HomeIngredientDevelopment of Poly(lipoic acid) Nanoparticles with Improved Oral Bioavailability and Hepatoprotective Effects of Quercetin

Development of Poly(lipoic acid) Nanoparticles with Improved Oral Bioavailability and Hepatoprotective Effects of Quercetin

March 31, 2022

Mol Pharm. 2022 Mar 30. doi: 10.1021/acs.molpharmaceut.2c00009. Online ahead of print.

ABSTRACT

Quercetin (QUE)-loaded poly(lipoic acid) nanoparticles (QUE/pLA) were developed to improve chemical stability in the gastrointestinal (GI) tract, oral bioavailability (BA), and pharmacological properties of QUE. QUE/pLA was prepared by emulsion solvent evaporation with ultrasonication followed by freeze-drying. Its mean particle size was 185 nm, with a high encapsulation efficiency of QUE (84.8%). QUE/pLA exhibited sustained release of QUE with improved dissolution compared with crystalline QUE and significantly enhanced chemical stability under physiological pH in the GI tract. Orally dosed QUE/pLA (50 mg QUE/kg) in rats exhibited significantly prolonged systemic exposure, possibly due to the sustained release of QUE. The oral BAs of QUE in QUE/pLA and crystalline QUE groups were 29 and 0.19%, respectively, suggesting significant enhancement of oral absorbability, likely due to the improved stability and dissolution property of QUE in the GI tracts. In hepatic injury model rats, QUE/pLA (50 mg QUE/kg) led to marked reductions in the plasma biomarker levels of alanine aminotransferase and aspartate aminotransferase by 70 and 46%, respectively, compared with the vehicle group. QUE/pLA also showed improved antioxidant potential as evidenced by the enhanced activities of hepatic glutathione, superoxide dismutase, and a decrease in the level of malondialdehyde, a marker of lipid peroxidation. Based on these findings, QUE/pLA might be a promising option to improve both the nutraceutical and pharmaceutical properties of QUE.

PMID:35353535 | DOI:10.1021/acs.molpharmaceut.2c00009

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Patrick Blanchard MD

Meet Dr. Blanchard Dr. Blanchard’s medical practice is an embodiment of Integrative health which brings conventional and complementary approaches together in a coordinated way. Conveniently located in sunny Florida and over the internet with ValiseMD’s secure HIPPA compliant telXmed servers. Since 1994, patients with a wide range of challenging medical problems have achieved optimum health using the best of natural medicine, judiciously combined with high-tech innovations. Breakthroughs are often achieved even after patients have consulted mainstream specialists and holistic practitioners. Dr. Blanchard is founder and CEO of ValiseMD, Inc. He is board certified in Family Medicine since 1994 and awarded Fellow of the American Academy of Family Physicians in 2001. He received the ‘Teacher of the Year’ award from the University of Kansas School of Medicine at completion of his residency in Family Medicine. He completed a fellowship at Wake Forest University in the field of vascular neurosonology. He holds a medical patent in the field of Gastroenterology. He holds an unrestricted license to practice medicine and surgery in Florida. He started his medical career as a Emergency Medical Technician, then as a Paramedic and later a Medical Doctor.