Preparation and evaluation of polymer based microcarriers for hydrophobic anti-cancer drugs

Demetçi, Demet
Chemotherapy is one of the most important treatments for cancer. However, systemic toxicity, drug resistance and unstable kinetics of the drug in the blood are serious problems of chemotherapy. The use of biodegradable polymers for controlled release of anticancer drugs has gained popularity in recent years. Controlled release of drugs from polymeric carriers has some advantages such as improvement in the efficiency of treatment, reduction in systemic toxicity and prevention of the drug resistance that is developed by the cancer cells. In this study, poly(D,L-lactide-co-glycolide) microparticles were used as carriers for the controlled release of all-trans-Retinoic acid, tamoxifen, tamoxifen citrate and idarubicin. It was aimed to prepare a drug carrier system for controlled release of hydrophobic anticancer drugs. The empty and drug loaded poly (D,L-lactide-co-glycolide) microparticles were prepared by solvent extraction/evaporation technique with single emulsion (oil/water). Optimized microparticles were characterized by using inverted light microscopy and scanning electron microscopy to examine their morphology and sizes. Drug content of microparticles and the amount of released drug were determined spectrophotometrically. In vitro toxicity of the microparticles on MCF-7 human breast cancer cells was investigated. It was revealed that the microparticles were smooth and spherical in shape. Their sizes differed in the range of 2-20 m. atRA-loaded microparticles showed approximately 90% encapsulation efficiency and it was confirmed that changing in drug/polymer ratio affected the extend of drug content. Increase in drug content caused a slower release pattern. Moreover, although the empty microparticles caused some toxicity, atRA-loaded PLGA microparticles showed slight cell growth inhibition.
Citation Formats
D. Demetçi, “Preparation and evaluation of polymer based microcarriers for hydrophobic anti-cancer drugs,” M.S. - Master of Science, Middle East Technical University, 2007.