Solid lipid nanoparticles (SLN) loaded with highly hydrophilic drug, rosiglitazone maleate were prepared by cold homogenization technique. Glyceryl monostearate was used as lipid core and lecithin E-80 as the shell material. Both lipid and drug were dissolved using dimethyl sulfoxide (DMSO). Oleic acid was also employed as surfactant. The physiochemical properties of SLNs with various lipid composition, drug content and altered homogenizing time were optimized to obtain high quality nanoparticles. The enhancement of lecithin content in lipid matrix resulted in smaller particle of SLNs. The mean particle size measured by photon correlation spectroscopy (PCS) was ranged from 140.2-467.6 nm. The drug entrapment efficiency (EE) and drug loading capacity (DL) were determined using fluorescence spectroscopy, were reach up to 81.2 ± 2.5% and 7.1±0.23% respectively. The drug release behavior was studied by using dialysis bag method. The study of drug release showed that the drug release could last up to 48 h, and the rate was delayed by the addition of lecithin and/or oleic acid in the formulations. The physical stability experiment showed that the SLNs were stable for 2 months under room temperature. Moreover, the cellular cytotoxicity of rosiglitazone maleate against cell could be improved by the entrapment of SLNs. In conclusion, SLN with small particle size, high EE and relatively high DL capacity for rosiglitazone maleate can be obtained by this method.
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