Nanostructured lipid carriers for oral delivery of baicalin: In vitro and in vivo evaluation

• Emulsion–evaporation and low temperature-solidification method was used to prepare baicalin nanostructured lipid carriers.
• Uniform design was utilized for formulation optimization.
• Enhanced drug loading and sustained release were realized by nanostructured lipid carriers.
• The oral bioavailability of baicalin was improved remarkably by nanostructured lipid carriers.

The present study aimed to develop a novel baicalin-loaded nanostructured lipid carrier (BA-NLC) system for oral delivery to enhance the bioavailability. BA-NLC were prepared by emulsion–evaporation and low temperature-solidification technique and optimized by a five-factor four-level uniform design. The characteristics of BA-NLC including morphology, particle size, zeta potential, entrapment efficiency and drug loading were investigated. The results showed that the optimized BA-NLC was nearly spherical in shape with a mean diameter of 244.7 nm. The entrapment efficiency and drug loading were 59.51 ± 0.57% and 3.54 ± 0.11%, respectively. In vitro drug release revealed a pattern with burst release initially and sustained release afterwards for BA-NLC. Moreover, BA-NLC exhibited prolonged MRT and increased AUC compared to pure BA. All the detailed evidence indicated that BA-NLC could be a potential delivery system for the oral administration of BA.

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