title: Development and In Vitro Evaluation of Vitamin E-Enriched Nanoemulsion Vehicles Loaded with Genistein for Chemoprevention Against UVB-Induced Skin Damage.
abstract: There is a great need for effective protection against cutaneous pathologies arising from chronic exposure to harmful solar UVB radiations. A promising pharmaceutical strategy to improve the efficacy of chemotherapeutic/preventative natural compounds (e.g., soy isoflavone Genistein, Gen) is to enhance their dermal delivery using nanoemulsion (NE) formulations. This report investigates the development of nanoemulsified tocotrienol(T3)-rich fraction of red palm oil (Tocomin®), to yield an optimal NE delivery system for dermal photoprotection (z-average size <150 nm, ζ-potential ≈ -30 mV, polydispersity index < 0.25). Physicochemical characterization and photostability studies indicate NE formulations utilizing surfactant mixture (Smix) of Solutol® HS-15 (SHS15) blended with vitamin E TPGS (TPGS) as cosurfactant was significantly superior to formulations that utilized Lutrol® F68 (LF68) as the cosurfactant. A ratio of 60:40 of SHS15-TPGS-NE was further identified as lead Tocomin® NE topical platform using in vitro pharmaceutical skin reactivity studies that assess cutaneous irritancy and cytotoxicity. Prototype Tocomin® NE loaded with the antiphotocarcinogenic molecule Gen (Gen-Tocomin® NE) showed slow-release profile in both liquid and cream forms. Gen-Tocomin® NE also showed excellent biocompatibility, and provided substantial UVB protection to cultured subcutaneous L929 fibroblasts, indicating the great potential of our Tocomin® NE warranting further prototype development as topical pharmaceutical platform for skin photoprotection applications.
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy-Glendale, Midwestern University, Glendale, Arizona, 85308.
authors.forename: Bill
authors.initials: B
authors.lastname: Brownlow
authors.affiliation: Department of Biochemistry, Midwestern University, Glendale, Arizona, 85308.
authors.forename: Vinay J
authors.initials: VJ
authors.lastname: Nagaraj
authors.affiliation: Midwestern University, College of Pharmacy-Glendale, Glendale, Arizona, 85308.
authors.forename: Amy
authors.initials: A
authors.lastname: Nayel
authors.affiliation: Arizona College of Osteopathic Medicine, Midwestern University, Glendale, Arizona, 85308.
authors.forename: Megha
authors.initials: M
authors.lastname: Joshi
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy-Glendale, Midwestern University, Glendale, Arizona, 85308.
authors.forename: Tamer
authors.initials: T
authors.lastname: Elbayoumi
mesh_terms: D000818:Animals; D016588:Anticarcinogenic Agents / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004285:Dogs; D016503:Drug Delivery Systems; D004355:Drug Stability; D004655:Emulsions; D019833:Genistein / Q000008:administration & dosage*; D061985:Madin Darby Canine Kidney Cells; D051379:Mice; D049329:Nanostructures; D000073878:Palm Oil; D014677:Pharmaceutical Vehicles; D010938:Plant Oils; D015595:Skin Aging / Q000187:drug effects* / Q000528:radiation effects*; D012878:Skin Neoplasms / Q000517:prevention & control; D013501:Surface-Active Agents; D014466:Ultraviolet Rays; D014810:Vitamin E / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D016588:Anticarcinogenic Agents; D004655:Emulsions; D014677:Pharmaceutical Vehicles; D010938:Plant Oils; D013501:Surface-Active Agents; D014810:Vitamin E; D000073878:Palm Oil; D019833:Genistein
keywords: biocompatibility; cancer chemoprevention; controlled release; in vitro models; nanoemulsion; photoprotection; physicochemical properties; self-emulsifying; skin reactivity; tocotrienol