Development of lipid-based nanocarriers for increasing gastro-intestinal absorption of lupinifolin extracted from Albizia myriophylla Benth.

Lupinifolin (L), a plant flavonoid, has been reported to possess various pharmacological effects [1]–[3]. It is most likely to exert low oral bioavailability because of poor water solubility [4]. The objective of this study was to develop lipid nanocarriers as drug delivery systems to increase gastro-intestinal absorption of lupinifolin extracted from Albizia myriophylla Benth. Three types of nanocarriers, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nanoemulsions (NE) were prepared by emulsification-sonification technique. All three types of nanocarriers loaded with lupinifolin, LSLN, LNLC, and LNE, were successfully synthesized. The lipid components chosen to formulate nanacarriers were Dynasan®116 and/or medium chain triglyceride. Physicochemical characterizations along with releasing profiles of lupinifolin-loaded lipid nanocarriers were compared. It was found that the best lipid nanocarriers for lupinifolin was LNLC, which demonstrated the particle size of 151.5 ± 0.1 nm, monodispersity distribution with PdI of 0.24, negative surface charge at − 41.2 ± 0.7 mV, high encapsulation (99.3%), and high loading capacity (5.0%). The obtained LNLC exhibited prolonged release in simulated circulatory system, but produced low release in gastro-intestinal condition (3.7%). Intestinal permeability of the nanocarriers was further evaluated in everted intestinal sacs method. The results from the ex vivo study indicated that LNLC significantly increased the absorption, compared to native lupinifolin. Lupinifolin absorption through LNLC was about 16 times higher than the native form. In conclusion, lupinifolin-loaded lipid nanocarriers were successfully formulated as delivery systems to enhance its oral bioavailability. Further in vivo experiments are needed to validate the results from this study.

• References

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