title: Formulation optimization and topical delivery of quercetin from solid lipid based nanosystems.
abstract: The presence of large amounts of reactive oxygen species (ROS) leads to oxidative stress that can damage cell membranes, lead to DNA breakage and cause inactivation of free radical scavenger enzymes, eventually resulting in skin damage. Quercetin is a natural flavonoid that has been shown to have the highest anti-radical activity, along with the ability to act as a scavenger of free radicals and an inhibitor of lipid peroxidation. In this research work, a solvent-free solid lipid based nanosystem has been developed and evaluated for topical delivery of quercetin. Systematic screening of the formulation and process parameters led to the development of a solid lipid (glyceryl dibehenate) based nanosystem using a probe ultrasonication method. The selected variant demonstrated good physical stability for up to 8 weeks at 2-8 °C. Transmission electron microscopy (TEM) images showed spherical particles in the nanometer range. In vitro release studies showed biphasic release of quercetin from the SLN formulation, with an initial burst release followed by prolonged release for up to 24h. In vitro permeation studies using full thickness human skin showed higher amounts of quercetin to be localized within the skin compared to a control formulation with particles in the micrometer range. Such accumulation of quercetin in the skin is highly desirable since the efficacy of quercetin in delaying ultra-violet radiation mediated cell damage and eventual necrosis mainly occurs in the epidermis.
authors.affiliation: Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA.
authors.forename: Sonali
authors.initials: S
authors.lastname: Bose
authors.forename: Yuechao
authors.initials: Y
authors.lastname: Du
authors.forename: Paul
authors.initials: P
authors.lastname: Takhistov
authors.forename: Bozena
authors.initials: B
authors.lastname: Michniak-Kohn
mesh_terms: D000279:Administration, Cutaneous; D000975:Antioxidants / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D004355:Drug Stability; D004356:Drug Storage; D005227:Fatty Acids / Q000737:chemistry; D006801:Humans; D008055:Lipids / Q000737:chemistry; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D010316:Particle Size; D011794:Quercetin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012869:Skin Absorption; D013696:Temperature; D014018:Tissue Distribution; D014465:Ultrasonics
chemical_list: D000975:Antioxidants; D003692:Delayed-Action Preparations; D005227:Fatty Acids; D008055:Lipids; C086409:glyceryl behenate; D011794:Quercetin