A Comprehensive Study on Folate-Targeted Mesoporous Silica Nanoparticles Loaded with 5-Fluorouracil for the Enhanced Treatment of Gynecological Cancers.

BACKGROUND

Gynecological cancers are a significant public health concern, accounting for 40% of all cancer incidence and 30% of deaths in women. 5-Fluorouracil (5-FU) can be used with chemotherapy to improve treatment in advanced-stage gynecological cancer. Mesoporous silica nanoparticles (MSNs) can improve drug effectiveness and reduce toxicity. Folic acid can target folate receptors in epithelial malignancies like ovarian and cervical cancer.

METHODS

The mixture of MSN-NH2 was synthesized by dissolving N-lauroylsarcosine sodium in a water-ethanol mixture, adding APTES and TEOS, and heating at 80 °C for 18 h, before being fully characterized. The drug is loaded into a 5-FU solution and functionalized with folate. The drug release mechanism, as well as ex vivo intestinal permeation from MSN-NH2 formulations, was tested. The cell viability study of the nanoparticles was evaluated in various cancer cell lines, and the cellular uptake was measured indirectly using HPLC.

RESULTS

The study analyzed the amine content, propylamine loading, and drug loading capacity of MSN-NH2 nanoparticles. It found that the loading of propylamine was around 0.733 mmol/g, and the surface density was 0.81 molecules/nm. The study also showed that the surface decoration of MSN-NH2 with folic acid was successfully achieved. The release rate of 5-FU from MSN-NH2 was slow and controlled, with a slower rate at pH 5.5. The study found that the amin surface functionalization of MSN-NH2 nanoparticles can reduce potential toxicity in ovarian and cervical cancer cells.

CONCLUSIONS

Based on the results, the encapsulation of 5-FU and functionalization of MSN-NH2 with folic acid can serve as potential carriers for 5-FU in treating gynecological cancer.