Design of High-Payload Ascorbyl Palmitate Nanosuspensions for Enhanced Skin Delivery
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Published:2024-01-25
Issue:2
Volume:16
Page:171
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ISSN:1999-4923
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Container-title:Pharmaceutics
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language:en
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Short-container-title:Pharmaceutics
Author:
Park Jun-Soo1, Choi Jun-Hyuk1, Joung Min-Yeong1, Yang In-Gyu1, Choi Yong-Seok1, Kang Myung-Joo1ORCID, Ho Myoung-Jin1
Affiliation:
1. College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan 31116, Republic of Korea
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.
Funder
National Research Foundation of Korea
Subject
Pharmaceutical Science
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