504P - Synthesis of folic acid-chitosan bioconjugate system for cancer cell targeting: reaction parameter optimization and characterization

Date 19 December 2015
Event ESMO Asia 2015 Congress
Session Poster presentation 1
Topics Basic Science
Presenter Akhilesh Singh
Citation Annals of Oncology (2015) 26 (suppl_9): 153-155. 10.1093/annonc/mdv534
Authors A.V. Singh
  • Materials Engineering, Indian Institute of Science, 560012 - Bangalore/IN

Abstract

Aim/Background

Folic acid (FA) based conjugate systems are frequently used in anticancer drug delivery because of its increased potential for internalization by receptor mediated endocytosis into the cancer cells. The conjugation reaction between conjugating polymer and FA depends on many reaction parameters that affect the degree of conjugation. In this study, an approach to synthesize FA-chitosan (CS) conjugate system was undertaken.

Methods

FA-chitosan (CS) conjugate system based on carbodiimide chemistry was developed by conjugating the free carboxyl group of folic acid moiety and primary amine group of CS. Two parameters were optimized: (i) reaction duration [4 to 48 h] and (ii) concentration of N-hydroxysuccinimide [0.25-1.00 g] to know their effect on percentage of conjugation. The conjugate formed was confirmed by FT-IR, and percentage conjugation of FA was analyzed by UV spectroscopy. The highly conjugated FA-CS system was further characterized by XRD, DSC and TGA. The morphology and bio-compatibility parameters were also studied by SEM and MTT assay, respectively.

Results

We found that conjugation was efficient when the reaction duration and NHS concentration were ≥24 h and 0.75 g, respectively. The bio-conjugate system formed was more amorphous as confirmed by XRD, DSC and TGA analysis. The conjugated material did not exhibit any cytotoxicity in HeLa cells.

Conclusions

The results showed a potential to be used this material in anti-cancer drug delivery application.

Clinical trial identification

Disclosure

All authors have declared no conflicts of interest.