Imatinib loaded pegylated Poly Propylene Imine dendrimer for delivery to leukemic cells; fabrication of formulation and evaluation

Document Type : Reasearch Paper


1 Department of Biotechnology, Acharya Nagarjuna University, Nagarjuna Nagar, Guntur, India

2 Faulty of Pharmaceutical Sciences, UCSI University, Kualalampur, Malaysia

3 Vignan Pharmacy College, Vadlamudi, India



PEGylated polypropyleneimine (PPI) dendritic scaffold was used for the delivery of an anti-leukemic drug, Imatinib. The current study evolves and emerges the use PEGylated PPI dendritic scaffold for the delivery of this drug. In this Imatinib was synthesized and loaded with PEGylated PPI dendritic scaffold. Parameters such as FT-IR, NMR, SEM, drug release, DSC and hemolytictoxicity are required. Other parameters such as drug entrapment of both PEGylated and non-PEGylated systems were comparatively determined. Drug-loading capacity was found to be increased with the PEGylation and reduces the haemolytic toxicity as well as drug release rate. By this, prolonged delivery of Imatinib was found to be suitable with this system. By delivering the drug for a prolonged period of time at a controlled rate, we expect that this approach will improve the management of drug therapy in leukemic patients.


Main Subjects

[1] Marie R., Griffin M. D., MPH X., (1998), Epidemiology of nonsteroidal anti-inflammatory drug–associated gastrointestinal Injury. The Am. J. Medic. 104: 23-29.
[2] Chi S. C., Jun H. W., (1990), Anti-inflammatory activity of ketoprofen gel on carrageenan-induced paw edema in rats. J. Pharm. Sci. 79: 974-977.
[3] Lin S. Z., Wouessidjewe D., Poelman M. C., Duchone A., (1994), In vivo evaluation of indomethacin/cyclodextrin complexes gastrointestinal tolerances and dermal anti-inflammatory activity. Int. J. Pharm. 106: 63-67.
[4] Chan T. A., (2002), Nonsteroidal anti-inflammatory drugs, apoptosis, and colon-cancer chemoprevention. Lancet Oncol. 3: 166-174.
[5] Jacobs J., Golstein A. G., Kelly M. E., Bloom B. S., (1998), NSAID dosing schedule and compliance. Drug Intell. Clin.Pharm. 22: 727-738.
[6] Tomalia D. A., Baker H., Dewald J. R., (1986), Dendritic macromolecules: synthesis of starburst dendrimers. Macromolecules. 19: 2466–2468.
[7] Kumar P. V., Asthana A., Datta T., Jain N. K., (2006), Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers. J. Drug Targ. 14: 546-556.
[8] Singhai A. K., Jain S., Jain N. K., (1997), Evaluation of an aqueous injection of ketoprofen. Pharmazie. 52: 149-151.
[9] Chauhan A. S., Jain N. K., Diwan P. V., Khopade A. J., (2004), Solubility enhancement of indomethacin with poly(amidoamine) dendrimers and targeting to inflammatory regions of arthritic rats. J. Drug Target. 12: 575-583.
[10] Calvo P., Gouritin B., Chacun H., Desmaele D., D Angelo J., Noel J. P.,  Georgin D., Fattal E., Andreux J., Couvreur P., (2001), Long-circulating PEGylated polycyanoacrylate nanoparticles as new drug carrier for brain delivery. P. Pharmaceu. Res. 18: 1157-1166.
[11] De Brabender-Van D. B., Meijer E. M., (1993), Poly (propylenimine) dendrimers: large-scale synthesis via heterogeneously catalyzed hydrogenation. Angew. Chem. Int. Ed. Engl. 32: 1665-1688.
[12] Bhadra D., Bhadra S., Jain S., Jain N. K., (2003), A PEGylated dendritic nanoparticulate carrier of fluorouracil. Int. J. Pharm. 257: 111-124.
[13] Marcelo C., Mohiuddin A Quadir., Miriam S., Rainer H., (2010), Functional dendritic polymer architectures as stimuli-responsive nanocarriers. Biochimie. 92: 1242-1251.
[14] Sanjay K., Shruti C., Sushma T., Kanchan K., (2008), Chitosansodium alginate nanoparticles as submicroscopic reservoirs for ocular delivery: Ormulation, optimisation and in vitro characterization. Europ. J. Pharm. and Biopharmac. 68: 513–525.
[15] Souto, E. B., Wissing S. A., Barbosa C. M., Müller R. H., (2004), Development of a controlled release formulation based on SLN and NLC for topical clotrimazole delivery. Int. J. Pharmac. 278: 71-77.
[16] Sunil A., Nadagouda N., Mallikarjuna T., Aminabhavi M., (2004), Recent advances on chitosan-based micro- and nanoparticles in drug delivery. J. Cont. Rel. 100: 5–28.
[17] Todorova N., Maneva K., Ilarionova M., (2003), Antileukemic effect of epirubicin conjugated with chitosan against mouse P388 ascitic leukemia. Biotechnol. Biotechnol. Eq. 17: 151-153.
[18] Virendra G., Vijayaraj K. P., Rakesh K. T., Narendra K J., (2009), PEGylated PPI dendritic architectures for sustained delivery of H2 receptor antagonist. Euro. J. Medl. Chem. 44: 1155-1166.