title: Promises of a biocompatible nanocarrier in improved brain delivery of quercetin: Biochemical, pharmacokinetic and biodistribution evidences.
abstract: In various neurological disorders, antioxidants are frequently prescribed along with the specific treatment modalities. One such promising natural flavonoid is quercetin, offering better outcomes than established vitamins E and C. Though with immense promises, various challenges like poor oral-bioavailability (<2%), extensive first-pass metabolism, poor brain permeability, hydrophobic nature and physiological pH instability hinder its proper usage. Hence, it was planned to prepare quercetin-loaded nano lipidic carriers (NLCs) employing biocompatible components like phospholipids and tocopherol acetate for enhanced brain delivery. The outcomes were also compared with solid lipid nanoparticles (SLNs) of comparable composition. Both the nanocolloids offered better drug loading and controlled drug release with appreciable stability. In vitro antioxidant performance was improved after encapsulation in nanoparticles and the nanoparticles were substantially uptaken by Caco-2 cells. The difference in outcomes was vivid in pharmacokinetic studies, where nanoparticles, esp. NLCs substantially enhanced the relative bioavailability (approx. 6 folds), biological residence (2.5 times) and appreciably retarded the drug clearance (approx. 6 folds). On the other hand, both nanoparticles were able to substantially deliver the drug to brain. NLCs were observed to enhance the brain permeability of drug in a noticeable manner. In Conclusion, SLNs/NLCs can offer a better-platform for brain-delivery of quercetin.
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt. Ajmer, Rajasthan, 305817, India.
authors.forename: Pramod
authors.initials: P
authors.lastname: Kumar
authors.affiliation: Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh,160014, India.
authors.forename: Gajanand
authors.initials: G
authors.lastname: Sharma
authors.affiliation: UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites, Panjab University, Chandigarh, 160014, India.
authors.forename: Rajendra
authors.initials: R
authors.lastname: Kumar
authors.affiliation: Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh,160014, India; UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites, Panjab University, Chandigarh, 160014, India.
authors.forename: Bhupinder
authors.initials: B
authors.lastname: Singh
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt. Ajmer, Rajasthan, 305817, India.
authors.forename: Ruchi
authors.initials: R
authors.lastname: Malik
authors.affiliation: Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh,160014, India.
authors.forename: Om Prakash
authors.initials: OP
authors.lastname: Katare
authors.affiliation: Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt. Ajmer, Rajasthan, 305817, India. Electronic address: drkaisar@curaj.ac.in.
authors.forename: Kaisar
authors.initials: K
authors.lastname: Raza
mesh_terms: D001672:Biocompatible Materials / Q000737:chemistry*; D001682:Biological Availability; D001921:Brain / Q000378:metabolism*; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry; D011794:Quercetin / Q000737:chemistry* / Q000493:pharmacokinetics*; D014018:Tissue Distribution / Q000187:drug effects
chemical_list: D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008055:Lipids; D011794:Quercetin
keywords: Bioavailability; NLCs; Nanoparticles; Neurological disorders; Neuroprotection; SLNs