| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1394039 | European Journal of Medicinal Chemistry | 2015 | 8 Pages |
•mPEG-b-P(CABCL-co-ACL) copolymers was synthesized and modified with folic acid.•Polymer characterization and drug release were studied.•Antitumor activity of targeted 5-FU delivery system was documented both in vitro and in vivo.•Biocompatibility and safety of polymer was also investigated.
Traditional chemotherapeutic drugs remain the major treatment for advanced colorectal cancer. However, due to the lack of tumor specificity these drug also destroy healthy tissue and organs, which has been the main reason for treatment failure and mortality. Folate-based drug delivery systems for improving nanoparticle endocytosis have been used to address these problems. Here, folic acid (FA) conjugated mPEG-b-P(CABCL-co-ACL) diblock copolymers were synthesized and characterized by TEM and NMR. Drug loaded nanoparticles were prepared using dialysis method and was obtained with a mean diameter of 45.2 nm with sustained in vitro release profile. In vitro cytotoxicity assay indicated that the cytotoxicity of folate modified nanoparticles were significantly increased compared to free drug and non-folate nanoparticles. In addition, results of hemolytic and histopathologic study suggested that the non-loaded nanoparticle (NL/NP) was non-toxic and biocompatible at the testing concentration. Moreover, in vivo results showed that FA/5-FU/NP effectively inhibited growth of HCT-8 cell-based xenograft tumors in BALB/c mice and revealed stronger antitumor efficacy than other treated groups. Thus, both in vitro and in vivo results exhibited that the folate conjugated mPEG-b-P(CABCL-co-ACL) copolymers have great potential to be used as sustainable and specific colon cancer targeting delivery system for anticancer agents.
Graphical abstractThe synthesis of 5-fluorouracil loaded, folate-conjugated nanoparticles for targeted delivery to cancer and antitumor efficacy evaluation both in vitro and in vivo.Figure optionsDownload full-size imageDownload as PowerPoint slide
