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Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery

Yıl 2023, Cilt: 27 Sayı: 5, 1821 - 1830, 28.06.2025

Öz

Retinyl palmitate (RP), also known as vitamin A palmitate, is a well-known anti-aging ingredient that promotes collagen production, enhances skin flexibility, and decreases the view of fine lines and wrinkles. Squalene, a natural lipid found in the skin, is also known to have anti-aging properties, including moisturizing and protecting the skin from environmental stressors. In this study, we demonstrate the encapsulation of RP and squalene within niosomes, and evaluate the in-vitro release and skin permeation of these active ingredients. The niosomes were prepared using a thin-film hydration method and characterized for their particle size, polydispersity index, zeta potential, and encapsulation efficiency. The encapsulation efficiencies of optimized niosome formulation for RP and Squalene were determined to be 83.5%±2.55% and 91.2%±5.12%, respectively. Narrow size distribution was accomplished with a particle size of 168.4 ± 8.2 nm. Cumulative release of 82.67%±5.23% for RP and 87.12%±5.65% for Squalene was acquired after 24 hours of in-vitro release study in sink conditions. Ex-vivo permeation studies indicated that niosomes had a much higher retention rate for RP and Squalene in both the Stratum Corneum (SC) and viable epidermis/dermis layers when compared to the commercial product. Stability studies showed that the optimized niosomes were convenient for keeping at 4°C for at least 90 days. The outcomes show that niosomes are effective in delivering RP and squalene to the skin and can provide a promising alternative to traditional anti-aging formulations.

Kaynakça

  • [1] Farage MA, Miller KW, Elsner P, Maibach HI. Characteristics of the Aging Skin. Adv Wound Care 2013;2:5. https://doi.org/10.1089/WOUND.2011.0356.
  • [2] Auten RL, Davis JM. Oxygen Toxicity and Reactive Oxygen Species: The Devil Is in the Details. Pediatr Res 2009;66:121–7. https://doi.org/10.1203/pdr.0b013e3181a9eafb.
  • [3] Bokov A, Chaudhuri A, Richardson A. The role of oxidative damage and stress in aging. Mech Ageing Dev 2004;125:811–26. https://doi.org/10.1016/j.mad.2004.07.009.
  • [4] Lephart ED. Skin aging and oxidative stress: Equol’s anti-aging effects via biochemical and molecular mechanisms. Ageing Res Rev 2016;31:36–54. https://doi.org/10.1016/J.ARR.2016.08.001.
  • [5] Masaki H. Role of antioxidants in the skin: Anti-aging effects. J Dermatol Sci 2010;58:85–90. https://doi.org/10.1016/J.JDERMSCI.2010.03.003.
  • [6] Lozano-Grande MA, Gorinstein S, Espitia-Rangel E, Dávila-Ortiz G, Martínez-Ayala AL. Plant Sources, Extraction Methods, and Uses of Squalene. Int J Agron 2018;2018. https://doi.org/10.1155/2018/1829160.
  • [7] Yarkent C, Oncel SS. Recent Progress in Microalgal Squalene Production and Its Cosmetic Application. Biotechnol Bioprocess Eng 2022;27(3):295-305. https://doi.org/10.1007/s12257-021-0355-z.
  • [8] Ronco AL, de Stéfani E. Squalene: a multi-task link in the crossroads of cancer and aging. Funct Foods Heal Dis 2013;3:462–76. https://doi.org/10.31989/FFHD.V3I12.30.
  • [9] Bjørklund G, Shanaida M, Lysiuk R, Butnariu M, Peana M, Sarac I, et al. Natural Compounds and Products from an Anti-Aging Perspective. Mol 2022;27:7084. https://doi.org/10.3390/MOLECULES27207084.
  • [10] Nandy A, Lee E, Mandal A, Saremi R, Sharma S. Microencapsulation of retinyl palmitate by melt dispersion for cosmetic application. Food Addit Contam Part A 2020;37:205–19. https://doi.org/10.1080/02652048.2020.1720029.
  • [11] Silva S, Ferreira M, Oliveira AS, Magalhães C, Sousa ME, Pinto M, et al. Evolution of the use of antioxidants in anti-ageing cosmetics. Int J Cosmet Sci 2019;41:378–86. https://doi.org/10.1111/ICS.12551.
  • [12] Gianeti MD, Gaspar LR, De Camargo FB, Campos PMBGM. Benefits of Combinations of Vitamin A, C and E Derivatives in the Stability of Cosmetic Formulations. Mol 2012;17:2219–30. https://doi.org/10.3390/MOLECULES17022219.
  • [13] Sadgrove NJ, Oblong JE, Simmonds MSJ. Inspired by vitamin A for anti-ageing: Searching for plant-derived functional retinoid analogues. Ski Heal Dis 2021;1:e36. https://doi.org/10.1002/SKI2.36.
  • [14] Chen S, Hanning S, Falconer J, Locke M, Wen J. Recent advances in non-ionic surfactant vesicles (niosomes): Fabrication, characterization, pharmaceutical and cosmetic applications. Eur J Pharm Biopharm 2019;144:18–39. https://doi.org/10.1016/J.EJPB.2019.08.015.
  • [15] Mawazi SM, Ann TJ, Widodo RT. Application of Niosomes in Cosmetics: A Systematic Review. Cosmet 2022;9:127. https://doi.org/10.3390/COSMETICS9060127.
  • [16] Hamishehkar H, Rahimpour Y, Kouhsoltani M. Niosomes as a propitious carrier for topical drug delivery. Expert Opin Drug Deliv 2013;10:261–72. https://doi.org/10.1517/17425247.2013.746310.
  • [17] Kaur D, Kumar S. NIOSOMES: PRESENT SCENARIO AND FUTURE ASPECTS. J Drug Deliv Ther 2018;8:35–43. https://doi.org/10.22270/JDDT.V8I5.1886.
  • [18] Mohanty D, Rani MJ, Haque MA, Bakshi V, Jahangir MA, Imam SS, et al. Preparation and evaluation of transdermal naproxen niosomes: formulation optimization to preclinical anti-inflammatory assessment on murine model. J Liposome Res 2020;30:377–87. https://doi.org/10.1080/08982104.2019.1652646.
  • [19] Essa EA. Effect of formulation and processing variables on the particle size of sorbitan monopalmitate niosomes. Asian J Pharm 2010;4. https://doi.org/10.22377/AJP.V4I4.289.
  • [20] Mohammed AR, Weston N, Coombes AGA, Fitzgerald M, Perrie Y. Liposome formulation of poorly water soluble drugs: Optimisation of drug loading and ESEM analysis of stability. Int J Pharm 2004;285:23–34. https://doi.org/10.1016/j.ijpharm.2004.07.010.
  • [21] Basiri L, Rajabzadeh G, Bostan A. Physicochemical properties and release behavior of Span 60/Tween 60 niosomes as vehicle for α-Tocopherol delivery. LWT 2017;84:471–8. https://doi.org/10.1016/J.LWT.2017.06.009.
  • [22] Piri-Gharaghie T, Jegargoshe-Shirin N, Saremi-Nouri S, Khademhosseini SH, Hoseinnezhad-lazarjani E, Mousavi A, et al. Effects of Imipenem-containing Niosome nanoparticles against high prevalence methicillin-resistant Staphylococcus Epidermidis biofilm formed. Sci Rep 2022;12:1–13. https://doi.org/10.1038/s41598-022-09195-9.
  • [23] Haddadian A, Robattorki FF, Dibah H, Soheili A, Ghanbarzadeh E, Sartipnia N, et al. Niosomes-loaded selenium nanoparticles as a new approach for enhanced antibacterial, anti-biofilm, and anticancer activities. Sci Rep 2022;12:1–16. https://doi.org/10.1038/s41598-022-26400-x.
  • [24] Karim K, Mandal A, Biswas N, Guha A, Chatterjee S, Behera M, et al. Niosome: A future of targeted drug delivery systems. J Adv Pharm Technol Res 2010;1:374–80. https://doi.org/10.4103/0110-5558.76435.
  • [25] Briuglia M-L, Rotella C, McFarlane A, Lamprou DA. Influence of cholesterol on liposome stability and on in vitro drug release. Drug Deliv Transl Res 2015;5:231–42. https://doi.org/10.1007/s13346-015-0220-8.
  • [26] Rasul A, Khan MI, Rehman MU, Abbas G, Aslam N, Ahmad S, et al. In vitro Characterization and Release Studies of Combined Nonionic Surfactant-Based Vesicles for the Prolonged Delivery of an Immunosuppressant Model Drug. Int J Nanomedicine 2020;15:7937–49. https://doi.org/10.2147/IJN.S268846.
  • [27] Allam A, Fetih G. Sublingual fast dissolving niosomal films for enhanced bioavailability and prolonged effect of metoprolol tartrate. Drug Des Devel Ther 2016;10:2421. https://doi.org/10.2147/DDDT.S113775.
  • [28] Arslan Azizoglu G, Tuncay Tanriverdi S, Aydin Kose F, Ballar Kirmizibayrak P, Ozer O. Dual-Prevention for UV-Induced Skin Damage: Incorporation of Melatonin-Loaded Elastic Niosomes into Octyl Methoxycinnamate Pickering Emulsions. AAPS PharmSciTech 2017;18:2987–98. https://doi.org/10.1208/S12249-017-0786-1.
  • [29] Abdelbary G, El-Gendy N. Niosome-Encapsulated gentamicin for ophthalmic controlled delivery. AAPS PharmSciTech 2008;9:740–7. https://doi.org/10.1208/S12249-008-9105-1.
  • [30] Agarwal R, Katare OP, Vyas SP. Preparation and in vitro evaluation of liposomal/niosomal delivery systems for antipsoriatic drug dithranol. Int J Pharm 2001;228:43–52. https://doi.org/10.1016/S0378-5173(01)00810-9.
  • [31] Sezgin-Bayindir Z, Antep MN, Yuksel N. Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug. AAPS PharmSciTech 2015;16:108–17. https://doi.org/10.1208/S12249-014-0213-9.
  • [32] Ruckmani K, Jayakar B, Ghosal SK. Nonionic Surfactant Vesicles (Niosomes) of Cytarabine Hydrochloride for Effective Treatment of Leukemias: Encapsulation, Storage, and In Vitro Release. Drug Dev Ind Pharm 2000;26(2):217-22. https://doi.org/10.1081/DDC-100100348.
  • [33] Varelas CG, Dixon DG, Steiner CA. Zero-order release from biphasic polymer hydrogels. J Control Release 1995;34:185–92. https://doi.org/10.1016/0168-3659(94)00085-9.
  • [34] England CG, Miller MC, Kuttan A, Trent JO, Frieboes HB. Release kinetics of paclitaxel and cisplatin from two and three layered gold nanoparticles. Eur J Pharm Biopharm 2015;92:120–9. https://doi.org/10.1016/j.ejpb.2015.02.017.
  • [35] Higuchi T. Rate of release of medicaments from ointment bases containing drugs in suspension. J Pharm Sci 1961;50:874–5. https://doi.org/10.1002/jps.2600501018.
  • [36] Hixson AW, Crowell JH. Dependence of Reaction Velocity upon Surface and Agitation. Ind Eng Chem 1931;23:1160–8. https://doi.org/10.1021/ie50262a025.
  • [37] Erdal MS, Özhan G, Mat MC, Özsoy Y, Güngör S. Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations. Int J Nanomedicine 2016;11:1027. https://doi.org/10.2147/IJN.S96243.
Yıl 2023, Cilt: 27 Sayı: 5, 1821 - 1830, 28.06.2025

Öz

Kaynakça

  • [1] Farage MA, Miller KW, Elsner P, Maibach HI. Characteristics of the Aging Skin. Adv Wound Care 2013;2:5. https://doi.org/10.1089/WOUND.2011.0356.
  • [2] Auten RL, Davis JM. Oxygen Toxicity and Reactive Oxygen Species: The Devil Is in the Details. Pediatr Res 2009;66:121–7. https://doi.org/10.1203/pdr.0b013e3181a9eafb.
  • [3] Bokov A, Chaudhuri A, Richardson A. The role of oxidative damage and stress in aging. Mech Ageing Dev 2004;125:811–26. https://doi.org/10.1016/j.mad.2004.07.009.
  • [4] Lephart ED. Skin aging and oxidative stress: Equol’s anti-aging effects via biochemical and molecular mechanisms. Ageing Res Rev 2016;31:36–54. https://doi.org/10.1016/J.ARR.2016.08.001.
  • [5] Masaki H. Role of antioxidants in the skin: Anti-aging effects. J Dermatol Sci 2010;58:85–90. https://doi.org/10.1016/J.JDERMSCI.2010.03.003.
  • [6] Lozano-Grande MA, Gorinstein S, Espitia-Rangel E, Dávila-Ortiz G, Martínez-Ayala AL. Plant Sources, Extraction Methods, and Uses of Squalene. Int J Agron 2018;2018. https://doi.org/10.1155/2018/1829160.
  • [7] Yarkent C, Oncel SS. Recent Progress in Microalgal Squalene Production and Its Cosmetic Application. Biotechnol Bioprocess Eng 2022;27(3):295-305. https://doi.org/10.1007/s12257-021-0355-z.
  • [8] Ronco AL, de Stéfani E. Squalene: a multi-task link in the crossroads of cancer and aging. Funct Foods Heal Dis 2013;3:462–76. https://doi.org/10.31989/FFHD.V3I12.30.
  • [9] Bjørklund G, Shanaida M, Lysiuk R, Butnariu M, Peana M, Sarac I, et al. Natural Compounds and Products from an Anti-Aging Perspective. Mol 2022;27:7084. https://doi.org/10.3390/MOLECULES27207084.
  • [10] Nandy A, Lee E, Mandal A, Saremi R, Sharma S. Microencapsulation of retinyl palmitate by melt dispersion for cosmetic application. Food Addit Contam Part A 2020;37:205–19. https://doi.org/10.1080/02652048.2020.1720029.
  • [11] Silva S, Ferreira M, Oliveira AS, Magalhães C, Sousa ME, Pinto M, et al. Evolution of the use of antioxidants in anti-ageing cosmetics. Int J Cosmet Sci 2019;41:378–86. https://doi.org/10.1111/ICS.12551.
  • [12] Gianeti MD, Gaspar LR, De Camargo FB, Campos PMBGM. Benefits of Combinations of Vitamin A, C and E Derivatives in the Stability of Cosmetic Formulations. Mol 2012;17:2219–30. https://doi.org/10.3390/MOLECULES17022219.
  • [13] Sadgrove NJ, Oblong JE, Simmonds MSJ. Inspired by vitamin A for anti-ageing: Searching for plant-derived functional retinoid analogues. Ski Heal Dis 2021;1:e36. https://doi.org/10.1002/SKI2.36.
  • [14] Chen S, Hanning S, Falconer J, Locke M, Wen J. Recent advances in non-ionic surfactant vesicles (niosomes): Fabrication, characterization, pharmaceutical and cosmetic applications. Eur J Pharm Biopharm 2019;144:18–39. https://doi.org/10.1016/J.EJPB.2019.08.015.
  • [15] Mawazi SM, Ann TJ, Widodo RT. Application of Niosomes in Cosmetics: A Systematic Review. Cosmet 2022;9:127. https://doi.org/10.3390/COSMETICS9060127.
  • [16] Hamishehkar H, Rahimpour Y, Kouhsoltani M. Niosomes as a propitious carrier for topical drug delivery. Expert Opin Drug Deliv 2013;10:261–72. https://doi.org/10.1517/17425247.2013.746310.
  • [17] Kaur D, Kumar S. NIOSOMES: PRESENT SCENARIO AND FUTURE ASPECTS. J Drug Deliv Ther 2018;8:35–43. https://doi.org/10.22270/JDDT.V8I5.1886.
  • [18] Mohanty D, Rani MJ, Haque MA, Bakshi V, Jahangir MA, Imam SS, et al. Preparation and evaluation of transdermal naproxen niosomes: formulation optimization to preclinical anti-inflammatory assessment on murine model. J Liposome Res 2020;30:377–87. https://doi.org/10.1080/08982104.2019.1652646.
  • [19] Essa EA. Effect of formulation and processing variables on the particle size of sorbitan monopalmitate niosomes. Asian J Pharm 2010;4. https://doi.org/10.22377/AJP.V4I4.289.
  • [20] Mohammed AR, Weston N, Coombes AGA, Fitzgerald M, Perrie Y. Liposome formulation of poorly water soluble drugs: Optimisation of drug loading and ESEM analysis of stability. Int J Pharm 2004;285:23–34. https://doi.org/10.1016/j.ijpharm.2004.07.010.
  • [21] Basiri L, Rajabzadeh G, Bostan A. Physicochemical properties and release behavior of Span 60/Tween 60 niosomes as vehicle for α-Tocopherol delivery. LWT 2017;84:471–8. https://doi.org/10.1016/J.LWT.2017.06.009.
  • [22] Piri-Gharaghie T, Jegargoshe-Shirin N, Saremi-Nouri S, Khademhosseini SH, Hoseinnezhad-lazarjani E, Mousavi A, et al. Effects of Imipenem-containing Niosome nanoparticles against high prevalence methicillin-resistant Staphylococcus Epidermidis biofilm formed. Sci Rep 2022;12:1–13. https://doi.org/10.1038/s41598-022-09195-9.
  • [23] Haddadian A, Robattorki FF, Dibah H, Soheili A, Ghanbarzadeh E, Sartipnia N, et al. Niosomes-loaded selenium nanoparticles as a new approach for enhanced antibacterial, anti-biofilm, and anticancer activities. Sci Rep 2022;12:1–16. https://doi.org/10.1038/s41598-022-26400-x.
  • [24] Karim K, Mandal A, Biswas N, Guha A, Chatterjee S, Behera M, et al. Niosome: A future of targeted drug delivery systems. J Adv Pharm Technol Res 2010;1:374–80. https://doi.org/10.4103/0110-5558.76435.
  • [25] Briuglia M-L, Rotella C, McFarlane A, Lamprou DA. Influence of cholesterol on liposome stability and on in vitro drug release. Drug Deliv Transl Res 2015;5:231–42. https://doi.org/10.1007/s13346-015-0220-8.
  • [26] Rasul A, Khan MI, Rehman MU, Abbas G, Aslam N, Ahmad S, et al. In vitro Characterization and Release Studies of Combined Nonionic Surfactant-Based Vesicles for the Prolonged Delivery of an Immunosuppressant Model Drug. Int J Nanomedicine 2020;15:7937–49. https://doi.org/10.2147/IJN.S268846.
  • [27] Allam A, Fetih G. Sublingual fast dissolving niosomal films for enhanced bioavailability and prolonged effect of metoprolol tartrate. Drug Des Devel Ther 2016;10:2421. https://doi.org/10.2147/DDDT.S113775.
  • [28] Arslan Azizoglu G, Tuncay Tanriverdi S, Aydin Kose F, Ballar Kirmizibayrak P, Ozer O. Dual-Prevention for UV-Induced Skin Damage: Incorporation of Melatonin-Loaded Elastic Niosomes into Octyl Methoxycinnamate Pickering Emulsions. AAPS PharmSciTech 2017;18:2987–98. https://doi.org/10.1208/S12249-017-0786-1.
  • [29] Abdelbary G, El-Gendy N. Niosome-Encapsulated gentamicin for ophthalmic controlled delivery. AAPS PharmSciTech 2008;9:740–7. https://doi.org/10.1208/S12249-008-9105-1.
  • [30] Agarwal R, Katare OP, Vyas SP. Preparation and in vitro evaluation of liposomal/niosomal delivery systems for antipsoriatic drug dithranol. Int J Pharm 2001;228:43–52. https://doi.org/10.1016/S0378-5173(01)00810-9.
  • [31] Sezgin-Bayindir Z, Antep MN, Yuksel N. Development and characterization of mixed niosomes for oral delivery using candesartan cilexetil as a model poorly water-soluble drug. AAPS PharmSciTech 2015;16:108–17. https://doi.org/10.1208/S12249-014-0213-9.
  • [32] Ruckmani K, Jayakar B, Ghosal SK. Nonionic Surfactant Vesicles (Niosomes) of Cytarabine Hydrochloride for Effective Treatment of Leukemias: Encapsulation, Storage, and In Vitro Release. Drug Dev Ind Pharm 2000;26(2):217-22. https://doi.org/10.1081/DDC-100100348.
  • [33] Varelas CG, Dixon DG, Steiner CA. Zero-order release from biphasic polymer hydrogels. J Control Release 1995;34:185–92. https://doi.org/10.1016/0168-3659(94)00085-9.
  • [34] England CG, Miller MC, Kuttan A, Trent JO, Frieboes HB. Release kinetics of paclitaxel and cisplatin from two and three layered gold nanoparticles. Eur J Pharm Biopharm 2015;92:120–9. https://doi.org/10.1016/j.ejpb.2015.02.017.
  • [35] Higuchi T. Rate of release of medicaments from ointment bases containing drugs in suspension. J Pharm Sci 1961;50:874–5. https://doi.org/10.1002/jps.2600501018.
  • [36] Hixson AW, Crowell JH. Dependence of Reaction Velocity upon Surface and Agitation. Ind Eng Chem 1931;23:1160–8. https://doi.org/10.1021/ie50262a025.
  • [37] Erdal MS, Özhan G, Mat MC, Özsoy Y, Güngör S. Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations. Int J Nanomedicine 2016;11:1027. https://doi.org/10.2147/IJN.S96243.
Toplam 37 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Eczacılık ve İlaç Bilimleri (Diğer)
Bölüm Articles
Yazarlar

Ali Asram Sağıroğlu 0000-0002-6960-6364

Beyza Sümeyye Aydın 0000-0003-4066-1105

Yayımlanma Tarihi 28 Haziran 2025
Yayımlandığı Sayı Yıl 2023 Cilt: 27 Sayı: 5

Kaynak Göster

APA Sağıroğlu, A. A., & Aydın, B. S. (2025). Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery. Journal of Research in Pharmacy, 27(5), 1821-1830.
AMA Sağıroğlu AA, Aydın BS. Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery. J. Res. Pharm. Temmuz 2025;27(5):1821-1830.
Chicago Sağıroğlu, Ali Asram, ve Beyza Sümeyye Aydın. “Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery”. Journal of Research in Pharmacy 27, sy. 5 (Temmuz 2025): 1821-30.
EndNote Sağıroğlu AA, Aydın BS (01 Temmuz 2025) Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery. Journal of Research in Pharmacy 27 5 1821–1830.
IEEE A. A. Sağıroğlu ve B. S. Aydın, “Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery”, J. Res. Pharm., c. 27, sy. 5, ss. 1821–1830, 2025.
ISNAD Sağıroğlu, Ali Asram - Aydın, Beyza Sümeyye. “Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery”. Journal of Research in Pharmacy 27/5 (Temmuz 2025), 1821-1830.
JAMA Sağıroğlu AA, Aydın BS. Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery. J. Res. Pharm. 2025;27:1821–1830.
MLA Sağıroğlu, Ali Asram ve Beyza Sümeyye Aydın. “Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery”. Journal of Research in Pharmacy, c. 27, sy. 5, 2025, ss. 1821-30.
Vancouver Sağıroğlu AA, Aydın BS. Preparation and Characterization of Topical Niosomal Formulation Containing Retinyl Palmitate and Squalane for Enhanced Skin Delivery. J. Res. Pharm. 2025;27(5):1821-30.