Folic Acid Functionalized Dasatinib Solid Lipid Nanoparticles as an Advantageous Drug Delivery System: Optimization, Characterization, and In-Vitro Assessment

Introduction: Functionalizing folic acid with a surfactant can enhance drug concentration at cancer sites by forming an outer layer on solid lipid nanoparticles. The formulation development and optimization employed Response Surface Methodology (RSM) based on a Central Composite Design, enabling quantitative evaluation of the effects of independent variables and their interactions on the response parameters. Methods: Poloxamer P 188 was conjugated with folic acid using 1,1-carbonyldimidazole. Folic Acid-Dasatinib Solid Lipid Nanoparticles (FA-DAS-SLN) were prepared using the hot homogenization and sonication method. The formulation was optimized through a central composite design, and the process was optimized using the OFAT approach. Evaluation criteria included particle size, PDI, % entrapment efficiency, surface morphology, and in-vitro drug release studied at pH 5.5 and 7.4. Results & Discussion: Functionalization of folic acid with Poloxamer P 188 was confirmed by FTIR, and the optimized formulation achieved 83.38 ± 0.14% entrapment efficiency, a particle size of 12.06 ± 2.24 nm, and sustained in-vitro release over 72 hours. Greater drug release at pH 5.5 than at pH 7.4 indicates tumor-targeting potential, with folic acid facilitating targeting of breast cancer cells. SEM imaging revealed that the freeze-dried optimized lipidic carriers had a spherical shape. Conclusion: This study demonstrated that folic acid functionalization enhances drug release at Triple-Negative Breast Cancer (TNBC) sites, while optimization using a central composite design identified statistically significant interactions between independent and dependent variables for FA-DAS-SLN.