ISSN: 7027-2221

Author : AL Haydar, Muder

Effects of formulation variables on the Candesartan cilexitil nanoparticles properties using poloxamer 188

Alaa Mohamed Baqer; Mowafaq Mohammed Ghareeb; Muder AL Haydar

karbala journal of pharmaceutical sciences, Volume 6, Issue 9, Pages 105-113

Candesartan celexitil (CC), a non-peptide angiotensin II type 1 (AT1) receptor antagonist, is
used in the treatment of hypertension. It has low solubility with low bioavailability thus
nanoparticles approach is one of the recently technique used to enhance the solubility of
drugs. The aim of this study is to improve the solubility of CC by preparing nanoparticles.
Seven formulas of nanoparticles were prepared by antisolvent precipitation method utilizing
poloxamer 188 as polymer. Three of them at different drugs: polymer ratio and another three
different solvent: anti solvent ratios. The prepared nanoparticles were characterized regarding
the particle size by nano laser particle size analyzer, saturated solubility, and thermal analysis
by DSC. The prepared nanoparticle reveals that all formulas produce nanoparticle in range of
70.6 - 1119 nm. Formula (F2) which utilizes PXM as polymer at polymer: drug ratio of (1:1)
and solvent: antisolvent ratio of (1:10) was considered as the best formula which shows good
evaluation parameters in addition to increment in solubility 10.54 times than that of pure
drug. The thermal analysis of nanoparticle of the selected formula (F2) shows reducing of
intensity of endothermic peak of the drug indicating reduced crystallinity of candesartan
cilexetil. Finally it could be concluded that the selected formula is promising for preparation
of candesartan cilexetil nanoparticles with improved solubility.