Lipid matrix composition-tuned nanoparticles for enhanced topical retinol delivery and anti-photoaging efficacy.
- 1Department of Biotechnology, College of Life Science and Biotechnology, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, South Korea.
- 2Graduate Program in Bioindustrial Engineering, College of Life Science and Biotechnology, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, South Korea.
- 3Genewel, 6F, Star Tower 37, Sagimakgol-ro 2beon-gil, Jungwon-gu, Seongnam-si, Gyeonggi-do 13211, South Korea.
Abstract
Retinol (Ret), a hydrophobic vitamin A derivative, is widely used for skin rejuvenation, inhibiting the degradation of major extracellular matrix components such as collagen. Ret has been incorporated into lipid nanoparticles, such as liposomes, to improve stability. However, the long-term stability of these formulations under temperature variations as well as systematic optimization remain unknown. To overcome these limitations, we developed a retinol-loaded nanostructured lipid carrier (Ret-NLC) by optimizing the solid-to-liquid ratio (SL ratio) to enhance long-term stability, cellular delivery efficacy, and skin permeation. The formulation was optimized at an SL ratio of 6:4, achieving a particle size of approximately 200 nm and acceptable size distribution (polydispersity index, PDI ≈ 0.3). Ret-NLC stored at 25 and 4 °C maintained favorable dispersion characteristics during 12 weeks of storage, and in vitro release studies showed sustained release of Ret. In addition, among the tested SL ratios, Ret-NLC (6:4) exhibited the highest skin-mimetic membrane permeation, with an approximately 4.5-fold increase compared with free Ret, indicating suitability for the delivery of hydrophobic bioactive compounds to the skin. Biological evaluation revealed that Ret-NLC effectively reduced reactive oxygen species (ROS) and suppressed matrix metalloproteinase-1 (MMP-1) expression by 63.6%, which are key factors associated with skin aging and extracellular matrix degradation. Finally, Ret-NLC was incorporated into a cream formulation for practical applications. Compared with the Ret cream, the Ret-NLC cream exhibited improved formulation stability, while maintaining its physicochemical properties. Overall, these findings support the potential of Ret-NLC as a nanoplatform for delivering hydrophobic bioactive compounds in biopharmaceutical applications.
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BibTeX
@article{shin2026lipid,
title = {{Lipid matrix composition-tuned nanoparticles for enhanced topical retinol delivery and anti-photoaging efficacy.}},
author = {Hae Kyung Shin and Eun Yong Lee and Seunghyeon Lee and Chaelin Min and Minyoung Yi and Sung Yeon Cho and Sang Hyeon Bok and Young Hoon Roh},
journal = {International journal of pharmaceutics: X},
year = {2026},
month = sep,
doi = {10.1016/j.ijpx.2026.100668},
url = {https://europepmc.org/article/MED/42840803},
note = {CC BY-NC-ND},
}
RIS
TY - JOUR
TI - Lipid matrix composition-tuned nanoparticles for enhanced topical retinol delivery and anti-photoaging efficacy.
AU - Hae Kyung Shin
AU - Eun Yong Lee
AU - Seunghyeon Lee
AU - Chaelin Min
AU - Minyoung Yi
AU - Sung Yeon Cho
AU - Sang Hyeon Bok
AU - Young Hoon Roh
PY - 2026
DA - 2026/09/24
JO - International journal of pharmaceutics: X
DO - 10.1016/j.ijpx.2026.100668
UR - https://europepmc.org/article/MED/42840803
AB - Retinol (Ret), a hydrophobic vitamin A derivative, is widely used for skin rejuvenation, inhibiting the degradation of major extracellular matrix components such as collagen. Ret has been incorporated into lipid nanoparticles, such as liposomes, to improve stability. However, the long-term stability of these formulations under temperature variations as well as systematic optimization remain unknown. To overcome these limitations, we developed a retinol-loaded nanostructured lipid carrier (Ret-NLC) by optimizing the solid-to-liquid ratio (SL ratio) to enhance long-term stability, cellular delivery efficacy, and skin permeation. The formulation was optimized at an SL ratio of 6:4, achieving a particle size of approximately 200 nm and acceptable size distribution (polydispersity index, PDI ≈ 0.3). Ret-NLC stored at 25 and 4 °C maintained favorable dispersion characteristics during 12 weeks of storage, and in vitro release studies showed sustained release of Ret. In addition, among the tested SL ratios, Ret-NLC (6:4) exhibited the highest skin-mimetic membrane permeation, with an approximately 4.5-fold increase compared with free Ret, indicating suitability for the delivery of hydrophobic bioactive compounds to the skin. Biological evaluation revealed that Ret-NLC effectively reduced reactive oxygen species (ROS) and suppressed matrix metalloproteinase-1 (MMP-1) expression by 63.6%, which are key factors associated with skin aging and extracellular matrix degradation. Finally, Ret-NLC was incorporated into a cream formulation for practical applications. Compared with the Ret cream, the Ret-NLC cream exhibited improved formulation stability, while maintaining its physicochemical properties. Overall, these findings support the potential of Ret-NLC as a nanoplatform for delivering hydrophobic bioactive compounds in biopharmaceutical applications.
SN - 2590-1567
ER -