Abstract

Oral delivery of nanoparticles containing Curcuma comosa Roxb. extract for inhibition of Acetylcholinesterase

Supakit Seerabsee

 Supathra Lamee

Damrongsak Jinarat

Wandee Rungseevijitprapa

Curcuma comosa Roxb., nanostructure lipid carrier, Alzheimer, Brain, AChE

Introduction: Alzheimer's disease is the most common cause of dementia among                             elderlies. Previous studies have shown that Curcuma comosa Roxb. extract has an anti-inflammatory activity and some beneficial effects on nervous system and brain on the ability to cross the Blood-Brain Barrier (BBB). The purpose of this research was to develop nanostructured lipid carriers (NLC) containing C. comosa Roxb. Extract for the increase in distribution of substance cross the BBB. Method: C. comosa Roxb. was extracted in n-hexane, ethyl acetate and ethanol. Antioxidation activities of the extracts were evaluated by DPPH assay. AChE inhibition activity was conducted by the measurement of 5-thio-2-nitrobenzene at 410 nm by using Donepezil as the control. NLC with C. comosa Roxb was prepared by hot homogenization technique. Mean particle sizes, size distribution and zeta potential were measured by laser light scattering. Stability of NLC loaded extracts were investigated at pH 1.2 and 6.8. In vitro release of the extract was performed in 0.5% SLS in PBS pH 6.8 by dialysis tubing at 37 ^oC. Result: IC₅₀ C. comosa Roxb extract in ethanol is 60 µg/mL. The ethanol, ethyl acetate and hexane of C. comosa exhibited % Inhibition of 26.40 ± 6.62, 45.80 ± 17.97 and 12.75 ± 4.36, respectively. The mean particle size of the developed NLC was in the range of 120 – 140 nm, zeta potential = -20 to -30 mV, PDI less than 0.4 with 98% DA2 encapsulation efficiency. Interestingly, NLC system has a trendency to protect C. comosa against acidic environment pH 6.8. Conclusion: The developed NLC containing C. comosa Roxb. extract could protect acid hydrolysis of active when administered orally. The formulation has a potential to inhibit AChE.