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  • Title: Doxorubicin-loaded liposomes: enhancing the oral bioavailability by modulation of physicochemical characteristics.
    Author: Daeihamed M, Haeri A, Ostad SN, Akhlaghi MF, Dadashzadeh S.
    Journal: Nanomedicine (Lond); 2017 May; 12(10):1187-1202. PubMed ID: 28447868.
    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.
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