Development and in vitro evaluation of folate conjugated polydopamine modified carmustine-loaded liposomes for improved anticancer activity

Surface-modified, targeted nanocarriers play important roles in chemotherapy. The addition of the ligand changes the chemical composition of the polymer; the ability to hold and encapsulate the drug may be lost during polymer modification. Polydopamine (PDA) has been an innovative, biocompatible, and adaptable approach for creating targeted nanoparticles that can be used as a platform for conjugating tailored ligands to polymer carriers that do not contain reactive chemical groups. Therefore, the current study aimed to explore the efficacy of PDA-modified folic acid (FA)-conjugated targeted delivery of carmustine (BCNU)-loaded liposomes for augmenting cancer therapy. Plain BCNU, FA-BCNU, and FA-PDA-BCNU liposomes were developed for a comparative investigation. The UV, FTIR, XPS, and TEM analyses confirm the formation of PDA coating and FA-PDA conjugation. FA-PDA-BCNU liposomes had a smaller particle size, and presented good stability, spherical morphology, and high cellular uptake comparative to conventional liposomes. The cytotoxicity of FA-BCNU and FA-PDA-BCNU liposomes on Human Glioblastoma Cell lines (U87MG) was also considerably higher than that of BCNU liposomes and pure BCNU solution at each concentration while significantly less cytotoxicity to normal cells (L929), proving its excellent biocompatibility. While only FA-PDA-BCNU liposomes showed pH-sensitive properties, which were attributed to the PDA layers; they can control the drug release better following the Higuchi matrix release model. From the present investigation, it has been revealed that the FA-PDA-BCNU liposomes can reduce the harm caused to normal tissues and improve liposomes' effectiveness in combating tumors, which is promising in the future. [Display omitted]