Preparation, Characterization, Pharmacokinetics and Tissue Distribution of Solid Lipid Nanoparticles Loaded with Tetrandrine
- 3 August 2011
- journal article
- Published by Springer Science and Business Media LLC in AAPS PharmSciTech
- Vol. 12 (3), 1011-1018
- https://doi.org/10.1208/s12249-011-9665-3
Abstract
Tetrandrine (TET) is a poorly water-soluble bisbenzylisoquinoline alkaloid. In this study, TET solid lipid nanoparticles (SLNs) were prepared by a melt–emulsification and ultrasonication technique. Precirol® ATO 5, glyceryl monostearate, and stearic acid were used as the lipid matrix for the SLNs, while Lipoid E80, Pluronic F68, and sodium deoxycholate were used as emulsifying and stabilizing agents. The physicochemical characteristics of the TET–SLNs were investigated when it was found that the mean particle size and zeta potential of the TET–SLNs were 134 ± 1.3 nm and −53.8 ± 1.7 mV, respectively, and the entrapment efficiency (EE) was 89.57% ± 0.39%. Differential scanning calorimetry indicated that TET was in an amorphous state in SLNs. TET–SLNs exhibited a higher release rate at a lower pH and a lower release rate at a higher pH. The release pattern of the TET–SLNs followed the Weibull model. The pharmacokinetics of TET–SLNs after intravenous administration to male rats was studied. TET–SLN resulted in a higher plasma concentration and lower clearance. The biodistribution study indicated that TET–SLN showed a high uptake in reticuloendothelial system organs. In conclusion, TET–SLNs with a small particle size, and high EE, can be produced by the method described in this study. The SLN system is a promising approach for the intravenous delivery of tetrandrine.Keywords
This publication has 38 references indexed in Scilit:
- Preparation and Enhanced Oral Bioavailability of Cryptotanshinone-Loaded Solid Lipid NanoparticlesAAPS PharmSciTech, 2010
- Effect of Formulation Components on the In Vitro Permeation of Microemulsion Drug Delivery System of FluconazoleAAPS PharmSciTech, 2009
- Preparation and Evaluation of Miconazole Nitrate-Loaded Solid Lipid Nanoparticles for Topical DeliveryAAPS PharmSciTech, 2009
- Anticancer effect of tetrandrine on primary cancer cells isolated from ascites and pleural fluidsCancer Letters, 2008
- Investigations on the structure of solid lipid nanoparticles (SLN) and oil-loaded solid lipid nanoparticles by photon correlation spectroscopy, field-flow fractionation and transmission electron microscopyJournal of Controlled Release, 2004
- Enzymatic degradation of SLN—effect of surfactant and surfactant mixturesInternational Journal of Pharmaceutics, 1999
- Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN™) dispersionsInternational Journal of Pharmaceutics, 1998
- Sterilization and freeze-drying of drug-free and drug-loaded solid lipid nanoparticlesInternational Journal of Pharmaceutics, 1997
- In Vitro Stability of Poly(D,L-lactide) and Poly(D,L-lactide)/Poloxamer Nanoparticles in Gastrointestinal FluidsDrug Development and Industrial Pharmacy, 1997
- Tetrandrine: A new ligand to block voltage-dependent Ca2+ and Ca2+-activated K+ channelsLife Sciences, 1994