by Nabil A. Alhakamy, Solomon Z. Okbazghi, Mohamed A. Alfaleh, Wesam H. Abdulaal, Rana B. Bakhaidar, Mohammed O. Alselami, Majed AL Zahrani, Hani M. Alqarni, Adel F. Alghaith, Sultan Alshehri, Shaimaa M. Badr-Eldin, Hibah M. Aldawsari, Omar D. Al-hejaili, Bander M. Aldhabi, Wael A. Mahdi
BackgroundLung cancer in men and women is considered the leading cause for cancer-related mortality worldwide. Anti-cancer peptides represent a potential untapped reservoir of effective cancer therapy.
MethodologyBox-Behnken response surface design was applied for formulating Alendronate sodium (ALS)-mastoparan peptide (MP) nanoconjugates using Design-Expert software. The optimization process aimed at minimizing the size of the prepared ALS-MP nanoconjugates. ALS-MP nanoconjugates’ particle size, encapsulation efficiency and the release profile were determined. Cytotoxicity, cell cycle, annexin V staining and caspase 3 analyses on A549 cells were carried out for the optimized formula.
ResultsThe results revealed that the optimized formula was of 134.91±5.1 nm particle size. The novel ALS-MP demonstrated the lowest IC50 (1.3 ± 0.34 μM) in comparison to ALS-Raw (37.6 ± 1.79 μM). Thus, the results indicated that when optimized ALS-MP nanoconjugate was used, the IC50 of ALS was also reduced by half. Cell cycle analysis demonstrated a significantly higher percentage of cells in the G2-M phase following the treatment with optimized ALS-MP nanoconjugates.
ConclusionThe optimized ALS-MP formula had significantly improved the parameters related to the cytotoxic activity towards A549 cells, compared to control, MP and ALS-Raw.
