Abstract
Objective: In the present study, Curcumin (CU)-loaded nanocarrier (NC) such as nanoemulsion (NE) was developed with the objective of increasing its cytotoxicity and bioavailability through lymphatic transport by enhancing its solubility and intestinal permeability.
Materials and methods: Based on the area obtained in pseudoternary phase diagram, various % combination of Labrafac Lipophile WL 1349, Solutol HS 15, Transcutol HP and distilled water were selected. Formulations which passed physical stability studies were selected for further studies such as globule size, zeta potential, in vitro release, ex vivo permeation, in vitro lipolysis studies, bioavailability studies and cytotoxicity against glioblastoma cells (U-87).
Result and discussion: The optimized NC (NE-SB1) had small average globule diameter of 67 ± 6 nm with zeta potential of −37 ± 2.5 mv which indicated long-term dispersion stability. During in vitro lipolysis study, the digestion rate of medium chain triglycerides increased with decreased globule diameter. Statistically significant difference was found in AUC0−inf of NC formulation (p < 0.05) compared to CU suspension. The relative bioavailability of NC was found 11.88 ± 0.47 with respect to CU suspension. During cytotoxicity studies, IC50 of CU solution on U87 cells was found 24.23 µM, while for the NE- SB1 it was 16.41 µM. The optimized formulation was found to be stable during 6 months of accelerated stability.
Conclusion: The overall results revealed that the CU-loaded NC is a very effective approach for enhancing the oral absorption of poorly water-soluble drug CU and have great potential for future clinical application.
Acknowledgements
The authors are thankful to University Grant Commission (UGC), Government of India for providing financial assistance to this project. The authors are also grateful to AIIMS, Delhi, India for providing facility to conduct TEM analysis of NE formulations. The authors are also thankful to Gattefose, India for providing oil, surfactant and co-surfactant as a gift sample.
Declaration of interest
The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.