Formulation, characterization, and in vitro/vivo studies of aclacinomycin A-loaded solid lipid nanoparticles

Objective: The aim of this study was to prepare aclacinomycin A (ACM)-loaded solid lipid nanoparticles (SLNs) and to evaluate their in vitro and in vivo characteristics. Methods: SLNs were prepared using an emulsion evaporation-solidification method, and characterized in accordance with the morphological examination, particle size distribution, entrapment efficiency, drug-loading, and in vitro release. Pharmacokinetic and biodistribution studies were employed to evaluate the in vivo of SLNs. Results: The SLNs were spherical in shape, uniform in size, and appropriate for administration via intravenous injection. The drug content, encapsulation efficiency, and drug loading of prepared SLNs were 96.4%+/- 4.6%, 86.7%+/- 2.3%, and 4.8%+/- 0.7% (n = 3), respectively, and the mean diameter was 68.2 +/- 5.6 nm from three batches. The SLNs were produced with stable physical properties and demonstrated significantly sustained release. The pharmacokinetic behavior of ACM was greatly improved by lyophilized injection of SLN with sustained drug release and high bioavailability. In addition, the results obtained from tissue distribution showed that ACM-SLNs were hepatic targeting in vivo. Conclusions: The present work demonstrated the feasibility of liver-targeted delivery of ACM utilizing SLNs.