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

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

  • BMC Pharmacol Toxicol. 2021 Jan 6;22(1):1. doi: 10.1186/s40360-020-00461-y.
Danni Li 1 Shaogang Liu 1 Jiahao Zhu 1 Liqun Shen 1 Qi Ying Zhang 1 Hua Zhu 2
Affiliations

Affiliations

  • 1 School of Chemistry and chemical engineering, Guangxi Key Laboratory for Polysaccharide Materials and Modifications, Guangxi University for nationalities, No.158, Da Xue Xi street, Xixiangtang District, Nanning, 530006, Guangxi Province, China.
  • 2 College of Pharmacy, Guangxi University for Chinese medicine, No.13, Wu He street, Qingxiu District, Nanning, 530200, Guangxi Province, China. che_2020@163.com.
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-α-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.

Keywords

Anti-tumor activity; Folic acid; Huh7 human hepatocellular carcinoma line; Nano-micelles; Nitidine chloride; TPGS.

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