Phytosomes against melanoma: disrupting molecular pathways with targeted phytochemical delivery
Source abstract
Abstract
Melanoma is still the most lethal form of skin cancer causing approximately 56,000 fatalities annually. This cancer is primarily caused by molecular variations in the MAPK, PI3K/AKT, Wnt/β-catenin, p53, and immune signalling pathways. Even though immunotherapies and targeted agents have extended survival, resistance to therapy, toxicity, and limited accessibility still hinder progress worldwide. Various phytoconstituents obtained from natural sources, incorporating flavonoids, terpenoids, alkaloids, and polyphenols, have shown potent antiproliferative, pro-apoptotic, anti-inflammatory, and anti-metastatic effects in melanoma. However, their clinical use is limited by rapid metabolism, minimal systemic stability, poor absorption, and lack of tumor targeting despite attractive preclinical data. A significant improvement in phytochemical delivery in the form of nanoliposomes has emerged, introducing phytosome technology. This technology overcomes the drawbacks by producing stable phospholipid complexes with phytochemicals, thereby enhancing their solubility, bioavailability, membrane-permeability, and pharmacokinetic parameters. This comprehensive study covers the cellular mechanisms of melanoma, the drawbacks of existing therapies, the benefits of nanotechnology-based strategies and the increasing importance of phytosomes as a delivery vehicle for anticancer phytochemicals. It explains the progress in preparation methods, therapeutic effects, preclinical investigations, and the challenges in translating phytosome-based drug delivery for cutaneous melanoma.
Source: openalex_inverted_index · Quality: baseline
Research context
OpenAlex topics: Silymarin and Mushroom Poisoning · Advancements in Transdermal Drug Delivery · Extracellular vesicles in disease
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
References (100+)
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1. Long GV, et al. Cutaneous melanoma. Lancet. 2023;402(10400):485–502.10.1016/S0140-6736(23)00821-8 ↗
2. Naik PP. Cutaneous malignant melanoma: a review of early diagnosis and management. World J Oncol. 2021;12(1):7–19.10.14740/wjon1349 ↗
3. Eggermont AMM, Spatz A, Robert C. Cutaneous melanoma Lancet. 2014;383(9919):816–27.
4. Giblin AV, Thomas JM. Incidence, mortality and survival in cutaneous melanoma. J Plast Reconstr Aesthetic Surg. 2007;60(1):32–40.10.1016/j.bjps.2006.05.008 ↗
5. Lu M, et al. Phyto-phospholipid complexes (phytosomes): a novel strategy to improve the bioavailability of active constituents. Asian J Pharm Sci. 2019;14(3):265–74.
6. Bhardwaj N, et al. New ring-a modified cycloartane triterpenoids from Dysoxylum malabaricum bark: isolation, structure elucidation and their cytotoxicity. Steroids. 2024;205:109390.10.1016/j.steroids.2024.109390 ↗
7. Bhardwaj N et al. Chapter Four - Advances in natural products driven drug discovery from medicinal plants for neuropathic pain. In: Altmann K-H, editor. Annual Reports in Medicinal Chemistry. Academic Press;2023. pp. 133–162.10.1016/bs.armc.2023.10.003 ↗
8. Rajayan JS, et al. In vitro evaluation of extracts from ixora species for a potential phytosomal formulation. Cureus. 2024;16(3):e55396.
9. Barani M, et al. Phytosomes as innovative delivery systems for phytochemicals: a comprehensive review of literature. Int J Nanomed. 2021;16(null):6983–7022.10.2147/IJN.S318416 ↗
10. Flaig TW, et al. A phase I and pharmacokinetic study of silybin-phytosome in prostate cancer patients. Investig New Drugs. 2007;25(2):139–46.10.1007/s10637-006-9019-2 ↗
11. Cheng Y, Zhang G, Li G. Targeting MAPK pathway in melanoma therapy. Cancer Metastasis Rev. 2013;32(3):567–84.10.1007/s10555-013-9433-9 ↗
12. Toma L, et al. Bioactive compounds formulated in phytosomes administered as complementary therapy for metabolic disorders. Int J Mol Sci. 2024;25(8):4162.10.3390/ijms25084162 ↗
13. Gaikwad SS et al. Overview of phytosomes in treating cancer: advancement, challenges, and future outlook. Heliyon. 2023;9(6):112–116.10.1016/j.heliyon.2023.e16561 ↗
14. Mahale J. Preclinical evaluation of Meriva (a formulation of curcumin) as a putative agent for chemoprevention of lung cancer. University of Leicester; 2016.
15. Epelbaum R, et al. Curcumin and gemcitabine in patients with advanced pancreatic cancer. Nutr Cancer. 2010;62(8):1137–41.10.1080/01635581.2010.513802 ↗
16. Pastorelli D, et al. Phytosome complex of curcumin as complementary therapy of advanced pancreatic cancer improves safety and efficacy of gemcitabine: Results of a prospective phase II trial. Pharmacol Res. 2018;132:72–9.10.1016/j.phrs.2018.03.013 ↗
17. Guo W, Wang H, Li C. Signal pathways of melanoma and targeted therapy. Signal Transduct Target Therapy. 2021;6(1):424.10.1038/s41392-021-00827-6 ↗
18. Haluska FG, et al. Genetic alterations in signaling pathways in melanoma. Clin Cancer Res. 2006;12(7):s2301–7.10.1158/1078-0432.CCR-05-2518 ↗
19. Bhardwaj N, et al. Anticancer activity of diosgenin and its semi-synthetic derivatives: role in autophagy mediated cell death and induction of apoptosis. Mini Rev Med Chem. 2021;21(13):1646–65.10.2174/1389557521666210105111224 ↗
20. Lopez-Bergami P, Fitchman B, Ronai Ze. Understanding signaling cascades in melanoma. Photochem Photobiol. 2008;84(2):289–306.10.1111/j.1751-1097.2007.00254.x ↗
21. Wu H, Goel V, Haluska FG. PTEN signaling pathways in melanoma. Oncogene. 2003;22(20):3113–22.10.1038/sj.onc.1206451 ↗
22. Madhunapantula SV, Mosca PJ, Robertson GP. The Akt signaling pathway. Cancer Biol Ther. 2011;12(12):1032–49.10.4161/cbt.12.12.18442 ↗
23. Lopez-Bergami P, et al. Rewired ERK-JNK signaling pathways in melanoma. Cancer Cell. 2007;11(5):447–60.10.1016/j.ccr.2007.03.009 ↗
24. Dhawan P, Richmond A. A novel NF-κB-inducing Kinase-MAPK signaling pathway up-regulates NF-κB activity in melanoma cells. J Biol Chem. 2002;277(10):7920–8.10.1074/jbc.M112210200 ↗
25. Fishman P, et al. Evidence for involvement of Wnt signaling pathway in IB-MECA mediated suppression of melanoma cells. Oncogene. 2002;21(25):4060–4.10.1038/sj.onc.1205531 ↗
26. Xue G, et al. Wnt/β-catenin signaling in melanoma: Preclinical rationale and novel therapeutic insights. Cancer Treat Rev. 2016;49:1–12.10.1016/j.ctrv.2016.06.009 ↗
27. Kaur A, Webster MR, Weeraratna AT. In the Wnt-er of life: Wnt signalling in melanoma and ageing. Br J Cancer. 2016;115(11):1273–9.10.1038/bjc.2016.332 ↗
28. Meier F, et al. The RAS/RAF/MEK/ERK and PI3K/AKT signaling pathways present molecular targets for the effective treatment of advanced melanoma. Front Biosci. 2005;10(2986–3001):2986–3001.10.2741/1755 ↗
29. Shain AH, et al. Genomic and transcriptomic analysis reveals incremental disruption of key signaling pathways during melanoma evolution. Cancer Cell. 2018;34(1):45–e554.10.1016/j.ccell.2018.06.005 ↗
30. Pappalardo F, et al. Computational modeling of PI3K/AKT and MAPK signaling pathways in melanoma cancer. PLoS ONE. 2016;11(3):e0152104.10.1371/journal.pone.0152104 ↗
31. Cunha C, Daniel-da-Silva AL, Oliveira H. Drug delivery systems and flavonoids: current knowledge in melanoma treatment and future perspectives. Micromachines. 2022;13(11):1838.10.3390/mi13111838 ↗
32. Bhardwaj N, et al. A comprehensive review on chemistry and pharmacology of marine bioactives as antimetastatic agents. Eur J Med Chem Rep. 2022;4:100023.
33. Smalley KSM, et al. Multiple signaling pathways must be targeted to overcome drug resistance in cell lines derived from melanoma metastases. Mol Cancer Ther. 2006;5(5):1136–44.10.1158/1535-7163.MCT-06-0084 ↗
34. Hussein MR, Haemel AK, Wood GS. p53-related pathways and the molecular pathogenesis of melanoma. Eur J Cancer Prev. 2003;12(2):93–100.10.1097/00008469-200304000-00002 ↗
35. Box NF, Terzian T. The role of p53 in pigmentation, tanning and melanoma. Pigment Cell Melanoma Res. 2008;21(5):525–33.10.1111/j.1755-148X.2008.00495.x ↗
36. Paluncic J et al. Melanotransferrin Functions as a Pro-Oncogenic WNT Agonist: A Yin-Yang Relationship in Melanoma with the WNT Antagonist and Metastasis Suppressor, NDRG1. bioRxiv, 2023: p. 2023.02.27.530353.10.1101/2023.02.27.530353 ↗
37. Paluncic J, et al. Roads to melanoma: Key pathways and emerging players in melanoma progression and oncogenic signaling. Biochim et Biophys Acta (BBA) - Mol Cell Res. 2016;1863(4):770–84.10.1016/j.bbamcr.2016.01.025 ↗
38. Rosero RA, Villares GJ, Bar-Eli M. Protease-activated receptors and other g-protein-coupled receptors: the melanoma connection. Front Genet. 2016;7:112.10.3389/fgene.2016.00112 ↗
39. Stachyra-Strawa P, et al. The role of immunotherapy and molecular-targeted therapy in the treatment of melanoma. Oncol Rep. 2021;46(2):158.10.3892/or.2021.8109 ↗
40. Imani S, et al. The evolution of BRAF-targeted therapies in melanoma: overcoming hurdles and unleashing novel strategies. Front Oncol. 2024;14:1504142.10.3389/fonc.2024.1504142 ↗
41. Tang J-Q, et al. Recent developments in nanomedicine for melanoma treatment. Int J Cancer. 2017;141(4):646–53.10.1002/ijc.30708 ↗
42. Ouyang B, et al. The dose threshold for nanoparticle tumour delivery. Nat Mater. 2020;19(12):1362–71.10.1038/s41563-020-0755-z ↗
43. Wang J, et al. Nanocarrier-mediated immunogenic cell death for melanoma treatment. Int J Nanomed. 2023;18(null):7149–72.10.2147/IJN.S434582 ↗
44. Bei D, Meng J, Youan B-BC. Engineering Nanomedicines for Improved Melanoma Therapy: Progress and Promises. Nanomedicine. 2010;5(9):1385–99.10.2217/nnm.10.117 ↗
45. Telange DR, et al. Formulation and characterization of an apigenin-phospholipid phytosome (APLC) for improved solubility, in vivo bioavailability, and antioxidant potential. Eur J Pharm Sci. 2017;108:36–49.10.1016/j.ejps.2016.12.009 ↗
46. Zeng H, et al. Melanoma and nanotechnology-based treatment. Front Oncol. 2022;12:858185.10.3389/fonc.2022.858185 ↗
47. Mishra H, et al. Melanoma treatment: from conventional to nanotechnology. J Cancer Res Clin Oncol. 2018;144(12):2283–302.10.1007/s00432-018-2726-1 ↗
48. Peltek OO, et al. Development of nanocarrier-based radionuclide and photothermal therapy in combination with chemotherapy in melanoma cancer treatment. ACS Appl Mater Interfaces. 2023;15(10):13460–71.10.1021/acsami.2c20619 ↗
49. Paleos CM, et al. Drug delivery using multifunctional dendrimers and hyperbranched polymers. Expert Opin Drug Deliv. 2010;7(12):1387–98.10.1517/17425247.2010.534981 ↗
50. Rai S, Pandey V, Rai G. Transfersomes as versatile and flexible nano-vesicular carriers in skin cancer therapy: the state of the art. Nano Reviews Experiments. 2017;8(1):1325708.10.1080/20022727.2017.1325708 ↗
51. Song M, et al. Self-assembled polymeric nanocarrier-mediated co-delivery of metformin and doxorubicin for melanoma therapy. Drug Delivery. 2021;28(1):594–606.10.1080/10717544.2021.1898703 ↗
52. Bombelli FB, et al. The scope of nanoparticle therapies for future metastatic melanoma treatment. Lancet Oncol. 2014;15(1):e22–32.10.1016/S1470-2045(13)70333-4 ↗
53. Park KS. Pharmacological effects of centella asiatica on skin diseases: evidence and possible mechanisms. Evidence-Based Complement Altern Med. 2021;2021(1):5462633.
54. Jha A, et al. Biopolymer-based tumor microenvironment-responsive nanomedicine for targeted cancer therapy. Nanomedicine. 2024;19(7):633–51.10.2217/nnm-2023-0302 ↗
55. Jha A, et al. Hyaluronic acid-oleylamine and chitosan-oleic acid conjugate-based hybrid nanoparticle delivery via. dissolving microneedles for enhanced treatment efficacy in localized breast cancer. Biomaterials Adv. 2024;160:213865.10.1016/j.bioadv.2024.213865 ↗
56. Kumar M, et al. Fabrication of lipid-modified drug nanocrystals loaded injectable hydrogel for breast cancer therapy. Discover Nano. 2025;20(1):30.10.1186/s11671-025-04195-w ↗
57. Jha A, et al. Chap. 17 - Glycerosomes: a new tool for effective drug delivery. In: Nayak AK, et al. editors. Systems of Nanovesicular Drug Delivery. Academic; 2022. pp. 277–91.10.1016/B978-0-323-91864-0.00010-3 ↗
58. Kumar M, Jha A, Mishra B. Marine Biopolymers for Transdermal Drug Delivery. Marine Biomaterials: Drug Delivery and Therapeutic Applications. Nature Singapore: Singapore: Springer; 2022. pp. 157–207. S. Jana and S. Jana, Editors.10.1007/978-981-16-4787-1_6 ↗
59. Jha A, Kumar M, Mishra B. Marine Biopolymer-Based Anticancer Drug Delivery Systems. Marine Biomaterials: Drug Delivery and Therapeutic Applications. Nature Singapore: Singapore: Springer; 2022. pp. 351–401. S. Jana and S. Jana, Editors.10.1007/978-981-16-4787-1_11 ↗
60. Yu F, et al. Monodisperse microparticles loaded with the self-assembled berberine-phospholipid complex-based phytosomes for improving oral bioavailability and enhancing hypoglycemic efficiency. Eur J Pharm Biopharm. 2016;103:136–48.10.1016/j.ejpb.2016.03.019 ↗
61. Riva A, et al. A novel boswellic acids delivery form (casperome (R)) in the management of musculoskeletal disorders: a review. Eur Rev Med Pharmacol Sci. 2017;21:5258–63.
62. Drobnic F, et al. Reduction of delayed onset muscle soreness by a novel curcumin delivery system (Meriva®): a randomised, placebo-controlled trial. J Int Soc Sports Nutr. 2014;11(1):31.10.1186/1550-2783-11-31 ↗
63. Gilardini L, et al. Effects of Greenselect Phytosome® on weight maintenance after weight loss in obese women: a randomized placebo-controlled study. BMC Complement Altern Med. 2016;16(1):233.10.1186/s12906-016-1214-x ↗
64. Di Pierro F, et al. GreenSelect (R) phytosome as an adjunct to a low-calorie diet for treatment of obesity: a clinical trial. Altern Med Rev. 2009;14(2):154.
65. Amit Gupta AG, Swarnlata Saraf SS, Saraf S. Phytosome: a novel approach for phytoconstituents. Plant archives. 2007;7(2):457–61.
66. Vigna GB, et al. Effect of a standardized grape seed extract on low-density lipoprotein susceptibility to oxidation in heavy smokers. Metabolism. 2003;52(10):1250–7.10.1016/S0026-0495(03)00192-6 ↗
67. Barani M et al. Phytosomes as innovative delivery systems for phytochemicals: a comprehensive review of literature. Int J Nanomed, 2021;12:6983–7022.10.2147/IJN.S318416 ↗
68. Yu Z, et al. Naringenin-loaded dipalmitoylphosphatidylcholine phytosome dry powders for inhaled treatment of acute lung injury. J aerosol Med pulmonary drug delivery. 2020;33(4):194–204.10.1089/jamp.2019.1569 ↗
69. Cesarone MR, et al. Supplementary prevention and management of asthma with quercetin phytosome: a pilot registry. Minerva Med. 2019;110(6):524–9.
70. Kidd P, Head K. A review of the bioavailability and clinical efficacy of milk thistle phytosome: a silybin-phosphatidylcholine complex (Siliphos). Altern Med Rev. 2005;10(3):2178-2180.
71. Petrangolini G, et al. A new food-grade coenzyme Q10 formulation improves bioavailability: Single and repeated pharmacokinetic studies in healthy volunteers. Curr Drug Deliv. 2019;16(8):759–67.10.2174/1567201816666190902123147 ↗
72. Riva A et al. Healthy Protection of Bergamot is linked to the Modulation of Microbiota. 2020.10.21203/rs.3.rs-25708/v1 ↗
73. Mollace V, et al. Hypoglycemic and hypolipemic effects of a new lecithin formulation of bergamot polyphenolic fraction: A double blind, randomized, placebo-controlled study. Endocrine, Metabolic & Immune Disorders-Drug Targets (Formerly Current Drug Targets-Immune. Endocr Metabolic Disorders). 2019;19(2):136–43.
74. Naik SR, Pilgaonkar VW, Panda VS. Evaluation of antioxidant activity of Ginkgo biloba phytosomes in rat brain. Phytotherapy Research: Int J Devoted Pharmacol Toxicol Evaluation Nat Prod Derivatives. 2006;20(11):1013–6.10.1002/ptr.1976 ↗
75. Barani M, et al. Phytosomes as innovative delivery systems for phytochemicals: a comprehensive review of literature. Int J Nanomed. 2021;16:6983–7022.10.2147/IJN.S318416 ↗
76. Demir B, et al. Gold nanoparticle loaded phytosomal systems: synthesis, characterization and in vitro investigations. RSC Adv. 2014;4(65):34687–95.10.1039/C4RA05108D ↗
77. Teja PK, et al. Herbal nanomedicines: recent advancements, challenges, opportunities and regulatory overview. Phytomedicine. 2022;96:153890.10.1016/j.phymed.2021.153890 ↗
78. Agarwal A, et al. Formulation and Characterization of Phytosomes as Drug Delivery System of Formononetin: An Effective Anti-Osteoporotic Agent. Curr Drug Deliv. 2024;21(2):261–70.10.2174/1567201820666230124114906 ↗
79. Vu HT, et al. Are phytosomes a superior nanodelivery system for the antioxidant rutin? Int J Pharm. 2018;548(1):82–91.10.1016/j.ijpharm.2018.06.042 ↗
80. Rani A, Kumar S, Khar RK. Murraya koenigii extract loaded phytosomes prepared using antisolvent precipitation technique for improved antidiabetic and hypolidemic activity. Indian J Pharm Educ Res. 2022;56:s326–38.10.5530/ijper.56.2s.103 ↗
81. Karole S, Gupta G. Preparation and evaluation of phytosomes containing ethanolic extract of leaves of Bombax ceiba for hepatoprotective activity. Evaluation. 2019;6(2):15.
82. Dewi MK, et al. Fabrication of Phytosome with Enhanced Activity of Sonneratia alba: Formulation Modeling and in vivo Antimalarial Study. Int J Nanomed. 2024;19(null):9411–35.10.2147/IJN.S467811 ↗
83. Freag MS, Elnaggar YSR, Abdallah OY. Lyophilized phytosomal nanocarriers as platforms for enhanced diosmin delivery: optimization and ex vivo permeation. Int J Nanomed. 2013;8(null):2385–97.
84. Mancini S, et al. Functionalized liposomes and phytosomes loading Annona muricata L. aqueous extract: Potential nanoshuttles for brain-delivery of phenolic compounds. Phytomedicine. 2018;42:233–44.10.1016/j.phymed.2018.03.053 ↗
85. Freag MS, Saleh WM, Abdallah OY. Self-assembled phospholipid-based phytosomal nanocarriers as promising platforms for improving oral bioavailability of the anticancer celastrol. Int J Pharm. 2018;535(1):18–26.10.1016/j.ijpharm.2017.10.053 ↗
86. Sahin OI, et al. Lyophilized nano-liposomal system for red onion (Allium cepa L.) peel anthocyanin: Characterization, bioaccessibility and release kinetics. Food Bioscience. 2023;53:102702.10.1016/j.fbio.2023.102702 ↗
87. Mardiyanti S, et al. Novel Enhalus acoroides Phytosomes: Formulation, Characterization, and Bioavailability Enhancement. Bioscientia Medicina: J Biomed Translational Res. 2025;9(7):8019–32.
88. Mazumder A, et al. In vitro wound healing and cytotoxic effects of sinigrin–phytosome complex. Int J Pharm. 2016;498(1):283–93.10.1016/j.ijpharm.2015.12.027 ↗
89. Mazumder A, et al. In vitro skin permeation of sinigrin from its phytosome complex. J Pharm Pharmacol. 2016;68(12):1577–83.10.1111/jphp.12594 ↗
90. Ju Ho P, et al. Anti-inflammatory effect of Centella asiatica phytosome in a mouse model of phthalic anhydride-induced atopic dermatitis. Phytomedicine. 2018;43:110–9.10.1016/j.phymed.2018.04.013 ↗
91. Hendawy OM, et al. Development of Olive Oil Containing Phytosomal Nanocomplex for Improving Skin Delivery of Quercetin: Formulation Design Optimization, In Vitro and Ex Vivo Appraisals. Pharmaceutics. 2023;15(4):1124–p.10.3390/pharmaceutics15041124 ↗
92. Vaghela HN, et al. Formulation of phytosomes with sun protection factor using Agave americana ethanolic extract. J Biologically Act Prod Nat. 2024;14(2):238–50.
93. Nair RS, et al. Characterization and ex vivo evaluation of curcumin nanoethosomes for melanoma treatment. Pharm Dev Technol. 2022;27(1):72–82.10.1080/10837450.2021.2023568 ↗
94. Patidar M, et al. Formulation and evaluation of face serum containing phytosome of gingerol oil, Carica papaya pulp extract, and aloe vera gel. World J Pharm Res. 2023;12:726–40.
95. Shukla S, Mhaske A, Shukla R. Nanocarriers for the Delivery of Cosmeceuticals. Nanotechnology Based Delivery of Phytoconstituents and Cosmeceuticals. Nature Singapore: Singapore: Springer; 2024. pp. 305–28. D. Pooja and H. Kulhari, Editors.10.1007/978-981-99-5314-1_10 ↗
96. Jahangir MA, et al. Theranostic Applications of Functionalized Vesicular Carriers. Multifunctional And Targeted Theranostic Nanomedicines: Formulation, Design And Applications. Nature Singapore: Singapore: Springer; 2023. pp. 49–76. K. Jain and N.K. Jain, Editors.10.1007/978-981-99-0538-6_3 ↗
97. Al-Samydai A, et al. Meta-analysis of nano-phytosomes: unleashing the potential of plant-derived compounds for advancing cancer therapy. Nat Prod Res. 2025;39(16):4623–42.10.1080/14786419.2024.2344182 ↗
98. Ahmad R, et al. Phytochemical delivery through nanocarriers: a review. Colloids Surf B. 2021;197:111389.10.1016/j.colsurfb.2020.111389 ↗
99. Semalty A, et al. Supramolecular phospholipids-polyphenolics interactions: The PHYTOSOME (R) strategy to improve the bioavailability of phytochemicals. Fitoterapia. 2010;81(5):306–14.10.1016/j.fitote.2009.11.001 ↗
100. Wongkaewkhiaw S, et al. Induction of apoptosis in human colorectal cancer cells by nanovesicles from fingerroot (Boesenbergia rotunda (L.) Mansf). PLoS ONE. 2022;17(4):e0266044.10.1371/journal.pone.0266044 ↗