In this study, we have established an effective and novel nanocarrier system for the effective treatment of
glioma. We have established the
glioma tissue penetrating nanocarrier system by conjugating Pep-1 as a targeting
ligand on the
liposome surface to enhance the anticancer efficacy of
cilengitide (CGL). The particles were nanosized and exhibited a controlled release of
drug in both the pH conditions. The cellular uptake assay showed that conjugation of Pep-1 on the
liposome surface remarkably increased the cellular uptake. The uptake of CGT-loaded
Pep-1 peptide-conjugated
liposome (PeCNL) increased to 89.8% compared to 47.5% for CNL indicating the efficient internalization of the nanocarriers. Consistently, PeCNL exhibited a significantly higher cytotoxic effect in
cancer cells compared to that of non-targeted CGT-loaded
liposome (CNL). PeCNL exhibited a higher apoptosis of
cancer cells (∼35%) compared to that of CNL. Most importantly, PeCNL exhibited a significantly superior anticancer effect with
tumor volume as low as ∼350mm3 indicating the superior anticancer potential of targeted formulations. Similarly, PeCNL showed the lowest staining for Ki67 indicating that the targeted NP has the maximum effect in controlling the proliferation of
cancer cells. Taken together, Pep-1 conjugated
liposome could exhibit better antitumor efficacy when applied to IL-13R2 receptor overexpressed specific brain
glioma.