title: Proretinal nanoparticles: stability, release, efficacy, and irritation.
abstract: Despite many potent biological activities, retinoids such as retinoic acid (RA) and retinal possess dose-related broad side effects. In this study, we show that this problem, which has been unsolvable for a long time, can be tackled through a controlled release strategy in which retinal is continuously delivered to the skin via sustained release from proretinal nanoparticles. The water dispersible proretinal nanoparticles are stable when kept in water at neutral pH and at room temperature for 8 months under light-proof conditions, and show sustained release of retinal into human synthetic sebum at a pH of 5. In the daily topical application tests performed for 4 weeks on rats' skin, the nanoparticles showed superior ability to increase epidermal thickness compared to RA and retinal, with no skin irritation observed for the proretinal particles, but severe skin irritation observed for RA and free retinal. When tested under occlusion conditions in human volunteers, insignificant skin irritation was observed for the proretinal nanoparticles. The 12-week, double-blind, split-face study on human volunteers indicates better antiaging efficacy of the particles as compared to the free RA.
authors: Program in Technopreneurship and Innovation Management, Graduate School.
authors: Pimolphan
authors: P
authors: Pisetpackdeekul
authors: Program in Biotechnology.
authors: Piyapan
authors: P
authors: Supmuang
authors: Department of Chemistry, Faculty of Science.
authors: Porntip
authors: P
authors: Pan-In
authors: Department of Pathology, Faculty of Veterinary Science, Chulalongkorn University.
authors: Wijit
authors: W
authors: Banlunara
authors: Department of Pathology, Faculty of Veterinary Science, Chulalongkorn University.
authors: Benchaphorn
authors: B
authors: Limcharoen
authors: Division of Dermatology, Department of Medicine, Faculty of Medicine, Ramathibodi Hospital.
authors: Chayada
authors: C
authors: Kokpol
authors: Department of Chemistry, Faculty of Science; Nanotec-Chulalongkorn University Center of Excellence on Food and Agriculture, Chulalongkorn University, Bangkok, Thailand.
authors: Supason
authors: S
authors: Wanichwecharungruang
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D000375:Aging / Q000187:drug effects; D000818:Animals; D004311:Double-Blind Method; D065546:Drug Liberation; D004355:Drug Stability; D004817:Epidermis / Q000187:drug effects / Q000473:pathology; D005260:Female; D006801:Humans; D007509:Irritants / Q000494:pharmacology*; D008297:Male; D008875:Middle Aged; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D051381:Rats; D012629:Sebum / Q000187:drug effects; D014212:Tretinoin / Q000008:administration & dosage / Q000494:pharmacology*; D055815:Young Adult
chemical_list: D007509:Irritants; D014212:Tretinoin
keywords: antiaging; drug delivery; release; sebum; skin