Exploring the protective effect exhibited by curcumin-loaded coconut oil microemulsion in the experimental models of neurodegeneration: an insight of formulation development, in vitro and in vivo study

Abstract

Background Neurodegenerative diseases are a major health concern which requires promising drugs with appropriate drug delivery systems. The aim of the present study was development and characterization of curcumin-loaded coconut oil microemulsion (Cur-ME) and to improve the pharmacokinetic and pharmacodynamics performance. Initially, solubility study and emulsification study were performed for preliminary screening of the components. Pseudoternary phase diagram was constructed using selected components, and composition of Cur-ME was finalized. Furthermore, in vitro drug release in vivo pharmacokinetics and pharmacodynamic was performed. Results The final formulation exhibited globule size less than 20 nm with PDI and zeta potential as 0.24 and −17 mV, respectively. The formulation showed more than 90% drug content with no signs of precipitation upon dilution and centrifugation. In vitro drug release revealed 2.12-fold improvement in dissolution. In vivo plasma pharmacokinetics of Cur-ME revealed twofolds and 2.48-fold improvement in AUC and Cmax, respectively, than that of Cur-Sol. In vivo pharmacokinetics in adult zebrafish revealed significant enhancement (p < 0.01) in curcumin delivery to the brain with 1.96-fold and 1.92-fold improvement in Cmax and AUC, respectively. Furthermore, the pharmacodynamics of the formulation was evaluated using trimethyl tin (TMT)-induced neurodegeneration in wistar rats. The results revealed that Cur-ME treated group significantly decreased the escape latency and pathlength as compared to the neurodegeneration control group. The observed effects were also markedly significant than Cur-Sol treated group. Further, the brain malondialdehyde (MDA) and glutathione (GSH) levels were found to be increased significantly as compared to Cur-Sol treated group. Conclusion The encouraging results exhibited by Cur-ME can be regarded as a mark of an effective formulation that can be used in neurodegeneration. Overall, these findings indicate that an orally delivered microemulsion has enormous potential for drug delivery to the brain.

Reactive Extrusion of Poly(lactic acid)-graft-Curcumin Antioxidant and Intelligent Packaging

“…The lack of curcumin migration in aqueous matrices (H 2 O, 10% EtOH, and 3% acetic acid) may be expected due to curcumin’s low water solubility. However, in coconut oil, curcumin has a reported solubility of up to 17.75 ± 2.40 mg/mL, which would equate to a maximum of 88.75 mg/cm 2 in this study. Considering <0.000625 mg/cm 2 curcumin migration was observed in coconut oil, low migration results could not be attributed to solubility limits.…”