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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