Chinedu C. Ochin and Mahdi Garelnabi* Pages 61 - 70 ( 10 )
Background: The developments of new parenteral approaches to target PCSK-9 for the treatment of LDL-Cholesterol has yielded impressive results; and have shown significant decreases in the risk of mortality associated with hypercholesterolemia. However improved and convenient alternate approaches that exploit the beneficial drug target properties of PCSK-9 also need to be explored and developed. One such approach is the oral administration of Berberine using nanotechnology.
Methods: Nanoprecipitation encapsulation and physiochemical characterization of Berberine Chloride in PLGA-PEG-PLGA block copolymer has been developed and characterized in Hep-G2 cells using Berberine Chloride encapsulated nanoparticle (Bc-NP). Evaluation of PCSK-9, SREBP- 1, LDL-r, HNF-1alpha mRNAs and PCSK-9 protein expression was performed using quantitative real-time PCR (qPCR) and median fluorescence intensity (MFI) of flow cytometric studies respectively. Pearson’s correlation analysis of PCSK-9 mRNA and protein levels in Berberine chloride delivery was performed.
Results: The PCSK-9 mRNA and protein expression shows a relationship to the release of Berberine from the encapsulating PLGA-PEG-PLGA polymer in a time dependent manner.
Conclusion: PCSK-9 modulation by oral administration of Berberine using nanotechnology approach can improve its pharmacokinetic profile. Further studies are needed to maximize its delivery efficiency.
PCSK9, lipoproteins, lipids, atherosclerosis, drug delivery, nanotechnology.
Biomedical Engineering and Biotechnology Program, Department of Biomedical and Nutritional Sciences, College of Health Sciences, University of Massachusetts, Lowell, MA, Biomedical Engineering and Biotechnology Program, Department of Biomedical and Nutritional Sciences, College of Health Sciences, University of Massachusetts, Lowell, MA