Abstract

Introduction: To address the issues of liposomal instability and enhance the delivery of docetaxel (DTX) to breast cancer cells, the development of polyethylene glycol (PEG)-coated proliposomes was proposed, utilizing a thin film hydration technique followed by lyophilization with an appropriate cryoprotectant. Various compositions of phospholipid, cholesterol, and docetaxel were optimized, and the PEG was used in a 1.3:1 ratio of the phospholipid.

Methods: The liposomes were converted to proliposomes using a lyophilizer. The optimized formulation possesses a particle size of 117.0 ± 9.78 nm, with a polydispersity index (PDI) of 0.265 ± 0.094, drug entrapment (DE) of 96.0± 6.14 %, and drug loading (DL) of 9.20 ± 3.17 %. In-vitro study demonstrated a controlled release pattern consistent with the Higuchi model, alongside significantly lower protein binding relative to free DTX, indicating a potential reduction in side effects.

Results: Cell viability study demonstrated increased cytotoxicity of PEG-DTX proliposomes (PEGDTX PL) against MDA-MB-231 cells, evidenced by a lower IC₅₀ (4.677 μg/mL) relative to free DTX, underscoring the promise of this nanocarrier for targeted therapy.

Conclusion: The findings are promising as a simple and scalable carrier comprising general and biocompatible materials that can provide a safe surfactant free nanosystem with improved efficacy and performance.

Keywords: Docetaxel, anticancer agents, biocompatible, drug delivery, protein binding, controlled release.