Paclitaxel (Ptx) is a taxane anticancer mitotic inhibitor, widely used in oncology for the last 20 years. Poor solubility of Ptx, as a consequence using of toxic solvents such as Cremofor EL, high affinity to P-glycoprotein are associated with serious side effects due to hypersensitivity reactions, low bioavailability and low therapeutic index. Development of new delivery solvent-free forms of Ptx is one of the key research problems in modern cancer chemotherapy. Ptx loaded into polylactic-co-glycolic acid (PLGA) nanoparticles (Ptx-PLGA-Nps) (size 200-300 nm) have been prepared using nanoprecipitation method. Impact of technological parameters on Ptx encapsulation efficacy and in vitro drug release was investigated. Drug encapsulation was determined using HPLC. Citotoxic activity and cell accumulation of nanosomal formulation of Ptx was studied on multiresistant cell line Jurkat WT (cells of human Т-limphoblastic leucosis). Obtained results suggest that formulation of PLGA Ptx nanoparticles have above 90-98% drug encapsulation efficacy, higher cell accumulation and cytotoxic activity.

Paclitaxel dosage form on nanoparticles of 200-300 nm based on lactic and glycolic acid copolymer was obtained by the co-precipitation method. The possibility of controlled release of paclitaxel at pH 7.4 for 24 h was studied in vitro. Studies on Jurkat/WT human T-lymphoblastic leukemia cells showed that incorporation of paclitaxel in the nanoparticles led to a 4-fold increase of its cytotoxicity (6.8×10(-6) M) in comparison with paclitaxel solution. The efficiency of compositions containing polysorbate-80 was comparable to that of non-modified nanoparticles containing paclitaxel.

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