The Physicochemical Properties, Antioxidant Potential, and Skin Penetration of Pterostilbene-Loaded NLCs
Abstract
Pterostilbene is a naturally occurring polyphenolic compound known for its antioxidant activity and potential use in topical skin care formulations. However, its poor water solubility and limited skin penetration reduce its therapeutic effectiveness. In this study, pterostilbene-loaded nanostructured lipid carriers (PT-NLCs) were developed and evaluated as a topical delivery system to enhance its stability and dermal performance. The PT-NLCs showed a mean particle size of 78–99 nm (88.57 ± 10.60 nm), a polydispersity index of 0.284, and an encapsulation efficiency of 99.98%, indicating a stable nanosystem. The NLC formulation increased apparent water solubility by over 5,000-fold and improved skin penetration by approximately 360% compared with raw pterostilbene. PT-NLCs also demonstrated enhanced antioxidant activity, with about a 34% increase in radical scavenging capacity in the DPPH assay and improved protection of skin cells against oxidative stress while maintaining good cytocompatibility. These findings demonstrate that NLC-based encapsulation effectively improves the solubility, dermal penetration, and antioxidant efficacy of pterostilbene, highlighting its potential as a promising ingredient for topical skin treatment applications.
Downloads
References
Akinwumi, B., Bordun, K.-A., & Anderson, H. (2018). Biological activities of stilbenoids. International Journal of Molecular Sciences, 19(3), 792. https://doi.org/10.3390/ijms19030792
Avelino, F. (2024). 2,2-Diphenyl-1-picrylhydrazyl (DPPH). (F. Avelino, Ed.). ScienceDirect; Academic Press. https://www.sciencedirect.com/science/article/abs/pii/B9780443215919000068?via%3Dihub
Barbieri, J. S., Wanat, K., & Seykora, J. (2014). Skin: Basic structure and function. Pathobiology of Human Disease, 1134–1144. https://doi.org/10.1016/b978-0-12-386456-7.03501-2
Bo, S., Chang, S. K., Zhu, H., Jiang, Y., & Yang, B. (2022). Naturally occurring prenylated stilbenoids: food sources, biosynthesis, applications and health benefits. Critical Reviews in Food Science and Nutrition, 1–24. https://doi.org/10.1080/10408398.2022.2056131
Chaiprateep, E., Wiemann, S., Eckert, R. W., Raab, C., Sengupta, S., & Keck, C. M. (2023). Influence of dose, particle size and concentration on dermal penetration efficacy of curcumin. Pharmaceutics, 15(11), 2645. https://doi.org/10.3390/pharmaceutics15112645
Chauhan, I., Yasir, M., Verma, M., & Singh, A. P. (2020). Nanostructured lipid carriers: A groundbreaking approach for transdermal drug delivery. Advanced Pharmaceutical Bulletin, 10(2), 150–165. https://doi.org/10.34172/apb.2020.021
Chen, A. Y., Lü, J.-M., Yao, Q., & Chen, C. (2016). Entacapone is an antioxidant more potent than vitamin C and vitamin E for scavenging of hypochlorous acid and peroxynitrite, and the inhibition of oxidative stress-induced cell death. Medical Science Monitor, 22, 687–696. https://doi.org/10.12659/msm.896462
Chu, L., Yu, Y., Choi, J., Kim, Y., Xiong, M., Lee, Y., & Xie, S. (2022). Research on the skin concerns of consumers with sensitive skin and their attitude and behavior toward derma products. Scientific and Social Research, 4(4), 124–141. https://doi.org/10.26689/ssr.v4i4.3681
Dutta, N., Garcia, G., & Ryo Higuchi‐Sanabria. (2024). Unveiling a novel cellular stress response mechanism to photodamage. Clinical and Translational Discovery, 4(2). https://doi.org/10.1002/ctd2.286
Fatiha, M., & Abdelkader, T. (2019). Study of antioxidant activity of pyrimidinium betaines by DPPH radical scavenging method. Journal of Analytical & Pharmaceutical Research, 8(2), 33–36. https://doi.org/10.15406/japlr.2019.08.00308
Fitriani, E. W., Avanti, C., Rosana, Y., & Surini, S. (2024). Nanostructured lipid carriers: A prospective dermal drug delivery system for natural active ingredients. Pharmacia, 71, 1–15. https://doi.org/10.3897/pharmacia.71.e115849
Garg, J., Pathania, K., Sah, S. P., & Pawar, S. V. (2022). Nanostructured lipid carriers: a promising drug carrier for targeting brain tumours. Future Journal of Pharmaceutical Sciences, 8(1). https://doi.org/10.1186/s43094-022-00414-8
Gomaa, E., Fathi, H. A., Eissa, N. G., & Elsabahy, M. (2021). Methods for preparation of nanostructured lipid carriers. Methods. https://doi.org/10.1016/j.ymeth.2021.05.003
Haq, N., Shakeel, F., Ghoneim, M. M., Asdaq, S. M. B., Alam, P., Aloatibi, F. O., & Alshehri, S. (2023). Determination of pterostilbene in pharmaceutical products using a new HPLC method and its application to solubility and stability samples. Separations, 10(3), 178. https://doi.org/10.3390/separations10030178
Herbig, M. E., Houdek, P., Gorissen, S., Zorn-Kruppa, M., Wladykowski, E., Volksdorf, T., Grzybowski, S., Kolios, G., Willers, C., Mallwitz, H., Moll, I., & Brandner, J. M. (2015). A custom tailored model to investigate skin penetration in porcine skin and its comparison with human skin. European Journal of Pharmaceutics and Biopharmaceutics, 95, 99–109. https://doi.org/10.1016/j.ejpb.2015.03.030
Hoshyar, N., Gray, S., Han, H., & Bao, G. (2016). The effect of nanoparticle size on in vivo pharmacokinetics and cellular interaction. Nanomedicine, 11(6), 673–692. https://doi.org/10.2217/nnm.16.5
Khan, S., Sharma, A., & Jain, V. (2022). An Overview of Nanostructured Lipid Carriers and Its Application in Drug Delivery through Different Routes. Advanced Pharmaceutical Bulletin. https://doi.org/10.34172/apb.2023.056
Lespade, L. (2017). Ab initio molecular dynamics of the reactivity of vitamin C toward hydroxyl and H2O2 radicals. Journal of Molecular Modeling, 23(12). https://doi.org/10.1007/s00894-017-3501-y
Mahor, A., Singh, P., Gupta, R., Bhardwaj, P., Rathore, P., Kishore, A., Goyal, R., Sharma, N., Verma, J., Rosenholm, J. M., & Bansal, K. K. (2023). Nanostructured lipid carriers for improved delivery of therapeutics via the oral route. Journal of Nanotechnology, 2023, 1–35. https://doi.org/10.1155/2023/4687959
Majeed, M., Majeed, S., Jain, R., Mundkur, L., Rajalakshmi, H., Lad, P. S., & Neupane, P. (2020). An open-label single-arm, monocentric study assessing the efficacy and safety of natural pterostilbene (pterocarpus marsupium) for skin brightening and antiaging effects. Clinical, Cosmetic and Investigational Dermatology, Volume 13, 105–116. https://doi.org/10.2147/ccid.s238358
Nagarajan, S., Mohandas, S., Ganesan, K., Xu, B., & Ramkumar, K. M. (2022). New Insights into Dietary Pterostilbene: Sources, Metabolism, and Health Promotion Effects. Molecules, 27(19), 6316. https://doi.org/10.3390/molecules27196316
Oh, W. Y., Gao, Y., & Shahidi, F. (2021). Stilbenoids: chemistry, occurrence, bioavailability and health effects—a review. Journal of Food Bioactives, 13. https://doi.org/10.31665/jfb.2020.13256
Ohenoja, K., Saari, J., Illikainen, M., Breitung‐Faes, S., Kwade, A., & Niinimäki, J. (2014). Effect of Polydispersity Index on the Grinding Limits of Highly Concentrated Limestone Suspensions. Chemical Engineering & Technology, 37(5), 833–839. https://doi.org/10.1002/ceat.201300415
Teng, W.-L., Huang, P.-H., Wang, H.-C., Tseng, C.-H., & Yen, F.-L. (2021). Pterostilbene attenuates particulate matter-induced oxidative stress, inflammation and aging in keratinocytes. Antioxidants, 10(10), 1552. https://doi.org/10.3390/antiox10101552
Waszczuk, M., Bianchi, S., Simony Martiny, Pittol, V., Denise, Sander, A., & Bassani, V. (2020). Development and validation of a specific-stability indicating liquid chromatography method for quantitative analysis of pterostilbene: application in food and pharmaceutical products. Analytical Methods, 12(35), 4310–4318. https://doi.org/10.1039/d0ay00989j
Yang, D., Liu, H., Meng, H., & Li, S. (2024). Preparation and physicochemical characterization of inclusion complex of pterostilbene-hydroxypropyl-β-cyclodextrin for enhancing the application of pterostilbene in cosmetics. Journal of Photochemistry and Photobiology a Chemistry, 447, 115221–115221. https://doi.org/10.1016/j.jphotochem.2023.115221
Zhang, R., Qin, X., Kong, F., Chen, P., & Pan, G. (2019). Improving cellular uptake of therapeutic entities through interaction with components of cell membrane. Drug Delivery, 26(1), 328–342. https://doi.org/10.1080/10717544.2019.1582730
Articles published in Indonesian Journal of Life Sciences are licensed under a Creative Commons Attribution-ShareAlike 4.0 International license. You are free to copy, transform, or redistribute articles for any lawful purpose in any medium, provided you give appropriate credit to the original author(s) and Indonesian Journal Life of Sciences, link to the license, indicate if changes were made, and redistribute any derivative work under the same license. Copyright on articles is retained by the respective author(s), without restrictions. A non-exclusive license is granted to Indonesian Journal Life of Sciences to publish the article and identify itself as its original publisher, along with the commercial right to include the article in a hardcopy issue for sale to libraries and individuals. By publishing in Indonesian Journal Life of Sciences, authors grant any third party the right to use their article to the extent provided by the Creative Commons Attribution-ShareAlike 4.0 International license.
