Folic acid modified TPGS as a novel nano-micelle for delivery of nitidine chloride to improve apoptosis induction in Huh7 human hepatocellular?carcinoma.

ABSTRACT:

Background

The development of novel and effective drugs for targeted human hepatocellular?carcinoma still remains a great challenge. The alkaloid nitidine chloride (NC), a component of a traditional Chinese medicine, has been shown to have anticancer properties, but doses at therapeutic levels have unacceptable side effects. Here we investigate folic acid modified D-?-tocopheryl polyethylene glycol 1000 succinate (TPGS-FA) as a potential carrier for controlled delivery of the drug.

Methods

Synthesized TPGS-FA was characterized by FTIR, UV-visible and ¹H NMR spectroscopy, and TPGS loaded with NC was evaluated for its ability to induce apoptosis in Huh7 cells by Annexin V/PI and MTT assays, and observed by laser scanning confocal microscopy and inverted phase contrast microscopy.

Results

TPGS-FA/NC complexes were prepared successfully, and were homogenious with a uniform size of ~?14?nm diameter. NC was released from the TPGS-FA/NC complexes in a controlled and sustained manner under physiological conditions (pH?7.4). Furthermore, its cytotoxicity to hepatocarcinoma cells was greater than that of free NC.

Conclusions

TPGS-FA is shown to be useful carrier for drugs such as NC, and TPGS-FA/NC could potentially be a potent and safe drug for the treatment of hepatocellular?carcinoma.

SUBMITTER: Li D 

PROVIDER: S-EPMC7789002 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature