In vitro cytotoxicity, in vivo pharmacokinetic studies and tissue distribution studies of multifunctional citric acid dendrimers using the drug Cytarabine

Abstract

Dendrimers are considered the emerging polymeric architectures, known for their well defined molecular-weight, polydispersity, uniformity and high-surface functionality. These nano-architectures are capable of encapsulating low-high molecular-weight drug moieties in their interior or exterior through covalent bonding and host-guest interactions. Further, large surface volume made researchers to implicate dendrimers in biomedical and therapeutic applications. Regardless of the massive applications, sometimes its use is limited because of the cytotoxicity produced.  Considering this, the present research is focused on the synthesis and PEGylation of citric acid dendrimers. PEGylation is an act of conjugating polyethylene glycol to dendrimers that completely eliminates the toxicity issues associated with dendrimers and render them biocompatible. Cytarabine was loaded in the dendritic architecture to target specifically the tumor cells. Dendrimers are made tumor specific by incorporating certain agents that get cleaved in tumor environment. Synthesized dendrimers were studied for its effect on acute cytotoxicity, tissue-distributions and pharmacokinetic parameters.