4.4 Article

Using PG-Liposome- Based System to Enhance Puerarin Liver-Targeted Therapy for Alcohol-Induced Liver Disease

Journal

AAPS PHARMSCITECH
Volume 17, Issue 6, Pages 1376-1382

Publisher

SPRINGER
DOI: 10.1208/s12249-015-0427-5

Keywords

alcohol-induced liver disease; distribution; pharmacokinetics; propylene glycol liposome; puerarin

Funding

  1. National Natural Science Foundation of China [81360195, 81301982, 81571392, 81272160, 81302726, 81460299]
  2. Zhejiang Provincial Foundation for Health Department [2015ZDA023]
  3. Medicine Grant from Wenzhou Bureau of Science and Technology [Y2014730]
  4. Major Scientific Project of Guangdong Province [2012A080201010]
  5. Science and Technology Program of Guangzhou, China [201508020001]

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A critical issue for alcohol-induced liver disease (ALD) therapeutics is the lack of a highly efficient delivery system. In this study, a Puerarin-propylene glycol-liposome system was prepared for the purpose of targeting puerarin, an isoflavon, to the liver. Transmission electron microscope (TEM) results showed the liposomes to be spherical in shape with an average diameter of 182 nm with a polydispersity index of 0.239. The zeta potential of the particles was about -30 mV. The entrapment efficiency of puerarin was above 90%. MTT-based assay in HpeG2 cells showed no significant cytotoxicity in the presence of up to 25% concentration of the system containing 3% puerarin. In vivo performance of this system was studied in mice. Pharmacokinetics and distribution of puerarin-PG-liposome system was studied relative to puerarin solution at the same dose levels. The results show that puerarin-PG-liposome prolonged drug retention time and decreased elimination of puerarin in mice (AUC of liposome system and solution was 9.5 and 4.0 mg h L-1, respectively). Furthermore, propylene glycol (PG)-liposome system enhanced puerarin distribution into liver and spleen, while decreasing puerarin distribution in other tissues. Overall, the puerarin-PG-liposome system showed enhanced therapeutic effect in mice with ALD.

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