Research: LI and COLLEAGUES,

Listed in Issue 274

Abstract

LI and COLLEAGUES, 1. The Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Rensselaer, NY 12144, USA; 2. The Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Rensselaer, NY 12144, USA; Department of Physiology, Veterinary Medicine Faculty, Uludag University, Bursa, Turkey; 3. Center for Functional Genomics, University at Albany, Rensselaer, NY, USA; 4. Center of Excellence for Osteoporosis Research, Department of Clinical Biochemistry, Faculty of Medicine and King Abdulaziz University Hospital, King Abdulaziz University, Jeddah, Saudi Arabia; 5. The Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Rensselaer, NY 12144, USA. shaker.mousa@acphs.edu studied self-assembly of green tea catechin derivatives in nanoparticles for oral lycopene delivery

Background

Lycopene is a natural anti-oxidant that has attracted much attention due to its varied applications such as protection against loss of bone mass, chronic diseases, skin cancer, prostate cancer, and cardiovascular disease.

Methodology

However, high instability and extremely low oral bioavailability limit its further clinical development. We selected a green tea catechin derivative, oligomerized (-)-epigallocatechin-3-O-gallate (OEGCG) as a carrier for oral lycopene delivery. Lycopene-loaded OEGCG nanoparticles (NPs) were prepared by a nano-precipitation method, followed by coating with chitosan to form a shell. This method not only can easily control the size of the NP to be around 200nm to improve its bioavailability, but also can effectively protect the lycopene against degradation due to EGCG's anti-oxidant property. OEGCG was carefully characterized with nuclear magnetic resonance spectroscopy and mass spectrometry. Lycopene-loaded polylactic-co-glycolic acid (PLGA) NPs were prepared by the same method.

Results

Chitosan-coated OEGCG/lycopene NPs had a diameter of 152±32nm and a ζ-potential of 58.3±4.2mv as characterized with transmission electron microscopy and dynamic light scattering. The loading capacity of lycopene was 9% and encapsulation efficiency was 89%. FT-IR spectral analysis revealed electrostatic interaction between OEGCG and chitosan. Freeze drying of the NPs was also evaluated as a means to improve shelf life. Dynamic light scattering data showed that no aggregation occurred, and the size of the NP increased 1.2 times (Sf/Si ratio) in the presence of 10% sucrose after freeze drying. The in vitro release study showed slow release of lycopene in simulated gastric fluid at acidic pH and faster release in simulated intestinal fluid. In an in vivo study in mice, lycopene pharmacokinetic parameters were improved by lycopene/OEGCG/chitosan NPs, but not improved by lycopene/PLGA/chitosan NPs.

Conclusion

The self-assembled nanostructure of OEGCG combined with lycopene may be a promising application in oral drug delivery in various indications.

References

Li W1, Yalcin M2, Lin Q3, Ardawi MM4, Mousa SA5. Self-assembly of green tea catechin derivatives in nanoparticles for oral lycopene delivery. J Control Release. 248:117-124. doi: 10.1016/j.jconrel.2017.01.009. 28 Feb  2017. Epub 8 Jan  2017.

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