透明质酸包裹的木犀草素胶束制备及其对小鼠肺癌移植瘤的抑制作用

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Abstract Objective: To prepare luteolin micelles encapsulated by hyaluronic acid and evaluate its inhibition on lung cancer xenografts in mice. Methods: Reverse phase evaporation method was used to prepare hyaluronic acid-coated luteolin micelles (HA-LE-MC). The prescription was screened with encapsulation efficiency and particle size as optimization indicators, and its apparent morphology，drug loa-ding, encapsulation efficiency and particle size were determined and finally in vivo imaging experiments and in vivo anti-tumor experiments. Results: The best mass ratio of poloxamer 407 (F127) and didecyl dimethyl ammonium bromide (DDAB) was 9 ∶1, and the particle size of HA-LE-MC was about (140.0±1.8) nm, the encapsulation rate was (61.2±2.4) %. The drug loading was (74.0±1.2) μg/mL. In vivo imaging experiments showed that micelles were concentrated in the tumor site after tail vein injection, indicating that micelles had strong tumor targeting. In vivo anti-tumor experiments showed that compared with luteolin HALEMC had stronger inhibitory effect on Lewis lung cancer xenograft tumors (P<0.01), and it had lower side effects compared with the positive drug cisplatin (P<0.05), and could enhance the immune function of tumor-bearing mice. Conclusion: The prepared HA-LE-MC had targeted properties, enhanced antitumor activity and could enhance the immune function of tumor-bearing mice and improve the survival of mice with explanted lung cancer.

Received: 06 October 2020

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http://zzs.ujs.edu.cn/xbyxb/EN/ OR http://zzs.ujs.edu.cn/xbyxb/EN/Y2021/V31/I01/33

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