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



Daeihamed M¹ ; Haeri A¹ ; Ostad SN² ; Akhlaghi MF³ ; Dadashzadeh S^{1, 4}
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.