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Diltiazem hydrochloride (DTZ) is a calcium channel antagonist depicted by extensive first pass metabolism and low oral bioavailability. The aim of this work was to develop niosomes for potential nasal delivery of DTZ. Niosomes protect hydrophilic drugs inside their core while nasal route offers both rapid onset and evasion of first-pass metabolism. Niosomes were prepared using a combination of Span 60 or Brij-52 with cholesterol (CHOL) in different molar ratios followed by determination of entrapment efficiency, particle size and in vitro drug release. A parallel design was adopted to evaluate the pharmacokinetic performance of DTZ-loaded niosomes in male Wistar rats. Non-compartmental analysis was performed where C_max, T_max, t_1/2, MRT, area under the release curve (AUC) and K_e were assessed. The prepared niosomes were spherical with mean particle size 0.82–1.59 μm. Span 60-cholesterol niosomes …