Lecturer , Mansoura University
Synthesis and characterization of a unique polymeric Micelle loaded with Cabazitaxel (Cancer therapeutic drug). The loading content and efficiency of these micelles is promising. The biocompatibility and releasing profile of these micelle were very interesting. Our hypothesis confirmed by several chemical and biological experiments
Abstract: Authors: Khaled M. Elattar ; Ibrahim Youssef ; Ahmed A. Fadda Article URL: http://www.tandfonline.com/doi/full/10.1080/00397911.2016.1166252?ai=z4&mi=3fqos0&af=R Citation: Synthetic Communications Publication Date: 2016-03-22T08:20:29Z Journal: Synthetic Communications: An International Journal for Rapid Communication of Synthetic Organic Chemistry
Pub.: 22 Mar '16, Pinned: 28 Jul '17
Abstract: Photo-active trans-3-(4-pyridyl)acrylic acid (PYA) modified chitosan (CSPA) was synthesized with different functionalization degrees and extensively examined using Fourier transform infrared spectra (FTIR), 1H nuclear magnetic resonance (NMR) in order to elucidate the chemical structure of the modified biopolymer. The modified CSPA with various substitution degrees were casted in form of thin membranes and cross-linked under photo-chemical condition by exposure to ultra-violet light via [2π + 2π] cycloaddition reaction of the incorporated PYA units. The photo-induced reaction were examined using UV-visible light spectra and the cross-linked hydrogel were investigated using both XRD and scanning electron microscope (SEM). Also, the mechanical properties of the hydrogel membranes were studied by measuring the variations of both tensile strength and elongation against corss-linking densities.
Pub.: 24 Apr '17, Pinned: 28 Jul '17
Abstract: We report the synthesis of an amphiphilic triblock copolymer composed of a hydrophilic poly(ethylene glycol) (PEG) block, a central poly(acrylic acid) (PAA) block, and a hydrophobic poly(methyl methacrylate) (PMMA) block using atom transfer radical polymerization technique. We examined the self-assembly of PEG-b-PAA-b-PMMA copolymers in aqueous solutions forming nanosized micelles and their ability to encapsulate hydrophobic guest molecules such as Nile Red (NR) dye and cabazitaxel (CTX, an anticancer drug). We used 2,2β′-(propane-2,2-diylbis(oxy))-diethanamine to react with the carboxylic acid groups of the central PAA block forming acid-labile, shell cross-linked micelles (SCLM). We investigated the loading efficiency and release of different guest molecules from non-cross-linked micelles (NSCLM) and shell cross-linked micelles (SCLM) prepared by reacting 50% (SCLM-50) and 100% (SCLM-100) of the carboxylic acid groups in the PAA in physiologic (pH 7.4) and acidic (pH 5.0) buffer solutions as a function of time. We examined the uptake of NR-loaded NSCLM, SCLM-50, and SCLM-100 micelles into PC-3 and C4-2B prostate cancer cells and the effect of different micelle compositions on membrane fluidity of both cell lines. We also investigated the effect of CTX-loaded NSCLM, SCLM-50, and SCLM-100 micelles on the viability of PC-3 and C4-2B cancer cells compared to free CTX as a function of drug concentration. Results show that PEG-b-PAA-b-PMMA polymers form micelles at concentrations ≥11 μg/mL with an average size of 40–50 nm. CTX was encapsulated in PEG-b-PAA-b-PMMA micelles with 55% loading efficiency in NSCLM. In vitro release studies showed that 30% and 85% of the loaded CTX was released from SCLM-50 micelles in physiologic (pH 7.4) and acidic (pH 5.0) buffer solutions over 30 h, confirming micelles’ sensitivity to solution pH. Results show uptake of NSCLM and SCLM into prostate cancer cells delivering their chemotherapeutic cargo, which triggered efficient cancer cell death. PEG-b-PAA-b-PMMA micelles were not hemolytic and did not cause platelet aggregation, which indicate their biocompatibility.
Pub.: 15 Mar '16, Pinned: 28 Jul '17