Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake

Xiuying Li, Dan Chen, Chaoyi Le, Chunliu Zhu, Yong Gan, Lars Hovgaard, Mingshi Yang

    104 Citations (Scopus)

    Abstract

    The aim of this study was to investigate the intestinal mucus-penetrating properties and intestinal cellular uptake of two types of liposomes modified by Pluronic F127 (PF127). The two types of liposomes, ie, PF127-inlaid liposomes and PF127-adsorbed liposomes, were prepared by a thin-film hydration method followed by extrusion, in which coumarin 6 was loaded as a fluorescence marker. A modified Franz diffusion cell mounted with the intestinal mucus of rats was used to study the diffusion characteristics of the two types of PF127 liposomes. Cell uptake studies were conducted in Caco-2 cells and analyzed using confocal laser scanning microcopy as well as flow cytometry. The diffusion efficiency of the two types of PF127-modified liposomes through intestinal rat mucus was 5-7-fold higher than that of unmodified liposomes. Compared with unmodified liposomes, PF127-inlaid liposomes showed significantly higher cellular uptake of courmarin 6. PF127-adsorbed liposomes showed a lower cellular uptake. Moreover, and interestingly, the two types of PF127-modified liposomes showed different cellular uptake mechanisms in Caco-2 cells. PF127-inlaid liposomes with improved intestinal mucus-penetrating ability and enhanced cellular uptake might be a potential carrier candidate for oral drug delivery.

    Original languageEnglish
    JournalInternational Journal of Nanomedicine (Online)
    Volume6
    Pages (from-to)3151-62
    Number of pages12
    ISSN1176-9114
    DOIs
    Publication statusPublished - 2011

    Keywords

    • Administration, Oral
    • Animals
    • Caco-2 Cells
    • Cell Membrane
    • Drug Delivery Systems
    • Humans
    • Intestinal Mucosa
    • Liposomes
    • Male
    • Mucus
    • Nanoparticles
    • Permeability
    • Poloxamer
    • Rats
    • Rats, Wistar

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