Design of High-Payload Ascorbyl Palmitate Nanosuspensions for Enhanced Skin Delivery
Open Access
- 25 January 2024
- journal article
- research article
- Published by MDPI AG in Pharmaceutics
- Vol. 16 (2) , 171
Abstract
A high-payload ascorbyl palmitate (AP) nanosuspension (NS) was designed to improve skin delivery following topical application. The AP-loaded NS systems were prepared using the bead-milling technique, and softly thickened into NS-loaded gel (NS-G) using hydrophilic polymers. The optimized NS-G system consisted of up to 75 mg/mL of AP, 0.5% w/v of polyoxyl-40 hydrogenated castor oil (Kolliphor® RH40) as the suspending agent, and 1.0% w/v of sodium carboxymethyl cellulose (Na.CMC 700 K) as the thickening agent, in citrate buffer (pH 4.5). The NS-G system was embodied as follows: long and flaky nanocrystals, 493.2 nm in size, −48.7 mV in zeta potential, and 2.3 cP of viscosity with a shear rate of 100 s−1. Both NS and NS-G provided rapid dissolution of the poorly water-soluble antioxidant, which was comparable to that of the microemulsion gel (ME-G) containing AP in solubilized form. In an ex vivo skin absorption study using the Franz diffusion cell mounted on porcine skin, NS-G exhibited faster absorption in skin, providing approximately 4, 3, and 1.4 times larger accumulation than that of ME-G at 3, 6, and 12 h, respectively. Therefore, the high-payload NS makes it a promising platform for skin delivery of the lipid derivative of ascorbic acid.Keywords
Funding Information
- National Research Foundation of Korea (NRF) (NRF-2022R1C1C1004561)
This publication has 59 references indexed in Scilit:
- The methods of determination of critical micellar concentrations of the amphiphilic systems in aqueous mediumArabian Journal of Chemistry, 2011
- The Influence of Sodium Carboxymethylcellulose on Drug Release from Polyethylene Oxide Extended Release MatricesAAPS PharmSciTech, 2011
- A New Approach for Increasing Ascorbyl Palmitate Stability by Addition of Non-irritant Co-antioxidantAAPS PharmSciTech, 2010
- Hydrogel-thickened nanoemulsion system for topical delivery of lipophilic drugsInternational Journal of Pharmaceutics, 2008
- Reversible degradation kinetics of ascorbic acid under reducing and oxidizing conditionsFood Chemistry, 2007
- Encapsulation of ascorbyl palmitate in nanostructured lipid carriers (NLC)—Effects of formulation parameters on physicochemical stabilityInternational Journal of Pharmaceutics, 2007
- Transcutaneous immunization of domestic animals: opportunities and challengesAdvanced Drug Delivery Reviews, 2000
- Swelling Behavior of Carboxymethylcellulose Hydrogels in Relation to Cross-Linking, pH, and Charge DensityMacromolecules, 2000
- Confocal laser scanning microscopy of porcine skin: implications for human wound healing studiesJournal of Anatomy, 1997
- The biodegradability and nontoxicity of carboxymethyl cellulose (DS 0.7) and intermediatesEnvironmental Toxicology and Chemistry, 1996