of drug delivery vehicles. The aim of this work is to study the effect of preparation parameters on the quality of the nanoparticles. In this study, doxorubicin (DOX)-loaded PSA nanocapsules were prepared by an emulsion method. Effects of factors such as type of organic solvent, co-solute (surfactant) and its concentration on drug-loading efficiency, particle size and size distribution, morphology and release profile were examined to gain insight in the preparation and stability of nanostructures. Particles with sizes in the range of 218-1198 nm were prepared. The smallest particles with a narrow size distribution were prepared by using polyvinyl alcohol as a co-solute and dichloromethane as a solvent. Efficiency and intracellular release of doxorubicin from the formulated particles were studied on MDA-MB-231 cells. It was observed that DOX-loaded PSA particles can diffuse into the cells and intracellular antitumour activity is directly related to the released amount of drug from the PSA nanocapsules

pH-Responsive Nano Carriers for Doxorubicin Delivery

Purpose The aim of this study was to design stimuli-responsive nanocarriers for anti-cancer drug delivery. For this purpose, doxorubicin (DOX)-loaded, polysebacic anhydride (PSA) based nanocapsules (NC) were combined with pH-sensitive poly (L-histidine) (PLH)