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Doxorubicin-Loaded Liposomes: Enhancing the Oral Bioavailability by Modulation of Physicochemical Characteristics Publisher Pubmed



Daeihamed M1 ; Haeri A1 ; Ostad SN2 ; Akhlaghi MF3 ; Dadashzadeh S1, 4
Authors
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Authors Affiliations
  1. 1. Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  2. 2. Department of Toxicology and Pharmacology, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Medicinal Chemistry, School of Pharmacy, Guilan University of Medical Sciences, Rasht, Iran
  4. 4. Pharmaceutical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran

Source: Nanomedicine Published:2017


Abstract

Aim: In this study, the effects of liposome characteristics on oral absorption of doxorubicin, as a hydrophilic low-permeability drug, were investigated. Materials & methods: Different doxorubicin-loaded liposomes were prepared, characterized and orally administered to 18 groups of rats. Plasma concentrations of doxorubicin and its aglycone metabolite were measured, and Caco-2 uptake and transport of optimum liposomes were investigated. Results: After studying different factors, a fourfold increase in oral bioavailability was achieved with the non-PEGylated, 120-nm-sized positively charged rigid liposomes (lipid to drug ratio = 10). The extent of drug's first-pass metabolism as well as endocytosis of nanoparticles were markedly affected by liposomal formulation. Conclusion: Oral absorption is highly dependent on liposomal properties, and optimum formulations are effective for low-permeability drugs. © 2017 Future Medicine Ltd.