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Preparation and pharmacokinetics of glycyrrhetinic acid and cell transmembrane peptides modified with liposomes for liver targeted-delivery.
Li, Li; Chen, Anqi; Liu, Bingmi; Pan, Hao; Yu, Yanjie; Liu, Yu.
Afiliación
  • Li L; School of Pharmacy, Liaoning University, Shenyang 110036, People's Republic of China.
  • Chen A; Liaoning Key Laboratory of New Drug Research & Development, Shenyang 110036, People's Republic of China.
  • Liu B; School of Pharmacy, Liaoning University, Shenyang 110036, People's Republic of China.
  • Pan H; School of Pharmacy, Liaoning University, Shenyang 110036, People's Republic of China.
  • Yu Y; Liaoning Pharmaceutical Engineering Research Center for Natural Medicine, Shenyang 110036, People's Republic of China.
  • Liu Y; School of Pharmacy, Liaoning University, Shenyang 110036, People's Republic of China.
Biomed Mater ; 17(4)2022 05 13.
Article en En | MEDLINE | ID: mdl-35483344
ABSTRACT
The article presents a hepatocellular carcinoma cell surface-specific ligand glycyrrhetinic acid (GA) and cell-penetrating peptide (TAT) with good cell membrane penetration to modify the anti-tumor drug pingyangmycin (PYM) liver delivery system, which achieve targeted delivery of drugs and improve anti-tumor efficiency. In this study, we synthesized the pingyangmycin liposome modified by glycyrrhetinic acid and cell penetrating peptide(GA-TAT-PYM-L) and evaluated the anti-tumor effect of GA-TAT-PYM-Lin vitro. Using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenylte-trazolium bromidecell proliferation method, GA-TAT-PYM-L had a stronger inhibitory effect on HepG2 cells than the free drug PYM at the same concentration. Acridine orange-ethidium bromide staining assays showed that GA-TAT-PYM-L had stronger apoptosis promotion effects on HepG2 cells in comparison to PYM. Pharmacokinetic studies indicated that, compared with PYM, GA-TAT-PYM-L enhanced mean residence time (MRT0-∞) and area under curve (AUC0-∞) by about 2.79-fold and 2.45-fold. TheT1/2was prolonged to 140.23 ± 14.13 min. Tissue distribution results showed that the PYM concentrations in livers from the GA-TAT-PYM-L group were always higher than other tissues at each monitoring period after 5 min, indicating that GA-TAT-PYM-L can achieve liver targeting.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Ácido Glicirretínico / Liposomas Límite: Humans Idioma: En Revista: Biomed Mater Asunto de la revista: ENGENHARIA BIOMEDICA Año: 2022 Tipo del documento: Article

Texto completo: 1 Base de datos: MEDLINE Asunto principal: Ácido Glicirretínico / Liposomas Límite: Humans Idioma: En Revista: Biomed Mater Asunto de la revista: ENGENHARIA BIOMEDICA Año: 2022 Tipo del documento: Article