Diagnosis of cancer in the early stages requires sensitive magnetic resonance (MR) probes to detect low concentrations of magnetic substances. In this study, ultrasensitive magnetic resonance contrast agents (UMRCAs) composed of magnetic nanocrystals and amphiphilic block copolymers were synthesized for cancer detection using polyethylene glycol and fatty acid. The chemical structures and the compositions of PEGylated magnetic nanoparticles were analyzed. UMRCAs displayed remarkable colloidal stability and high sensitivity as MR probes. Furthermore, UMRCAs exhibited low cytotoxicity and excellent cancer detection ability in an in vivo animal model.
Hyaluronic acid (HA) coated drug carriers (HCDCs) were successfully synthesized by chemical conjugation method for targeted delivery of doxorubicin (DOX) as a prototype anticancer drug to CD44 expressed human breast cancer cell. From XPS analysis, the HCDCs by conjugation methods demonstrated the superior HA fixation amount and colloidal stability compared with the nanoparticles by nanoprecipitation. The cytotoxicity of the HCDCs formulation accessed by the MTT assay against the higher CD44 expressed cell line (MDA-MB-231) and lower CD44 expressed cell line (ZR-75-1) human breast cancer cell lines demonstrated that the HCDCs formulation exhibited excellent tumoricidal effect and their affinity to cancer cells was predominant. The in vitro drug release profile of the HCDCs showed sustained release behavior and after 14 days, 80% of the encapsulated DOX was released due to a high release rate of DOX from HCDCs. We synthesized that HCDCs have therapeutic potentials of cancer as a target specific fashion by increasing the tumoricidal efficacy of targeted cancer cells while reducing their cytotoxicity of non-targeted cells to minimize the side effect.
We prepared magnetic (Fe(3)O(4)) poly epsilon-caprolactone (PCL) nanoparticles (mean diameter 164 +/- 3 nm) containing an anticancer drug (gemcitabine) using emulsion-diffusion method in order to develop more efficient drug delivery for cancer treatment. Nanoparticles were smooth, well individualized and homogeneous in size. The values of magnetizations for the magnetic PCL nanoparticles were observed around 10.2 emu/g at 2000 Oe magnetic field intensity and showed super-paramagnetic property. In case of the drug, the drug loading contents was 18.6% and entrapment efficiency was 52.2%. The anti-tumor effects caused by these particles were examined using nude mice bearing subcutaneous human pancreatic adenocarcinoma cells (HPAC) in vivo. We divided that these mice were randomly assigned to one of five treatment groups for experimental contrast. The antitumor effect was showed with 15-fold higher dose when compared to free gemcitabine. From the result, the magnetic PCL nanoparticles may provide a therapeutic benefit by delivering drugs efficiently to magnetically targeted tumor tissues, thus achieving safe and successful anti-tumor effects with low toxicity.
Magnetic poly(ethyl-2-cyanoacrylate) (PECA) nanoparticles containing anti-cancer drugs (Cisplatin and Gemcitabine) were prepared by inter-facial polymerization. The spherical nanoparticles (d = 250 +/- 15 nm) with smooth surfaces and moderately uniform size distributions were obtained. The amount of magnetite encapsulated inside the polymer matrix was increased up to 14.26% (w/w) by controlling the initial weight ratio of monomer/magnetite. It was found that the amount of Cisplatin encapsulated in the magnetic nanoparticle is much higher than that of Gemcitabine because Cisplatin (hydrophobic) is highly soluble in the oil phase and encapsulated easier inside nanoparticles compared to Gemcitabine (hydrophilic). The presence of magnetite and its super-paramagnetic characteristic were confirmed by FTIR spectra and VSM. In-vitro experiments of drug release and magnetic mobility under external magnetic field demonstrated that magnetic poly(ethyl-2-cyanoacrylate) (PECA) nanoparticles can be a highly versatile magnetic drug carrier with sustained release behaviour and sufficient magnetic susceptibility.
In general, high broth viscosity is a key factor to be considered in a submerged fermentation of filamentous fungi. High broth viscosity was also observed in a batch fermentation of Monascus sp. J101 at 30 degrees C. In a batch culture at 30 degrees C, most cell growth was accomplished within 48 h, which induced highly entangled clumps. The resultant high viscosity induced heterogeneity inside the fermentor, poor oxygen transfer, and low pigment yield. However, these problems could be overcome by reducing fungal growth rate through culture at low temperature (25 degrees C). Cell growth was moderate and continued for 120 h, and low viscosity was maintained. The DO levels remained at 50% or higher with good mixing. As a result, the pigment yield at 25 degrees C was 10 times greater than at 30 degrees C.
Novel multifunctional magnetic polycation drug carriers (MPDCs) were synthesized to provide simultaneous magnetically targeted cancer therapy and diagnosis via magnetic resonance imaging (MRI). The MPDCs consist of ultra-sensitive magnetic nanocrystals as MR probes and for magnetic targeting, and a chemotherapeutic agent encapsulated in poly(hexadecylcyanoacrylate) (PHDCA) nanoparticles. The PHDCA nanoparticles were further coated with polycationic polyethylenimine (PEI) to enhance cellular uptake efficiency. The MPDCs demonstrated ultra-sensitivity via MRI and sufficient magnetic mobility under an external magnetic field. Drug loading efficiency and release kinetics were also investigated. From the cell viability data, the MPDCs were nontoxic and the doxorubicin hydrochloride (DOX)-loaded MPDCs exhibited excellent tumorcidal efficacy.
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