Phosphatidylinositol 3-kinase inhibitor (PIK75) containing surface functionalized nanoemulsion for enhanced drug delivery, cytotoxicity and pro-apoptotic activity in …
Pharmaceutical research, 2012•Springer
Purpose Ovarian cancer is a debilitating disease, which needs multi-pronged approach of
targeted drug delivery and enhanced efficacy with the use of combination therapeutics. In
this study, we have examined the anticancer activity of PIK75 incorporated in surface
functionalized nanoemulsions for targeted delivery to SKOV-3 cells. A pro-apoptotic
molecule C 6-ceramide was also co-delivered to augment therapeutic efficacy. Methods
EGFR and FR functionalized nanoemulsions incorporating PIK75 and C 6-ceramide were …
targeted drug delivery and enhanced efficacy with the use of combination therapeutics. In
this study, we have examined the anticancer activity of PIK75 incorporated in surface
functionalized nanoemulsions for targeted delivery to SKOV-3 cells. A pro-apoptotic
molecule C 6-ceramide was also co-delivered to augment therapeutic efficacy. Methods
EGFR and FR functionalized nanoemulsions incorporating PIK75 and C 6-ceramide were …
Purpose
Ovarian cancer is a debilitating disease, which needs multi-pronged approach of targeted drug delivery and enhanced efficacy with the use of combination therapeutics. In this study, we have examined the anticancer activity of PIK75 incorporated in surface functionalized nanoemulsions for targeted delivery to SKOV-3 cells. A pro-apoptotic molecule C6-ceramide was also co-delivered to augment therapeutic efficacy.
Methods
EGFR and FR functionalized nanoemulsions incorporating PIK75 and C6-ceramide were characterized for particle size, surface charge, entrapment efficiency and morphology. Fluorescence and quantitative uptake studies were conducted in SKOV-3 cells to determine intracellular distribution. Cell viability was assessed using MTT assay while mechanism of cytotoxicity was evaluated using capsase-3/7, TUNEL and hROS assay.
Results
Cytotoxicity assay showed 57% decrease in IC50 value of PIK75 following treatment with EGFR targeted nanoemulsion and 40% decrease following treatment with FR targeted nanoemulsion. Combination therapy with PIK75 and ceramide enhanced the cytotoxicity of PIK75 compared to therapy with individual formulations. The increase in cytotoxicity was attributed to increase in cellular apoptosis and hROS activity.
Conclusion
The results of this study showed that the targeted system improved cytotoxicity of PIK75 compared to the non-targeted system. Combination therapy with ceramide augmented PIK75’s therapeutic activity.
Springer
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