Development of Docetaxel-loaded Folate-modified Poly(lactic-co-glycolic acid) Particles
| Author | Yuri Poltavets | en |
| Author | Vasilisa V. Zavarzina | en |
| Author | Sergey L. Kuznetsov | en |
| Author | Anna A. Krasheninnikova | en |
| Author | Danil O. Dronov | en |
| Author | Nadezhda V. Gukasova | en |
| Author | Valentina G. Shuvatova | en |
| Author | Vadim Yu. Balabanyan | en |
| Issued Date | 2019-12-31 | en |
| Abstract | Background: Poly(lactic-co-glycolic acid) (PLGA) particles with small vector molecules are used for targeted delivery of anticancer agents. To be effective, they must be small, noncytotoxic, sterile, and stable. Aim: The aim of this study was to prepare docetaxel-loaded folate-modified PLGA-based nanoparticles (FD-Dtx-NPs) and to assess their as parenteral folate-receptor targeted delivery systems during γ-sterilization and long-term storage. Materials and Methods: NPs were prepared by oil/water single emulsion-solvent evaporation method and simultaneous loading of polymer particles with docetaxel and folic acid derivative. NPs’ physicochemical characteristics and antitumor activity were assessed. Findings: FD-Dtx-NPs presented uniform characteristics over repeated measurements: ~250 nm size, 2.5% docetaxel content in the finished lyophilizate. The observed slow docetaxel release from FD-Dtx-NPs was acceptable for proposed usage. γ-irradiated NPs were sterile under all tested protocols and maintained their physicochemical properties at a 10-kGy cumulative dose, 0.500 Gy/s dose rate, and 5.57-h exposure. No significant differences were observed in physicochemical characteristics of FD-Dtx-NPs over 12 months. Finally, FD-Dtx-NPs showed a high anticancer activity in vitro. Conclusion: The proposed method generates FD-Dtx-NPs with reproducible characteristics, high activity, and elevated stability during the long-term storage. Results of γ-sterilization and stability studies may be valuable for the development of polymer-based drugs. | en |
| DOI | https://doi.org/10.4103/jrptps.JRPTPS_64_19 | en |
| Keyword | Docetaxel | en |
| Keyword | folic acid | en |
| Keyword | γ-irradiation | en |
| Keyword | long-term storage | en |
| Keyword | nanoparticles | en |
| Keyword | poly(lactic-co-glycolic acid) | en |
| Keyword | stability | en |
| Publisher | Brieflands | en |
| Title | Development of Docetaxel-loaded Folate-modified Poly(lactic-co-glycolic acid) Particles | en |
| Type | Research Article | en |