Microfluidic Preparation and Optimization of Biotin Modified Pegylated Liposomes for Targeted Delivery of Cisplatin Publisher



Malakouti A ; Motedayen M ; Vaziri M ; Al Tamimi JHZ ; Akrami M
Source: Journal of Drug Delivery Science and Technology Published:2026

Abstract

Conventional chemotherapy with Cisplatin (Cis) is widely used for treating breast cancer but is severely limited by poor tumor selectivity, systemic toxicity, and rapid drug clearance, which reduce its therapeutic efficacy. These challenges underscore the need for advanced drug delivery systems capable of enhancing tumor-specific accumulation while minimizing off-target effects. In this study, we developed a microfluidic platform to fabricate Cis-loaded biotin-modified PEGylated liposomes (Cis-BPLip), designed to improve drug encapsulation, targeted delivery, and controlled drug release. Key synthesis process parameters, including cholesterol content, flow rate ratio (FRR), and total flow rate (TFR), were optimized using Response Surface Methodology (RSM). The optimized nanoparticles (NPs) exhibited a mean size of 101.1 ± 2.4 nm, a high encapsulation efficiency (EE) of 79.1 ± 0.9%, with a controlled drug release profile. In-vitro cytotoxicity studies on MCF-7 breast cancer cells confirmed significantly enhanced anti-tumor activity of Cis-BPLip compared to free Cis and non-targeted liposomes, attributed to improved uptake via biotin-mediated active targeting. Moreover, the formulation remained physically stable for 60 days at 4 °C. These findings support the use of microfluidically engineered, actively targeted liposomes as a promising strategy to overcome the limitations of conventional Cis therapy. Copyright © 2026. Published by Elsevier B.V.