Synthesis, Characterization, and In-Vitro Evaluation of Silibinin-loaded PEGylated Niosomal Nanoparticles: Potential Anti-Cancer Effects on SW480 Colon Cancer Cells.

OBJECTIVE: Colorectal cancer is a significant global health concern with high mortality rates. Silibinin is a compound derived from milk thistle with anticancer properties and may be a potential treatment option for colorectal cancer. Its poor solubility limits its clinical application, but various strategies, such as nanoparticle encapsulation, have shown promise. In this study, a PEGylated niosomal drug delivery system was used to enhance the solubility of silibinin, and its anti-proliferative effects were evaluated against human colorectal cancer cell lines.

METHODS: The silibinin-loaded PEGylated niosomal nanoparticles (NIO-SIL) were fabricated using the thin-film hydration method and characterized with dialysis bag, AFM, SEM, DLS, and FTIR systems. Finally, the cancerous cells and human normal cells were treated with NIO-SIL and pure silibinin. The proliferation, apoptosis, and cell cycle of these cells were evaluated. Subsequently, the expression of Bax, Bcl-2, p53, and cyclin D1 genes was measured using real-time PCR.

RESULT: The drug release profile, size, morphology, and chemical interactions of the synthesized PEGylated niosomal nanoparticles were suitable for use as a drug delivery system. Both pure silibinin and NIO-SIL could reduce the proliferation of cancerous cells, induce apoptosis, and cause cell cycle arrest, with no significant negative effects reported on human normal cells. Both pure silibinin and NIO-SIL reduced the expression of the Bcl-2 and cyclin D1 genes while increasing the expression of Bax and p53. (p-value < 0.05 *).

CONCLUSION: The outcomes of this study indicate the high potential of PEGylated niosomal nanoparticles for encapsulation and delivery of silibinin to cancer cells, with no negative effects on normal cells.