Objective: The aim of present study is to develop and explore efficiency of 5.0G EDA PAMAM dendrimers as long-duration drug release carriers for the treatment of tuberculosis.
Method: Rifampicin (RIF) was selected as a major drug for incorporation into PAMAM dendrimers based on its anti-tubercular activity and hydrophobic nature. Further polyethylene glycol (PEGylated) PAMAM dendrimers were evaluated for their hemolytic toxicity and in vivo anti-tubercular studies. The 5.0G PAMAM dendrimers are prepared by using initiator core ethylene diamine and methyl acrylate. Furthermore, the PEGylation was done by polyethylene glycol 2000 using epichlorhydrin as a cross linking agent.
Result: The Rifampicin loaded PEGylated 5.0G PAMAM dendrimers were characterized by FTIR, NMR, DSC and SEM analysis. The in vivo study report ensures the suitability of PEGylated dendrimer in connection to prolonged delivery of Rifampicin. Moreover, PEGylated system has shown a reduced hemolytic toxicity.
Conclusion: The observed results concluded that the PEGylated method was less time consuming, inexpensive, and reproducible, and it also reduces toxicity.
Keywords: PAMAM dendrimers, rifampicin, PEGylation, in vivo PAMAM dendrimers, anti-tubercular studies, hemolytic toxicity.