Wyniki wyszukiwania - BazTech

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Macromolecular conjugates of paclitaxel: Synthesis, characterization, and In Vitro paclitaxel release studies based on HPLC validated method

Stefanowicz Z., Sobczak M., Piętniewicz A., Kołodziejski W. L.

Acta Chromatographica

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2016

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Vol. 28, no. 1

99--117

EN

Biodegradable and bioresorbable macromolecular conjugates of paclitaxel were prepared. The release of drug from conjugates has been carried out in vitro at 37 °C in phosphate buffered saline solution (PBS, pH 7.4), with 0.1% (w/v) Cremophor® EL. Periodically, all the solution in the samples was removed and replaced with fresh buffer until limit of detection (LOD) of paclitaxel was released. The quantity of released drug was analyzed by means of high-performance liquid chromatography (HPLC) method. Chromatographic separations were conducted using the NUCLEODUR C18 Gravity column with a guard column at 30 °C. Mobile phase consisted of a mixture of acetonitrile, methanol, and deionized water (60:2:38). The flow rate was 1.0 mL min -1, and paclitaxel was detected at 229 nm, retention time of 3.5 min. The applied analytical method was validated according to International Conference on Harmonization (ICH) procedures or recommendations. The chromatographic separation was excellent. The linearity in the range 0.1–4.5 μg Ml -1 was found to be very good (R2 = 0.9999). LOD and limit of quantification (LOQ) were calculated to be 0.023 μg Ml -1 and 0.068 μg Ml -1, respectively. The release profiles were evaluated and compared. The process of paclitaxel release from Paclcon-2 conjugate seems to be the most interesting. Paclitaxel is released the longest and the most evenly.

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Wstępne badania nad syntezą i charakterystyką wielkocząsteczkowych koniugatów kamptotecyny

Sobczak M., Olędzka E., Plichta A., Kolmas J., Piotrowska U.

Engineering of Biomaterials

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2014

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Vol. 17, no. 128-129

36--39

PL

Otrzymano nowe wielkocząsteczkowe koniugaty kamptotecyny. Matryce polimerowe zostały otrzymane w wyniku polimeryzacji z otwarciem pierścienia ε-kaprolaktonu, glikolidu, rac-laktydu oraz węglanu trimetylenu. Zsyntezowane matryce i kamptotecynę połączono za pomocą 1,6-diizocyjanianu heksametylenu. Otrzymane koniugaty wielkocząsteczkowe scharakteryzowano za pomocą spektroskopii 1H i 13C NMR oraz FTIR. Toksyczność otrzymanych produktów polimerycznych oceniono na podstawie testów przeprowadzonych przy użyciu bakterii luminescencyjnych oraz pierwotniaków. Ponadto, przeprowadzono badania kinetyki uwalniania kamptotecyny w warunkach in vitro.

EN

New macromolecular conjugates of camptothecin were prepared. The polymeric matrixes were obtained by the ring-opening polymerization of ε-caprolactone, glycolide, rac-lactide or trimethylene carbonate. The synthesized polymers and camptothecin were coupled via 1,6-hexamethylene diisocyanate. The synthesized macromolecular conjugates of camptothecin were characterized by 1H and 13C NMR or FTIR spectroscopy. Toxicity of the obtained polymeric products were evaluated with bacterial luminescence test and two protozoan assays. Furthermore, the in vitro release of camptothecin from the obtained conjugates was investigated.

3

Synteza biodegradowalnych antybakteryjnych poliuretanów

Sobczak M., Olędzka E., Dębek C.

Engineering of Biomaterials

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2011

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Vol. 14, no. 106-108

30--34

PL

W niniejszej pracy przedstawiono wyniki badań nad syntezą nowych biodegradowalnych antybakteryjnych poliuretanów (PURs). PURs zostały otrzymane w reakcji alifatycznych oligoestrów, ciprofloksacyny i diizocyjanianu 1,6-heksametylenu. Polimery zostały scharakteryzowane za pomocą technik FT-IR, 1H i 13C NMR. Przeprowadzono badania uwalniania ciprofloksacyny z otrzymanych koniugatów poliuretanowych w warunkach in vitro. Badania biodegradacji zostały przeprowadzone w roztworze buforowym o pH 7 w obecności Cholesterol esterase. Wstępne wyniki sugerują, że nowe biodegradowalne antybakteryjne poliuretany rokują pozytywnie na zastosowanie ich jako materiały implantacyjne.

EN

A series of novel biodegradable antimicrobial polyurethenes (PURs) were synthesized by the reactions between aliphatic oligoesters, ciprofloxacin and 1,6- hexane diisocyanate. The obtained polymers were characterized by FT-IR, 1H and 13C NMR techniques. The in vitro release of ciprofloxacin from the received polyurethane conjugates was investigated. The biodegradation studies were carried out by the incubating of PURs with Cholesterol esterase in the buffer solution at pH 7. The preliminary results suggest that these novel antimicrobial polyurethanes are promising for application as the implantation materials.