Abstract

Purpose: Breast cancer is a prevalent form of cancer in woman. Vorinostat (VOR) is a chemotherapeutic drug that has been utilized for treatment of breast cancer, but its effectiveness is limited due to low bioavailability and several side effects. The primary aim of this study is to prepare folic acid (FA) conjugated pegylated bilosomes containing VOR for the selective targeting of breast cancer cells with the FA receptor expression. Accordingly, lithocholic acid (LCA) was used as a bile acid in bilosomes due to its anti-cancer and anti-proliferation effects. Methods: VOR loaded bilosomes were prepared using the thin-film hydration method and optimized by applying two-level fractional factorial design. Various properties of the considered bilosomes, including particle size, zeta potential (ZP), polydispersity index (PdI), encapsulation efficiency (EE) % and drug loading (DL) %, were then investigated and synthesized FA-PEG-Cholesterol was incorporated in the optimized bilosomes. The anti-cancer efficacy of VOR loaded FA-PEG- bilosomes was also evaluated in vitro using the MCF-7 and 4T1 breast cancer cell lines. Furthermore, drug-free FA-PEG-bilosomes and bilosomes were evaluated for biocompatibility in the L929 cell line. Results: The optimized VOR loaded bilosomes exhibited spherical particles with the size of 305.33 ± 18.50 nm, PdI of 0.37 ± 0.03, zeta potential of -17.66 ± 0.15 mV, EE of 92.91 ± 0.22 % and DL% of 23.64 ± 0.04%. Incorporation of FA-PEG-cholesterol in nanobilosomes increased the particle size and absolute value of zeta potential. In vitro cytotoxicity study also revealed that VOR loaded FA- PEG-bilosomes demonstrated a greater cytotoxic effect, as compared to the free VOR and VOR- bilosomes in both MCF-7 and 4T1 cancer cells. Conclusion: This showed that FA- PEG-bilosomes could be a promising formulation for the treatment of FA (+) tumors.

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