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Abstract
Objective: The objective of the present investigation was to assess and compare the effect of surface capping by different groups (-OH, -COOH and -NH2) on tumor targeting potential of folate conjugated poly (propylene imine) (PPI) (F-PPI) dendrimers using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay.
Materials and methods: The synthesized nanoconjugates (F-PPI, F-COOH-PPI, F-OH-PPI and F-CONH-PPI) were characterized by Fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (1H-NMR) and transmission electron microscopic (TEM) studies. The formulations were evaluated for drug entrapment, in vitro drug release and hemolytic toxicity, and cytotoxicity was evaluated on HeLa and SiHa cell line using MTT assay.
Results: In case of all surface capped formulation, Methotrexate (MTX) loading was found to increased; however MTX release rate was found to decrease as compared to unmodified formulation. Further, F-COOH-PPI displayed highest tumor targeting potential as compared to other formulations. This is the first study to explore the effect of surface capping on the targeting potential of folate-conjugated fifth generation (5.0 G) PPI dendrimer.
Conclusions: In conclusion, the targeting potential of all the formulations (anticancer activity) for both HeLa and SiHa cells follows in the following order: F-COOH-PPI > F-OH-PPI > F-CONH-PPI > F-PPI.
Declaration of interest
The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article. Mr. Birdhariya reports grants from University Grants Commission (UGC) New Delhi, India, other from M/s Khandelwal Labs Ltd., Mumbai, India, during the conduct of the study. Dr. Kesharwani reports grants from Indian Council of Medical Research (ICMR), New Delhi, India, during the conduct of the study. Dr. Jain has nothing to disclose.