Target-based Pharmaceutical Formulation: Nanostructured lipid carriers for oral delivery of chrysin: Effect of surface modification on absorption

Chrysin (5, 7-dihydroxyflavone), a natural polyphenol, occurs in many passiflora flowers, along with honey, and propolis. It appears to have a blend of many pharmacological activities such as anticarcinogenic, pro-apoptotic, antiangiogenic, antimetastatic, immunomodulatory, and antioxidant properties. However, therapeutic use of this compound is limited owing to its poor solubility and subsequent low bioavailability. The current studies entail the development and evaluation of novel nanostructured lipidic carriers (NLCs) of 5, 7-dihydroxy flavone i.e., chrysin (CHN). The effect of ligand (biotin) modification on oral absorption of CHN encapsulated in NLCs is also explored. CHN-loaded NLCs (CHN–NLCs) were prepared employing apt lipid and surfactant. NLCs were prepared using melt dispersion-high pressure homogenization method. Biotin modification of CHN–NLCs was achieved by coupling reagents like, EDC and NHS in aqueous phase. The obtained biotin-decorated CHN–NLCs (BIO-CHN–NLCs) were 287.6 nm in size with an entrapment efficiency of 71.25 %. Oral bioavailability was enhanced up to 4.2-folds with the use of Bio-CHN–NLCs vis-a-vis pure CHN. However, there was a small difference in the enhancement of bioavailability between Bio-CHN–NLCs and conventional NLCs. Although severe lipolysis happened both on Bio-CHN–NLCs and non-modified NLCs, the performance of Bio-CHN–NLCs in the bioavailability improvement was more significant. Overall, Bio-CHN–NLCs can further promote the oral absorption of CHN by a ligand-mediated active transport. It may be a promising carrier for the oral delivery of molecules similar to CHN.

Author(s): Teenu Sharma

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