Polymeric Micelles of PEG-PE as Carriers of All-Trans Retinoic Acid for Stability Improvement
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- Wichit, A., Tangsumranjit, A., Pitaksuteepong, T. et al. AAPS PharmSciTech (2012) 13: 336. doi:10.1208/s12249-011-9749-0
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 (PEG750-DPPE) micelles. The PEG750-DPPE micelle could significantly retard ATRA oxidation compared to ATRA in 75% methanol/HBS solution. Up to 87% of ATRA remained in the PEG750-DPPE micelle solution after storage in ambient air for 28 days. This result suggests that PEG750-DPPE micelle can improve ATRA stability. Therefore, ATRA in PEG750-DPPE micelle is an interesting alternative structure for the development of cosmeceutical formulations.