Formulation and statistical optimization of intravenous temozolomide-loaded PEGylated liposomes to treat glioblastoma multiforme by three-level factorial design

Abstract

The aim of the presented study was to develop PEGylated liposomes of Temozolomide (TMZ) that provide optimum drug concentration at tumor site. Reverse phase evaporation (REV) method was used to prepare TMZ-loaded PEGylated liposomes. Formulation was optimized by using design expert software by 3² factorial design. The physicochemical properties including size, morphology, entrapment efficiency, drug loading, etc. of formulated liposomes were evaluated. Finally, the optimized formulation was selected for in vitro drug release and stability study. In vivo pharmacokinetic study in rats showed that TMZ-loaded PEGylated liposomes leads to 1.6-fold increase in AUC_Total in blood and 4.2-fold increase in brain as compared to free drug solution. This formulated PEGylated liposomes offers a promising approach for treatment of Glioblastoma Multiforme.

Keywords:

• Glioblastoma multiforme
• reverse phase evaporation
• intravenous
• PEGylation
• liposomes

Acknowledgements

Authors would like to acknowledge Lipoid GmbH, Germany for providing the lipids as gift sample as well as TIFAC-CORE, The M.S. University of Baroda for providing instrument facilities.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

Authors would like to acknowledge Lipoid GmbH, Germany for providing the lipids as gift sample as well as TIFAC-CORE, The M.S. University of Baroda for providing instrument facilities.