Formulation design, preparation, and in vitro and in vivo characterizations of β-Elemene- loaded nanostructured lipid carriers

Abstract

Feng Shi,1 Gang Yang,1 Juan Ren,2 Teng Guo,1 Yan Du,1 Nianping Feng1 1Department of Pharmaceutics, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China; 2Department of Traditional Chinese Medicine, Changhai Hospital, Shanghai, People's Republic of China Abstract: In the present study, nanostructured lipid carriers (NLCs) were prepared and optimized for the intravenous delivery of β-Elemene (β-E). Aqueous dispersions of NLCs were successfully prepared by high-pressure homogenization method using glycerol monostearate as the solid lipid and a mixture of Maisine 35-1 and Labrafil M1944 CS as the liquid lipid. The results revealed that the morphology of the NLCs was spheroidal. The particle size, zeta potential, and entrapment efficiency (EE) for the optimized formulation were observed as 138.9 nm, –20.2 mV, and 82.11%, respectively. X-ray diffraction analysis revealed the formation of less ordered structures in the inner core of the NLC particles. Moreover, the β-E-loaded NLCs were also less irritating and less toxic compared to Elemene injection. In addition, β-E-NLCs showed a significantly higher bioavailability and anti-tumor efficacy than Elemene injection. Taken together, our data indicate that the β-E-NLCs described in this study are well-suited for the intravenous delivery of β-E. Keywords: nanostructured lipid carriers, high-pressure homogenization, β-Elemene, venous irritation, anti-tumor efficacy