Qi Zhou1, Kezhu Hou1, Zhiqiang Fu1. 1. Department of Thoracic Surgery, Shanghai Shidong Hospital, Shanghai, 200438, People's Republic of China.
Abstract
Introduction: Mangiferin is a plant antitumor compound with poor water solubility and low bioavailability. In this study, transferrin-modified mangiferin-loaded solid lipid nanoparticles (Tf-modified MGF-SLNs) were prepared to overcome the above defects. Methods: Tf-modified MGF-SLNs were prepared by the emulsification-solvent evaporation method. The physicochemical properties of Tf-MGF-SLNs such as particle size, zeta potential and in vitro drug release were investigated. We also demonstrated the effect of Tf-MGF-SLNs in lung cancer. Results: The mean hydrodynamic diameter of the Tf-MGF-SLNs was 121.8±2.9 nm with a polydispersity index of 0.134±0.03. According to TEM micrographs, Tf-MGF-SLNs are spherical and uniform, and the EE% was found to be 72.5±2.4%. In vitro release, we identified an initial burst effect release, followed by controlled release, in SLNs at both pHs and the Tf-MGF-SLNs drug accumulation release percentages reached over 68% at pH 4.0 and 72% at pH 7.4 in 6 hours, respectively. In vivo studies showed that depending on surface modification, Tf-MGF-SLNs, which suggested that cell internalization was changed and more drugs entered the cells successfully. Discussion: Tf-MGF-SLNs were highly efficient in suppressing the tumor growth in xenograft tumor model. Sustained release of the drug delivery system and Tf-modified MGF-SLNs played a major role. Tf-MGF-SLNs would be a promising formulation for the treatment of lung cancer.
Introduction: Mangiferin is a plant antitumor compound with poor water solubility and low bioavailability. In this study, transferrin-modified mangiferin-loaded solid lipid nanoparticles (Tf-modified MGF-SLNs) were prepared to overcome the above defects. Methods: Tf-modified MGF-SLNs were prepared by the emulsification-solvent evaporation method. The physicochemical properties of Tf-MGF-SLNs such as particle size, zeta potential and in vitro drug release were investigated. We also demonstrated the effect of Tf-MGF-SLNs in lung cancer. Results: The mean hydrodynamic diameter of the Tf-MGF-SLNs was 121.8±2.9 nm with a polydispersity index of 0.134±0.03. According to TEM micrographs, Tf-MGF-SLNs are spherical and uniform, and the EE% was found to be 72.5±2.4%. In vitro release, we identified an initial burst effect release, followed by controlled release, in SLNs at both pHs and the Tf-MGF-SLNs drug accumulation release percentages reached over 68% at pH 4.0 and 72% at pH 7.4 in 6 hours, respectively. In vivo studies showed that depending on surface modification, Tf-MGF-SLNs, which suggested that cell internalization was changed and more drugs entered the cells successfully. Discussion: Tf-MGF-SLNs were highly efficient in suppressing the tumor growth in xenograft tumor model. Sustained release of the drug delivery system and Tf-modified MGF-SLNs played a major role. Tf-MGF-SLNs would be a promising formulation for the treatment of lung cancer.
Authors: Rajneet Kaur Khurana; Arvind K Bansal; Sarwar Beg; Andrea Julie Burrow; O P Katare; Kamalinder K Singh; Bhupinder Singh Journal: Int J Pharm Date: 2016-12-23 Impact factor: 5.875
Authors: Tracy R Daniels; Ezequiel Bernabeu; José A Rodríguez; Shabnum Patel; Maggie Kozman; Diego A Chiappetta; Eggehard Holler; Julia Y Ljubimova; Gustavo Helguera; Manuel L Penichet Journal: Biochim Biophys Acta Date: 2011-08-05