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| Study on folic acid-modifed nanostructured lipid carriers loaded with gambogenic acid |
| Hits 468 Download times 1091 Received:February 05, 2023 |
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| DOI
10.11656/j.issn.1673-9043.2023.03.13 |
| Key Words
anti-tumor;breast cancer;folic acid;gambogenic acid;nanostructured lipid carrier |
| Author Name | Affiliation | E-mail | | SONG Xunan | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | YAN Hongli | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | MA Zhe | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | ZHANG Bing | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | ZHANG Ying | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | QIN Huan | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | ZHANG Yukun | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | PI Jiaxin | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | pijiaxin@tjutcm.edu.cn | | LIU Zhidong | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | liuzhidong@tjutcm.edu.cn |
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| Abstract
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| [Objective] To construct a folic acid(FA) modified nanostructured lipid carrier loaded with gambogenic acid(FA-GNA-NLC) to enhance the bioavailability of gambogenic acid(GNA),improve its accumulation in tumor sites,and reduce the systemic toxic side effects. Characterized the physical and chemical properties and evaluated the efficacy both in vivo and in vitro. [Methods] Nanostructured lipid carriers encapsulating GNA(GNA-NLC),modified with the FA via PEG linker,were constructed by emulsification-evaporation method. The formulations were characterized for particle size and zeta potential,morphology,encapsulation efficiency and drug loading. The cell uptake was performed on 4T1 cell and MDA-MB-231;the cytotoxicity in vitro was tested on 4T1 cell. Furthermore,the in vivo antitumor efficacy and bio-distribution assays were performed on female 4T1 tumor-bearing BALB/c mice. [Results] FA-GNA-NLC with round morphology,uniform particle size,(16.01±0.03) nm,potential(-6.8±0.59) mV,and encapsulation efficiency of 99% was prepared. The GNA-NLC modified with FA(FA-GNA-NLC) was successfully fabricated with a round morphology,a small size of(16.01±0.03) nm,a good uniformity,a potential of (-6.8±0.59) mV,and an encapsulation efficiency of 99%. Cytotoxicity and in vivo anti-tumor experiments show that FA-GNA-NLC performed higher anti-tumor efficiency,better tumor inhibition rate and lower toxicity to normal tissues than other group;cell uptake and biodistribution in vivo experiments show that FA-NLC performed better targeting,and significantly enhanced the accumulate at tumor tissues. [Conclusion] FA-GNA-NLC enhanced the anti-tumor activity of GNA,improved the accumulation in tumor sites. It can be concluded that the FA-GNA-NLC could be a potential and suitable vehicle for breast cancer. |
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