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Oridonin (Ori) is a natural compound with notable anti-inflammation and anti-cancer activities. However, therapeutic use of this compound is limited by its poor solubility and low bioavailability. Here a novel biotin-modified nanostructured lipid carrier (NLC) was developed to enhance the bioavailability of Ori. The effect of ligand (biotin) modification on oral absorption of Ori encapsulated in NLCs was also explored. Ori-loaded NLCs (Ori–NLCs) were prepared by the melt dispersion-high pressure homogenization method. Biotin modification of Ori–NLCs was achieved by EDC and NHS in aqueous phase. The obtained biotin-decorated Ori–NLCs (Bio-Ori–NLCs) were 144.9 nm in size with an entrapment efficiency of 49.54% and a drug load of 4.81%. Oral bioavailability was enhanced by use of Bio-Ori–NLCs with a relative bioavailability of 171.01%, while the value of non-modified Ori–NLCs was improved to 143.48%. Intestinal perfusion showed that Ori solution unexpectedly exhibited a moderate permeability, indicating that permeability was not a limiting factor of Ori absorption. Ori could be rapidly metabolized that was the main cause of low bioavailability. However, there was a difference in the enhancement of bioavailability between Bio-Ori–NLCs and conventional NLCs. Although severe lipolyses happened both on Bio-Ori–NLCs and non-modified NLCs, the performance of Bio-Ori–NLCs in the bioavailability improvement was more significant. Overall, Bio-Ori–NLCs can further promote the oral absorption of Ori by a ligand-mediated active transport. It may be a promising carrier for the oral delivery of Ori.