Development of niacinamide loaded elastic liposome as a potential transepidermal delivery system

Waree Tiyaboonchai; Panatda Ngammuangman; Suchiwa Pan-On; Duy Toan Pham

doi:10.7324/JAPS.2025.214096

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Abstract

Niacinamide (NA), one of the most frequently utilized materials in cosmeceutical areas, possesses a drawback in its ability to penetrate the skin layers. To overcome this, the present study developed and characterized novel NA-loaded elastic liposomes (EL) to enhance the NA transepidermal penetration. The EL were prepared by reverse phase evaporation technique with different NA content of 100, 150, and 200 mg. The developed NA-loaded EL demonstrated mean sizes of ~300 nm, polydispersity indexes of 0.2–0.3, zeta potentials of ~-20 mV, and moderate entrapment efficiencies of up to 40%. The liposome formation was confirmed by a Maltese cross-like structure, observed under polarized light microscopy, with a high elasticity property. Interestingly, the NA-loaded EL showed 100 times greater in-vitro permeation-enhancing effect than the NA cream counterpart. Conclusively, the novel NA-loaded EL have much potential in the transepidermal delivery of hydrophilic molecules, such as NA, across the skin.

Keyword: Elastic liposomes drug delivery system niacinamide permeation transepidermal delivery

Citation:

Tiyaboonchai W, Ngammuangman P, Pan-On S, Pham DT. Development of niacinamide loaded elastic liposome as a potential transepidermal delivery system. J Appl Pharm Sci. 2025. Online First. http://doi.org/10.7324/JAPS.2025.214096

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Reference

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2. Gensler HL. Prevention of photoimmunosuppression and photocarcinogenesis by topical nicotinamide. Nutr Cancer. 1997;29:157-62. https://doi.org/10.1080/01635589709514618
3. Shalita AR, Smith JG, Parish LC, Sofman MS, Chalker DK. Topical nicotinamide compared with clindamycin gel in the treatment on inflammatory acne vulgaris. Pharmacol Therap. 1995;34:434-7. https://doi.org/10.1111/j.1365-4362.1995.tb04449.x
4. Levin J, Momin SB. How much do we really know about our favorite cosmeceutical ingredients? J Clin Aesthet Dermatol. 2010;3:22-41.
5. Hakozaki T, Minwalla L, Zhuang J, Chhoa M, Matsubara A, Miyamoto K, et al. The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br J Dermatol. 2002;147:20-31. https://doi.org/10.1046/j.1365-2133.2002.04834.x
6. Tanno O, Ota Y, Kitamura N, Katsube T, Inoue SNicotinamide increases biosynthesis of ceramides as well as other stratum corneum lipids to improve the epidermal permeability barrier. Br J Dermatol. 2000;143:524-31. https://doi.org/10.1111/j.1365-2133.2000.03705.x
7. Matts PJ, Oblong JE, Bissett DL. A review of the range of effects of nacinamide in human skin. IFSCC Mag. 2016;5:285-9.
8. Namazi MR. Nicotinamide as a potential addition to the anti-atopic dermatitis armamentarium. Int Immunopharmacol. 2004;4:709-12. https://doi.org/10.1016/j.intimp.2003.11.008
9. Lee MH, Lee KK, Park MH, Hyun SS, Kahn SY, Joo KS, et al. In vivo anti-melanogenesis activity and in vitro skin permeability of niacinamide-loaded flexible liposomes (bounsphere™). J Drug Deliv Sci Technol. 2016;31:147-52. https://doi.org/10.1016/j.jddst.2015.12.008
10. Manela-Azulay M, Bagatin E. Cosmeceuticals vitamins. Clin Dermatol. 2009;27(5):469-74. https://doi.org/10.1016/j.clindermatol.2009.05.010
11. Feldmann RJ, Maibach HI. Absorption of some organic compounds through the skin in man. J Invest Dermatol. 1970;54:399-404. https://doi.org/10.1111/1523-1747.ep12259184
12. Boo YC. Mechanistic basis and clinical evidence for the applications of nicotinamide (niacinamide) to control skin aging and pigmentation. Antioxidants. 2021;10:1-24. https://doi.org/10.3390/antiox10081315
13. Kasetvatin C, Rujivipat S, Tiyaboonchai W. Combination of elastic liposomes and low frequency ultrasound for skin permeation enhancement of hyaluronic acid. Colloids Surf B Biointerfaces. 2015;135:458-64. https://doi.org/10.1016/j.colsurfb.2015.07.078
14. Pan-On S, Rujivipat S, Ounaroon A, Kongkaew C, Tiyaboonchai W. Development, characterization and skin irritation of mangosteen peel extract solid dispersion containing clay facial mask. Int J Appl Pharm. 2018;10:202-7. https://doi.org/10.22159/ijap.2018v10i5.28247
15. Pham DT, Chokamonsirikun A, Phattaravorakarn V, Tiyaboonchai W. Polymeric micelles for pulmonary drug delivery: a comprehensive review. J Mater Sci. 2020a;56:2016-36. https://doi.org/10.1007/s10853-020-05361-4
16. Pham DT, Saelim N, Tiyaboonchai W. Paclitaxel loaded EDC-crosslinked fibroin nanoparticles: a potential approach for colon cancer treatment. Drug Deliv Transl Res. 2020b;10:413-24. https://doi.org/10.1007/s13346-019-00682-7
17. Pham DT, Tiyaboonchai W. Fibroin nanoparticles: a promising drug delivery system. Drug Deliv. 2020c;27:431-48. https://doi.org/10.1080/10717544.2020.1736208
18. Akbarzadeh A, Rezaei-Sadabady R, Davaran S, Joo SW, Zarghami N, Hanifehpour Y, et al. Liposome: classification, preparation, and applications. Nanoscale Res Lett. 2013;8:1-9. https://doi.org/10.1186/1556-276X-8-102
19. Hussain A, Singh S, Sharma D, Webster TJ, Shafaat K, Faruk A. Elastic liposomes as novel carriers: recent advances in drug delivery. Int J Nanomed. 2017;12:5087-108. https://doi.org/10.2147/IJN.S138267
20. Benson HA. Elastic liposomes for topical and transdermal drug delivery. Methods Mol Biol. 2010;605:77-86. https://doi.org/10.1007/978-1-60327-360-2_4
21. Iqbal B, Ali J, Baboota S. Recent advances and development in epidermal and dermaldrug deposition enhancement technology. Int Soc Dermatol. 2018;57:646-60. https://doi.org/10.1111/ijd.13902
22. Chen G, Li D, Jin Y, Zhang W, Teng L, Bunt C, et al. Deformable liposomes by reverse-phase evaporation method for an enhanced skin delivery of (+)-catechin. Drug Dev Ind Pharm. 2014;40(2):260-5. https://doi.org/10.3109/03639045.2012.756512
23. El Zaafarany GM, Awad GA, Holayel SM, Mortada ND. Role of edge activators and surface charge in developing ultradeformable vesicles with enhanced skin delivery. Int J Pharm. 2010;397(1-2):164-72. https://doi.org/10.1016/j.ijpharm.2010.06.034
24. Léonard A, Dufourc EJ. Interactions of cholesterol with the membrane lipid matrix. A solid state NMR approach. Biochimie. 1991;73:1295-302. https://doi.org/10.1016/0300-9084(91)90092-F
25. Magarkar A, Dhawan V, Kallinteri P, Viitala T, Elmowafy M, Róg T, et al. Cholesterol level affects surface charge of lipid membranes in saline solution. Sci Rep. 2014;4:1-5. https://doi.org/10.1038/srep05005
26. Moore TL, Rodriguez-Lorenzo L, Hirsch V, Balog S, Urban D, Jud C, et al. Nanoparticle colloidal stability in cell culture media and impact on cellular interactions. Chem Soc Rev. 2015;44:6287-305. https://doi.org/10.1039/C4CS00487F
27. Vicit Rizal ES, Chung I, Misran M. Pegylated oleic acid-lecithin liposomes (poll) for anticancer drug delivery. Sains Malays. 2020;49:19-27. https://doi.org/10.17576/jsm-2020-4901-03
28. Jacobi U, Kaiser M, Toll R, Mangelsdorf S, Audring H, Otberg N, et al. Porcine ear skin: an in vitro model for human skin. Skin Res Technol. 2007;13:19-24. https://doi.org/10.1111/j.1600-0846.2006.00179.x
29. Haque T, Lane ME, Sil BC, Crowther JM, Moore DJ. In vitro permeation and disposition of niacinamidein silicone and porcine skin of skin barrier-mimetic formulations. Int J Pharm. 2017;30:158-62. https://doi.org/10.1016/j.ijpharm.2017.01.054
30. Cevc G. Lipid vesicles and other colloids as drug carriers on the skin. Adv Drug Deliv Rev. 2004;56:675-711. https://doi.org/10.1016/j.addr.2003.10.028
31. van den Bergh BA, Bouwstra JA, Junginger HE, Wertz PW. Elasticity of vesicles affects hairless mouse skin structure and permeability. J Control Release. 1999a;62:367-79. https://doi.org/10.1016/S0168-3659(99)00168-6
32. van den Bergh BA, Vroom J, Gerritsen H, Junginger HE, Bouwstra JA. Interactions of elastic and rigid vesicles with human skin in vitro: electron microscopy and two-photon excitation microscopy. Biochim Biophys Acta. 1999b;1461:155-73. https://doi.org/10.1016/S0005-2736(99)00176-5
33. Verma A, Jain A, Hurkat P, Jain SK. Transfollicular drug delivery: current perspectives. Res Rep Transdermal Drug Deliv. 2016;5:1-17. https://doi.org/10.2147/RRTD.S75809
34. Subongkot T, Wonglertnirant N, Songprakhon P, Rojanarata T, Opanasopit P, Ngawhirunpat T. Visualization of ultradeformable liposomes penetration pathways and their skin interaction by confocal laser scanning microscopy. Int J Pharm. 2013;441:151-61. https://doi.org/10.1016/j.ijpharm.2012.12.003

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1. Bowes J, Piper J, Thiemermann C. Inhibitors of the activity of poly (ADP-ribose) synthetase reduce the cell death caused by hydrogen peroxide in human cardiac myoblasts. Br J Pharmacol. 1998;124:1760-6. https://doi.org/10.1038/sj.bjp.0702009

2. Gensler HL. Prevention of photoimmunosuppression and photocarcinogenesis by topical nicotinamide. Nutr Cancer. 1997;29:157-62. https://doi.org/10.1080/01635589709514618

3. Shalita AR, Smith JG, Parish LC, Sofman MS, Chalker DK. Topical nicotinamide compared with clindamycin gel in the treatment on inflammatory acne vulgaris. Pharmacol Therap. 1995;34:434-7. https://doi.org/10.1111/j.1365-4362.1995.tb04449.x

4. Levin J, Momin SB. How much do we really know about our favorite cosmeceutical ingredients? J Clin Aesthet Dermatol. 2010;3:22-41.

5. Hakozaki T, Minwalla L, Zhuang J, Chhoa M, Matsubara A, Miyamoto K, et al. The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br J Dermatol. 2002;147:20-31. https://doi.org/10.1046/j.1365-2133.2002.04834.x

6. Tanno O, Ota Y, Kitamura N, Katsube T, Inoue SNicotinamide increases biosynthesis of ceramides as well as other stratum corneum lipids to improve the epidermal permeability barrier. Br J Dermatol. 2000;143:524-31. https://doi.org/10.1111/j.1365-2133.2000.03705.x

7. Matts PJ, Oblong JE, Bissett DL. A review of the range of effects of nacinamide in human skin. IFSCC Mag. 2016;5:285-9.

8. Namazi MR. Nicotinamide as a potential addition to the anti-atopic dermatitis armamentarium. Int Immunopharmacol. 2004;4:709-12. https://doi.org/10.1016/j.intimp.2003.11.008

9. Lee MH, Lee KK, Park MH, Hyun SS, Kahn SY, Joo KS, et al. In vivo anti-melanogenesis activity and in vitro skin permeability of niacinamide-loaded flexible liposomes (bounsphere™). J Drug Deliv Sci Technol. 2016;31:147-52. https://doi.org/10.1016/j.jddst.2015.12.008

10. Manela-Azulay M, Bagatin E. Cosmeceuticals vitamins. Clin Dermatol. 2009;27(5):469-74. https://doi.org/10.1016/j.clindermatol.2009.05.010

11. Feldmann RJ, Maibach HI. Absorption of some organic compounds through the skin in man. J Invest Dermatol. 1970;54:399-404. https://doi.org/10.1111/1523-1747.ep12259184

12. Boo YC. Mechanistic basis and clinical evidence for the applications of nicotinamide (niacinamide) to control skin aging and pigmentation. Antioxidants. 2021;10:1-24. https://doi.org/10.3390/antiox10081315

13. Kasetvatin C, Rujivipat S, Tiyaboonchai W. Combination of elastic liposomes and low frequency ultrasound for skin permeation enhancement of hyaluronic acid. Colloids Surf B Biointerfaces. 2015;135:458-64. https://doi.org/10.1016/j.colsurfb.2015.07.078

14. Pan-On S, Rujivipat S, Ounaroon A, Kongkaew C, Tiyaboonchai W. Development, characterization and skin irritation of mangosteen peel extract solid dispersion containing clay facial mask. Int J Appl Pharm. 2018;10:202-7. https://doi.org/10.22159/ijap.2018v10i5.28247

15. Pham DT, Chokamonsirikun A, Phattaravorakarn V, Tiyaboonchai W. Polymeric micelles for pulmonary drug delivery: a comprehensive review. J Mater Sci. 2020a;56:2016-36. https://doi.org/10.1007/s10853-020-05361-4

16. Pham DT, Saelim N, Tiyaboonchai W. Paclitaxel loaded EDC-crosslinked fibroin nanoparticles: a potential approach for colon cancer treatment. Drug Deliv Transl Res. 2020b;10:413-24. https://doi.org/10.1007/s13346-019-00682-7

17. Pham DT, Tiyaboonchai W. Fibroin nanoparticles: a promising drug delivery system. Drug Deliv. 2020c;27:431-48. https://doi.org/10.1080/10717544.2020.1736208

18. Akbarzadeh A, Rezaei-Sadabady R, Davaran S, Joo SW, Zarghami N, Hanifehpour Y, et al. Liposome: classification, preparation, and applications. Nanoscale Res Lett. 2013;8:1-9. https://doi.org/10.1186/1556-276X-8-102

19. Hussain A, Singh S, Sharma D, Webster TJ, Shafaat K, Faruk A. Elastic liposomes as novel carriers: recent advances in drug delivery. Int J Nanomed. 2017;12:5087-108. https://doi.org/10.2147/IJN.S138267

20. Benson HA. Elastic liposomes for topical and transdermal drug delivery. Methods Mol Biol. 2010;605:77-86. https://doi.org/10.1007/978-1-60327-360-2_4

21. Iqbal B, Ali J, Baboota S. Recent advances and development in epidermal and dermaldrug deposition enhancement technology. Int Soc Dermatol. 2018;57:646-60. https://doi.org/10.1111/ijd.13902

22. Chen G, Li D, Jin Y, Zhang W, Teng L, Bunt C, et al. Deformable liposomes by reverse-phase evaporation method for an enhanced skin delivery of (+)-catechin. Drug Dev Ind Pharm. 2014;40(2):260-5. https://doi.org/10.3109/03639045.2012.756512

23. El Zaafarany GM, Awad GA, Holayel SM, Mortada ND. Role of edge activators and surface charge in developing ultradeformable vesicles with enhanced skin delivery. Int J Pharm. 2010;397(1-2):164-72. https://doi.org/10.1016/j.ijpharm.2010.06.034

24. Léonard A, Dufourc EJ. Interactions of cholesterol with the membrane lipid matrix. A solid state NMR approach. Biochimie. 1991;73:1295-302. https://doi.org/10.1016/0300-9084(91)90092-F

25. Magarkar A, Dhawan V, Kallinteri P, Viitala T, Elmowafy M, Róg T, et al. Cholesterol level affects surface charge of lipid membranes in saline solution. Sci Rep. 2014;4:1-5. https://doi.org/10.1038/srep05005

26. Moore TL, Rodriguez-Lorenzo L, Hirsch V, Balog S, Urban D, Jud C, et al. Nanoparticle colloidal stability in cell culture media and impact on cellular interactions. Chem Soc Rev. 2015;44:6287-305. https://doi.org/10.1039/C4CS00487F

27. Vicit Rizal ES, Chung I, Misran M. Pegylated oleic acid-lecithin liposomes (poll) for anticancer drug delivery. Sains Malays. 2020;49:19-27. https://doi.org/10.17576/jsm-2020-4901-03

28. Jacobi U, Kaiser M, Toll R, Mangelsdorf S, Audring H, Otberg N, et al. Porcine ear skin: an in vitro model for human skin. Skin Res Technol. 2007;13:19-24. https://doi.org/10.1111/j.1600-0846.2006.00179.x

29. Haque T, Lane ME, Sil BC, Crowther JM, Moore DJ. In vitro permeation and disposition of niacinamidein silicone and porcine skin of skin barrier-mimetic formulations. Int J Pharm. 2017;30:158-62. https://doi.org/10.1016/j.ijpharm.2017.01.054

30. Cevc G. Lipid vesicles and other colloids as drug carriers on the skin. Adv Drug Deliv Rev. 2004;56:675-711. https://doi.org/10.1016/j.addr.2003.10.028

31. van den Bergh BA, Bouwstra JA, Junginger HE, Wertz PW. Elasticity of vesicles affects hairless mouse skin structure and permeability. J Control Release. 1999a;62:367-79. https://doi.org/10.1016/S0168-3659(99)00168-6

32. van den Bergh BA, Vroom J, Gerritsen H, Junginger HE, Bouwstra JA. Interactions of elastic and rigid vesicles with human skin in vitro: electron microscopy and two-photon excitation microscopy. Biochim Biophys Acta. 1999b;1461:155-73. https://doi.org/10.1016/S0005-2736(99)00176-5

33. Verma A, Jain A, Hurkat P, Jain SK. Transfollicular drug delivery: current perspectives. Res Rep Transdermal Drug Deliv. 2016;5:1-17. https://doi.org/10.2147/RRTD.S75809

34. Subongkot T, Wonglertnirant N, Songprakhon P, Rojanarata T, Opanasopit P, Ngawhirunpat T. Visualization of ultradeformable liposomes penetration pathways and their skin interaction by confocal laser scanning microscopy. Int J Pharm. 2013;441:151-61. https://doi.org/10.1016/j.ijpharm.2012.12.003