Ayşe Ünal, Şenay Hamarat Şanlıer

Magnetic Targeted Pemetrexed-Loaded Albumin Nanoparticles and Their Efficacy in Lung Cancer

Introduction

Magnetic targeted pemetrexed-loaded albumin nanoparticles and their efficacy in lung cancer. Discover magnetic albumin nanoparticles delivering pemetrexed for lung cancer. Genipin crosslinking & magnetic targeting enhance stability, enabling site-specific, pH-responsive drug delivery.

Abstract

Objective: Albumin, a biodegradable, biocompatible, and non-toxic plasma protein, is widely used as a nanocarrier in drug delivery systems. Pemetrexed, a potent thymidylate synthase inhibitor for non-small cell lung cancer (NSCLC), is limited by severe systemic side effects. Embedding magnetite within albumin carriers enables external-field guidance (magnetic targeting), which enhances tumor accumulation while reducing off-target exposure. Additionally, employing genipin as a natural, biodegradable, and low-cytotoxicity crosslinker stabilizes the albumin matrix while eliminating the use of toxic aldehyde-based agents.This study introduces a genipin-crosslinked, magnetically targetable albumin nanoparticle platform for enhanced and controlled delivery of pemetrexed to lung cancer cells. Unlike previous pemetrexed–albumin systems, this dual design—combining genipin crosslinking with magnetite-mediated targeting—offers improved structural stability, biocompatibility, and site-specific delivery potential Methods: Bovine serum albumin (BSA) nanoparticles were prepared via desolvation using genipin as the crosslinker and magnetite for magnetic responsiveness. Key formulation parameters—BSA concentration, genipin content, magnetite ratio, reaction time, and drug loading—were systematically optimized. Drug release from free pemetrexed and nanoparticle formulations was evaluated at pH 7.4 and 5.5. Nanoparticles were characterized by SEM, FTIR, and zeta potential; cytotoxic efficacy was assessed in A549-luc-C8 and CRL-5807 lung cancer cells. Results: The nanoparticle yielded spherical, negatively charged nanoparticles with sustained, pH-responsive release. In vitro, the genipin-crosslinked, magnetite-containing nanoparticles demonstrated improved antitumor efficacy versus free drug. Conclusion: Magnetite provides a handle for external magnetic guidance, supporting targeted delivery, while genipin crosslinking minimizes residual crosslinker toxicity and stabilizes the carrier network. Together, genipin crosslinking + magnetic targeting define the novelty and translational potential of this system, with the prospect of reducing systemic exposure via controlled, site-directed delivery.

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