International Journal of Pharmaceutics 2013-03-25

Solid lipid nanoparticle preparation by a warm microemulsion based process: influence of microemulsion microstructure.

P Fadda, M Monduzzi, F Caboi, S Piras, P Lazzari

Index: Int. J. Pharm. 446(1-2) , 166-75, (2013)

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Abstract

Warm microemulsions (WME) containing lipids are used as starting systems to obtain solid lipid nanoparticles (SLN) in alternative processes to those based on high pressure homogenization technique. SLN characteristics can be influenced by the microemulsion composition and the specific conditions adopted in the quenching process related to the transformation of WME into nanoparticles. To establish optimized conditions for the production of SLN starting from WME, in a first step of this work we have defined the microstructure of warm microemulsions highlighted in the lecithin (LCT)/water (W)/tripalmitin (TP)/1-butanol (B)/taurocholate sodium salt (ST) phase behavior at 70°C. Moreover, we have further studied the LCT/W/TP/B system by evaluating the effect on the microemulsion area due to the LCT/B weight ratio, the replacement of 1-butanol with different alcohols (ROH), and the addition of taurocholate sodium salt (ST) at different LCT/ST weight ratios. The microstructure of the isotropic phase region obtained in the presence of ST has been characterized by both (1)H NMR PGSE measurements and electrical conductivity. The characteristics of final nanoparticles are discussed taking into account both the microstructure of the parent WME and the conditions of the quenching process leading to SLN. The present results highlight the relevance of the microstructural characteristic of WME to assure the obtainment of SLN with average diameter in the order of 100-2000 nm and narrow size distribution.Copyright © 2013 Elsevier B.V. All rights reserved.