title: Polymeric micelles of PEG-PE as carriers of all-trans retinoic acid for stability improvement.
abstract: The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several skin disorders, including photo-aging. Unfortunately, ATRA is susceptible to light, heat, and oxidizing agents. Thus, this study aimed to investigate the ability of polymeric micelles prepared from polyethylene glycol conjugated phosphatidylethanolamine (PEG-PE) to stabilize ATRA under various storage conditions. ATRA entrapped in polymeric micelles with various PEG and PE structures was prepared. The critical micelle concentrations were 97-243 μM, depending on the structures of the PEG and PE molecules. All of the micelles had particle diameters of 6-20 nm and neutral charges. The highest entrapment efficiency (82.7%) of the tested micelles was exhibited by ATRA in PEG with a molecular weight of 750 Da conjugated to dipalmitoyl phosphatidylethanolamine (PEG(750)-DPPE) micelles. The PEG(750)-DPPE micelle could significantly retard ATRA oxidation compared to ATRA in 75% methanol/HBS solution. Up to 87% of ATRA remained in the PEG(750)-DPPE micelle solution after storage in ambient air for 28 days. This result suggests that PEG(750)-DPPE micelle can improve ATRA stability. Therefore, ATRA in PEG(750)-DPPE micelle is an interesting alternative structure for the development of cosmeceutical formulations.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand.
authors.forename: Angkana
authors.initials: A
authors.lastname: Wichit
authors.forename: Anothai
authors.initials: A
authors.lastname: Tangsumranjit
authors.forename: Tasana
authors.initials: T
authors.lastname: Pitaksuteepong
authors.forename: Neti
authors.initials: N
authors.lastname: Waranuch
mesh_terms: D002152:Calorimetry, Differential Scanning / Q000379:methods; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D004355:Drug Stability; D008823:Micelles; D010714:Phosphatidylethanolamines / Q000008:administration & dosage / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D014212:Tretinoin / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D008823:Micelles; D010714:Phosphatidylethanolamines; C067972:dioleoyl-N-(monomethoxypolyethylene glycol succinyl)phosphatidylethanolamine; D011092:Polyethylene Glycols; D014212:Tretinoin