1.Characterization of paclitaxel-PLGA nanoparticles and their antitumor effects in vitro
Xiaojing WANG ; Zishuo GUO ; Haitong ZHANG ; Wanling CHEN ; Jialing LI ; Shouying DU ; Pengyue LI
China Pharmacy 2024;35(22):2721-2725
OBJECTIVE To characterize paclitaxel nanoparticles (PTX-PLGA-NPs) and evaluate their in vitro inhibitory effect on Lewis lung cancer cells. METHODS The PTX-PLGA-NPs prepared by the emulsion-solvent evaporation method were characterized in terms of particle size, polydispersity index (PDI), Zeta potential, microscopic morphology, encapsulation efficiency, drug loading, ultraviolet-visible absorption characteristics and stability. Using mouse Lewis lung cancer cells as the subjects and paclitaxel reference substance as the control, the cytotoxicity and in vitro killing activity of PTX-PLGA-NPs were detected using CCK-8 method and Calcein-AM/PI double staining method, respectively. The effects of PTX-PLGA-NPs on cell apoptosis and cell cycle were assessed by Annexin Ⅴ-FITC/PI staining method and PI staining method, respectively. RESULTS PTX-PLGA-NPs were spherical with an average particle size of (172.03±0.95) nm, PDI of 0.098±0.012, and Zeta potential of (-1.76±0.02) mV. The encapsulation efficiency and drug loading were (52.32±0.66)% and (7.07±0.18)%, respectively, and the ultraviolet-visible absorption characteristics were not affected by the carrier polylactic-co-glycolic acid. When stored in the dark at 4 °C for 7 days, no significant change was noted in particle size, and the average PDI (after 1, 2, 4 and 7 days of storage) was under 0.3. Compared with the paclitaxel reference substance group, the PTX-PLGA-NPs group had more cells in a state of death, the survival rate (at the PTX concentration of 11.2 μg/mL) was significantly decreased, and both the apoptosis rate and the proportion of G2 phase cells were significantly increased (P<0.05). CONCLUSIONS The prepared PTX-PLGA-NPs indicate homogeneity in particle size, uniform dispersion, stable properties, and stronger in vitro killing effect on lung cancer cells than PTX.