Design of High-Payload Ascorbyl Palmitate Nanosuspensions for Enhanced Skin Delivery

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 syste...

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Bibliographic Details
Published in:Pharmaceutics 2024-01, Vol.16 (2), p.171
Main Authors: Park, Jun-Soo, Choi, Jun-Hyuk, Joung, Min-Yeong, Yang, In-Gyu, Choi, Yong-Seok, Kang, Myung-Joo, Ho, Myoung-Jin
Format: Article
Language:English
Subjects:
Acids
Antioxidants
ascorbyl palmitate
bead-milling
Care and treatment
Cellulose
colloidal dispersion
dissolution
hydrogel
Hydrogels
Lipids
Molecular weight
Nanocrystals
Nanoparticles
nanosuspension
Organic acids
Particle size
Polyethylene glycol
Polymers
Polyvinyl alcohol
Skin
Surfactants
Viscosity
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Summary: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% / of polyoxyl-40 hydrogenated castor oil (Kolliphor RH40) as the suspending agent, and 1.0% / 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 . 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.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics16020171