Design and synthesis of new heterocyclic compounds containing 5-[(1-1,2,4-triazol-1-yl)methyl]-3-1,2,4-triazole-3-thione structure as potent hEGFR inhibitors.

EGFR is one of the important mediators of the signaling cascade that determines key roles in various biological processes such as growth, differentiation, metabolism and apoptosis in the cell in response to external and internal stimuli. In recent years, it has been proven that although this enzyme activity is tightly regulated in normal cells, if the enzyme activity cannot be controlled, it can lead to malignancy. EGFR is also considered a prominent macromolecule in targeted cancer chemotherapy.

Preparation, characterization and evaluation of cisplatin-bound triblock polymeric micelle solution for ovarian cancer treatment.

The main objective of this study was to prepare cisplatin (CDDP) bound triblock polymeric micelle solution which will have a hydrophilic shell not being phagocytosed by mononuclear phagocyte system, and evaluate behavior for the treatment of ovarian cancer. For this aim, CDDP was bound to polyglutamic acid (PGA) and the triblock polymer was prepared using polyethylene glycol)-polylactide--glycolide (PEG-PLGA). CDDP-bound triblock copolymer conjugation was characterized, release and permeability studies were performed using USP II method and Caco-2 cell lines, respectively.

Brain-targeted, drug-loaded solid lipid nanoparticles against glioblastoma cells in culture.

The aim of this study was the preparation of solid lipid nanoparticles (SLN) formed from cetyl palmitate with having targeting molecules for monocarboxylate transporter-1 (MCT-1): β-hydroxybutyric acid and anticancer agents: carmustine (BCNU) and temozolomide (TMZ) for enhanced anti-proliferation against glioblastoma multiforme (GBM). Properties including size, morphology, chemical structure, zeta potential, drug encapsulation efficacy, drug release, biocompatibility, stability were determined, and in vitro studies were done. BCNU and TMZ loaded SLNs had a hydrodynamic size of 227 nm ± 46 a zeta potential of -25 mV ± 4 with biocompatible features.

An intravenous application of magnetic nanoparticles for osteomyelitis treatment: An efficient alternative.

The infection of bone and bone marrow is called osteomyelitis. Treatment is difficult since antibiotics can not reach with enough concentration to the infected area. For the first time in this study, we have developed gentamicin-loaded magnetic gelatin nanoparticles (GMGNPs) for nanocarrier-mediated and magnetically targeted osteomyelitis therapy.

Development of Ultrasound-Triggered and Magnetic-Targeted Nanobubble System for Dual-Drug Delivery.

Non-small cell lung cancer (NSCLC) constitutes more than 85% of lung cancer case. Pemetrexed is used to treat types of NSCLC, and pazopanib is used for some types of soft tissue sarcoma. The aim of the study was development of pemetrexed and pazopanib carrying nanobubble system with magnetic responsiveness and ultrasound sensitivity properties for targeted NSCLC therapy.

In vitro and in vivo evaluation of folate receptor-targeted a novel magnetic drug delivery system for ovarian cancer therapy.

Doxorubicin is widely used anticancer drug; however, use of doxorubicin is limited. Under externally applied magnetic field, magnetic agents can help to transport drug directly to tumor. Folate receptor is overexpressed in ovarian carcinomas.

Synthesis of Methotrexate Loaded Chitosan Nanoparticles and in vitro Evaluation of the Potential in Treatment of Prostate Cancer.

The objective of the study was to investigate the cytotoxic and apoptotic effects of Methotrexate (MTX)-loaded chitosan (CS) on LNCaP prostate cancer cell line in vitro. For this purpose, CS nanoparticles (NPs) were synthesized through ionic gelation method and MTX was loaded into the carrier with encapsulation. SEM images of the CS NPs have revealed that they have size of about 85 nm in mono-disperse manner.

Development of gemcitabine-adsorbed magnetic gelatin nanoparticles for targeted drug delivery in lung cancer.

Magnetic iron oxide nanoparticles (IONPs) were coated with gelatin type B by means of the two-step desolvation method. Drug loading by adsorption was studied under various conditions such as different temperature, contact time, pH, and initial gemcitabine concentration. Further, Langmuir isotherm curves were constracted and constants were calculated.