Invasomes of isradipine for enhanced transdermal delivery against hypertension: formulation, characterization, and in vivo pharmacodynamic study

Abstract

Context Isradipine is an effective calcium channel blocker used in the management of hypertension. It undergoes extensive first pass metabolism and has low oral bioavailability. Hence we attempted to develop isradipine-loaded invasomes. Objective The purpose of this work was to prepare and characterize invasomes carrier for isradipine, and to evaluate the optimized formulation obtained for pharmacodynamic study. Materials and methods Isradipine-loaded invasomes were prepared by conventional thin layer evaporation technique using Phospholipon® 90G, β-citronellene (terpene) and ethanol. Prepared formulations were characterized in terms of size, size distribution, morphology, entrapment efficiency, and antihypertensive activity. Results and discussion It was observed that prepared isradipine-loaded invasomes delivers ameliorated flux, reasonable entrapment efficiency, and more effectiveness for transdermal delivery. The optimized formulation presented the particle size of 194 ± 18 nm, entrapment efficiency (88.46%), and attained mean transdermal flux of 22.80 ± 2.10 μg/cm²/h through rat skin. Confocal laser scanning microscopy revealed an enhanced permeation of Rhodamine-Red-loaded isradipine invasomes to the deeper layers of the rat skin. During antihypertensive study, the treatment group showed a substantial and constant decrease in blood pressure, for up to 24 h. The isradipine invasomes formulation was found to be effective, with a 20% reduction in blood pressure by virtue of better permeation through Wistar rat skin. Conclusion It was concluded that the developed isradipine invasomes accentuate the transdermal flux and the results obtained encouraged the use of the isradipine-loaded invasomes as the formulation for the potential management of hypertension.

Keywords:

• Hypertension
• invasomes
• isradipine
• transdermal

Disclosure statement

All authors have approved the final manuscript and the authors declare that they have no conflicts of interest to disclose.