Preparation Of Tf-BCNU-PLGA Nanoparticles And Effects On Rats C6 Glioma Cell

Background and purpose:Glioma is the most common intracranial tumor, micro-surgery, radiotherapy, chemotherapy and other measures, though effective, but results were not satisfactory, high relapse rate, the average survival time of patients do not more than one year. BCNU (carmustine,1,3-bis (2-chloroethyl)-1-nitrosourea, BCNU) is the most commonly used glioma chemotherapy drug, with fat-soluble and relatively low molecular weight, through the blood-brain barrier. However, intravenous administration of BCNU, a series of serious complications can occur such as bone marrow suppression, liver toxicity, lung fibrosis, the treatment effects were rather limited.Therefore, it is necessary to develop new BCNU release preparations, the prolonged half-life, increased bioavailability. This study has nano controlled-release system as a novel drug carrier to prepare the drug-loaded nanoparticles.with sustained release, high bioavailability and low side effects.Methods:Tf-BCNU-PLGA nanoparticles were prepared by ultrasonic emulsification solvent evaporation method, drug loading and encapsulation efficiency examined by ultraviolet spectrophotometry, nano-particle size measured by laser particle size measurer, nanoparticle morphology observed by transmission electron microscopy.Through the PLGA concentration, ultrasonic power, transferrin concentration, PVA concentration of orthogonal experimental design to optimize the Tf-BCNU-PLGA nanoparticles and the best conditions, and obtained the Tf-BCNU-PLGA nanoparticles to form study, in vitro release, stability and other aspects of study.Transferrin modified drug-loaded nanoparticles, no transferrin modified drug-loaded nanoparticles blank nanoparticles group, study of the rat C6 glioma cells inhibition ratesResults:The optimal orthogonal experimental design optimum conditions for PLGA concentration of 6%, ultrasonic power 500W, PVA concentration of 4.5%, transferrin concentration of 2%.Obtained under optimal conditions the Tf-BCNU-PLGA nanoparticles in the TEM physical particles are spherical, the average particle size of 0.138μm,3.53% drug loading,encapsulation efficiency was 17.65%.Dynamic dialysis method Tf-BCNU-PLGA nanoparticles at 37℃, pH7.4 phosphate buffer solution in the release characteristics.The results show that Tf-BCNU-PLGA nanoparticle drug delivery characteristics, burst effect significantly.Rat C6 glioma cell inhibition experiments showed that:empty nano-capsules no inhibition of tumor cells, indicating that carrier material biocompatibility, Tf-BCNU-PLGA nanoparticles on the inhibition of C6 rat glioma cells rate have higher slow-release inhibitory properties than the same amount of free drug, no transferrin modified nanoparticles.Conclusion:Tf-BCNU-PLGA nanoparticles showed good sphericity, narrow diameter distribution, high encapsulation efficiency and good inhibitory properties.