Pharmaceutical Research 2015-05-01

Rifampicin loaded mannosylated cationic nanostructured lipid carriers for alveolar macrophage-specific delivery.

Xu Song, Qing Lin, Ling Guo, Yao Fu, Jianfeng Han, Huan Ke, Xun Sun, Tao Gong, Zhirong Zhang

Index: Pharm. Res. 32(5) , 1741-51, (2015)

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Abstract

In this study, cationic mannosylated nanostructured lipid carriers (Man-NLCs) were developed for the targeted delivery of rifampicin to alveolar macrophages.Rifampicin loaded Man-NLCs (RFP-Man-NLCs) and rifampicin loaded unmodified nanostructured lipid carriers (REP-NLCs) were prepared using thin film homogenization method and characterized by particle size, polydispersity index, zeta potential, transmission electron microscopy, encapsulation efficiency, pharmacokinetics, biodistribution, cell specific targeting, cytotoxicity and inflammatory response.RFP-Man-NLCs and REP-NLCs obtained displayed a size distribution around 160 nm (PDI <0.30) with positive charges of approximately 30 mV. The encapsulation efficiency of RFP was above 90%. In the biodistribution study, both RFP-Man-NLCs and RFP-NLCs, compared with the commercially available rifampicin solution, displayed superior lung-targeting ability. Compared to REP-NLCs, RFP-Man-NLCs exhibited significantly higher uptake efficiency in NR8383 cells and alveolar macrophages, which achieved cell-specific targeting. In addition, RFP-Man-NLCs were demonstrated to be a safe formulation with minimum toxicity and no inflammatory response.RFP-Man-NLCs provided an alternative strategy for selectively delivering rifampicin to alveolar macrophages.