Folate receptor targeted NIR cleavable liposomal delivery system augment penetration and therapeutic efficacy in breast cancer

• Published in: Biochimica et biophysica acta. General subjects Vol. 1867; no. 9; p. 130396
• Main Authors: Dinakar, Yirivinti Hayagreeva, Karole, Archana, Parvez, Shabi, Jain, Vikas, Mudavath, Shyam Lal
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.09.2023
• Subjects: antineoplastic activity; apoptosis; Breast cancer; breast neoplasms; caspase-3; cell lines; cell movement; drugs; folate receptors; folic acid; ligands; Liposomes; Luteolin; nanocarriers; Near infrared irradiation; neoplasm cells; Receptor mediated drug delivery; Breast cancer; Luteolin; Liposomes; Near infrared irradiation; Receptor mediated drug delivery
• ISSN: 0304-4165; 1872-8006; 1872-8006
• DOI: 10.1016/j.bbagen.2023.130396

Liposomes are predominantly used sorts of nanocarriers for active a targeted delivery through surface functionalization using targeting ligand. The folate receptors are overexpressed in various cancers including breast cancer and because of its binding aptitude specifically to folate receptors, folic acid became the attractive ligand. In this research, we have developed a folate and Poly-l-Lysine conjugate and coated this conjugate onto the liposomes. The prepared liposomes were characterized using DLS, FTIR, NMR, SEM, TEM, XRD, AFM, stability and drug release studies. Furthermore, in vitro studies were carried out on FR overexpressed breast cancer cell line. The FA-LUT-ABC-Lip have diameter of 183 ± 3.17 nm with positive surface charge +33.65 ± 3 mV and the drug release studies confirm the NIR responsive payload cleavage. The coated formulation (in presence of NIR light) effectively reduced the IC50 values and kills breast cancer cells through FR mediated internalization and accelerated drug release. Moreover, LUT Formulation shows anticancer effect due to significant inhibition of cell migration and proliferation by regulating VEGF expression and induced apoptosis through the caspase-3 up-regulation. It is evident from the in vitro studies that the formulation was found to be very effective and can be explored for triggered and targeted delivery of the substances through active targeting. Combining receptor mediated drug delivery with triggered release aid in more amounts of drug reaching the target site and achieving enhanced therapeutic activity. [Display omitted] •The folate coated liposomes were developed for the targeted drug delivery through folate receptor mediated endocytosis.•The triggered release of LUT was achieved upon NIR irradiation following the uptake.•The targeted liposomes exerted effect on apoptosis, angiogenesis, cell migration etc.•The significant effect on FR+ breast cancer cells is attributed to augmented uptake with site-specific drug releasing.