Studies on lactoferrin nanoparticles of gambogic acid for oral delivery. (February 2013)

• Record Type: Journal Article
• Authors: Zhang, Zhen-Hai; Wang, Xiao-Pan; Ayman, Waddad Y.; Munyendo, Were L. L.; Lv, Hui-Xia; Zhou, Jian-Ping
• Is Part Of: Drug delivery. Volume 20:Number 2(2013:Feb.)
• Page Start: 86
• Page End: 93
• Publication Date: 2013-02
• Subjects: Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.3109/10717544.2013.766781
• Languages: English
• ISSNs: 1071-7544

Abstract

<abstract> <title>Abstract</title> <p> <italic>Purpose</italic>: Lactoferrin (Lf), a mammalian cationic iron-binding glycoprotein belonging to the transferrin (Tf) family, has been widely used in a variety of fields ranging from treating infant diarrhea and supporting newborn growth to food and pharmaceutical applications. In this study, Lf nanoparticles were firstly used as carriers of gambogic acid (GA) to enhance oral absorption and anti-cancer activity, hence reducing the related toxic effect.</p> <p> <italic>Methods</italic>: Gambogic acid-lactoferrin nanoparticles (GL-NPs) were prepared by the nanoparticle albumin-bound (NAB) technology. The formed nanoparticles were characterized by DSC, TEM, etc. <italic>In situ</italic> intestinal perfusion experiment was performed to clarify the absorption mechanism of GL-NPs. Furthermore <italic>in vivo</italic> and <italic>in vitro</italic> anti-tumor activities of GL-NPs were also investigated.</p> <p> <italic>Results</italic>: GL-NPs was successfully prepared with about 150 nm mean size, +20 mV ζ potential, 92.3 ± 7.2% encapsulation efficiency and 9.04 ± 0.7% DL; GL-NPs also exhibited a better stability and a desirable slow release <italic>in vitro</italic> experiment. The results of <italic>in situ</italic> intestinal perfusion showed a transformation of GA absorption from passive diffusion into active transport or facilitated diffusion by GL-NPs. MTT assay of GL-NPs showed almost an equal anti-proliferative effect with arginine solution of GA (Arg-GA) in HepG2 cell. The inhibitory rate against S180 tumor mice after oral administration of GL-NPs was up to 86.01% which was1.39-folds of intravenous injection of Arg-GA.</p> <p> <italic>Conclusion</italic>: The <italic>in vitro</italic> results showed that the NAB technology was feasible for industrial production of Lf nanoparticles and the <italic>in vivo</italic> results proved that the effective GL-NPs is a promising approach for the oral delivery of GA. These obtained research works have also paved the preliminary way for the study of Lf as an oral drug delivery carrier.</p> </abstract>