What question did this study set out to answer?

The aim is to enhance the efficacy of melatonin as an anti-cancer agent through targeted delivery using niosome nanoparticles.

June 20, 2026Advanced Pharmaceutical Bulletin0 citationsOpen Access

Design, Characterization, and In-Vitro Targeted Delivery of Melatonin via pH-Responsive Niosome Nanoparticles Decorated with Folate Against Colon Cancer Cells

DJDavoud Jafari-GharabaghlouTabriz University of Medical Sciences UAUrjwan AlaliBaqiyatallah University of Medical Sciences FAFadhil Jawad Al-Tu’maAlsalam University College

Key Points

The aim is to enhance the efficacy of melatonin as an anti-cancer agent through targeted delivery using niosome nanoparticles.
Synthesized niosomal nanoparticles decorated with folic acid using thin film hydration method.
Characterized nanoparticles through AFM, SEM, DLS, and FT-IR techniques.
Assessed cytotoxic effects with MTT and gene expression changes using real-time PCR.
Melatonin-loaded folic acid-decorated nanoparticles demonstrated a size of 239.9 ± 39.64 nm and released approximately 73% of melatonin at pH 5.
Increased cytotoxicity observed with folic acid-decorated niosomes compared to pure melatonin and standard niosomal formulation.
Enhanced apoptosis and cell cycle arrest induced by melatonin-loaded folic acid-decorated niosomes versus other treatments.

Abstract

Purpose: Utilizing targeted drug delivery in oncology represents a valuable strategy to enhance the therapeutic efficacy of chemotherapy and simultaneously mitigate its adverse effects. Our present investigation focused on harnessing the therapeutic properties of melatonin as an anti-cancer agent and improving its bioavailability by employing a drug delivery system based on folic acid-decorated niosomal nanoparticles. Methods: To deliver melatonin, a niosomal and a folic acid decorated niosomal system was used. Nanoparticles were synthesized with the thin film hydration method and characterized by AFM, SEM, DLS, and FT-IR techniques. The cytotoxic effects and changes in gene expression were assessed using MTT and real-time PCR techniques, respectively. Additionally, flow cytometry experiments were conducted to investigate their impact on cell cycle arrest and apoptosis induction. Results: Nanoparticle analysis revealed that the size distribution of blank niosomes, melatonin-loaded niosomal nanoparticles, and melatonin-loaded folic acid-decorated niosomal nanoparticles were 157 ± 8.96 nm, 198 ± 12.34 nm, and 239.9 ± 39.64 nm, respectively. Controlled release studies indicated that over 96 hours, the maximum amount of melatonin released was approximately 60% at pH 7.4 and 73% at pH 5. The results demonstrated enhanced cell cytotoxicity of melatonin when encapsulated in melatonin-loaded folic acid-decorated niosomal compared to pure melatonin and niosomal nanoparticles. Furthermore, melatonin-loaded folic acid-decorated niosomal nanoparticles exhibited superior outcomes in terms of promoting apoptosis and cell cycle arrest compared to other tested substances. Conclusion: Overall, melatonin-loaded folic acid-decorated niosomal nanoparticles demonstrate a significant capability as an effective therapeutic strategy for targeting colorectal cancer cells.

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