Romanian Society of Pharmaceutical Sciences

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VINORELBINE-LOADED pH-SENSITIVE LIPOSOMES: DEVELOPMENT, CHARACTERIZATION AND IN VITRO EVALUATION

IOANA TOMA 1, LAJOS RADULY 2, ALINA PORFIRE 1*, LUCIA RUXANDRA TEFAS 1, OANA ZANOAGA 2, IOANA BERINDAN-NEAGOE 2, IOAN TOMUȚĂ 1

1 Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 41 Victor Babeș Street, 400012, Cluj-Napoca, Romania
2 Research Centre for Functional Genomics, Biomedicine and Translational Medicine, University of Medicine and Pharmacy “Iuliu Hațieganu”, 23 Gheorghe Marinescu Street, 400337, Cluj-Napoca, Romania

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Vinorelbine (NVB) is an anti‑mitotic drug used to treat multiple types of cancers, demonstrating a high antitumor activity and low neurotoxicity. The pH-sensitive liposomes (PSL) undergo destabilization of the vesicular membranes in the acidic environment of tumours which triggers the release of active substance at the tumour site. The aim of this study was to design and evaluate the NVB-PSL formulations in non-small cell lung cancer (NSCLC) cell lines regarding their anti-tumour effect. The liposomes were obtained using the thin lipid film hydration method. An optimization study was performed using the Design of Experiments (DoE) methodology. The obtained liposomes were characterised in terms of particle size, homogeneity, surface charge, encapsulation efficiency and NVB content. The DoE analysis showed significant relation between the chosen factors (the ratio and concentration of lipids and NVB concentration) and the responses, which enabled the prediction of an optimum PSL formulation. We performed the in vitro release study at different pH values and the results demonstrated a pH-dependent release profile of the NVB-PSL optimal formulation. The in vitro evaluation of the optimal NVB-PSL formulation on two NSCLC cell lines revealed significant cytotoxicity of the liposomal formulations. In conclusion, this study reports the successful formulation and characterization of NVB-PSL as promising tool in NSCLC therapy.