Abstract
Objective: Ivabradine hydrochloride (IH), a benzazepine derivative used to treat cardiovascular disease angina pectoris. In this study IH-loaded novel carrier systems transfersomes (TFs) and conventional liposomes (CLs) were developed and compared for their efficacy to enhance the stability of drugs from degradation.
 Methods: TFs formulations (TF-1, TF-2 and TF-3) were prepared by using different biocompatible surfactants; tween-80 (TW), span-80(S) and sodium deoxycholate (SC) in the concentration ratio of 15 parts with 85 parts of soy phosphatidylcholine as phospholipid by thin-film hydration method. These vesicles were compared with CLs formulation (L-1) prepared in 7:3 molar ratio of soy phosphatidylcholine: cholesterol by following the same method. These vesicles were compared for physical appearance, vesicle shape, and size, percentage drug entrapment efficiency (%DEE), deformability index (DI), in vitro percentage cumulative drug release study, and physical stability studies. The chosen optimized novel carriers were observed under scanning electron microscopy.
 Results: The compared data demonstrated that the physical appearance for all vesicles was turbid and had a spherical shape. The size distribution was in the range of 129.0 nm to 273.5 nm in vesicles. The %DEE (79.0±0.94) and DI (35.0±1.9) was found maximum in TF-1 formulation that was 2.3 times higher than L-1 formulation. The in vitro percentage cumulative drug release study followed second-order polynomial kinetics that was 2.0 times higher than L-1and 2.9 times higher than the plain drug in 30 min (90.4±0.06%) from TF-1. The vesicles were found to be stable at refrigeration conditions.
 Conclusion: Thus, amongst of all vesicles TW loaded TFs (TF-1) was chosen as an excellent novel vesicular carrier for hydrophilic drugs due to its higher deformability behavior than CLs that protects the certain drugs from biodegradation and provides stability.
Highlights
Ivabradine hydrochloride (IH), an inhibitor of the If pacemaker current, selectively targets the heart rate and to beta-blockers that does not reduce myocardial contractility or relaxation [1]
The conventional liposomes (CLs) formulation L-1 was developed with cholesterol with Soy phosphatidylcholine phospholipid
It was found that all vesicles formulations were turbid and colloidal against the black background
Summary
IH, an inhibitor of the If pacemaker current, selectively targets the heart rate and to beta-blockers that does not reduce myocardial contractility or relaxation [1]. Results of a postmarketing surveillance study in thousands of patients, where therapy with Ivabradine tablets was associated with a significant reduction in the frequency of angina attacks and consumption of short-acting nitrates of 87% This includes an increase in myocardial diastolic perfusion time [2], enhancement in coronary flow reserve [3], and improvement in endothelial function [4] in patients with chronic stable coronary artery disease [5]. TFs having flexible membrane by phospholipid and surfactants in the proper ratios that minimize the risk of complete vesicle rupture They can deform and pass through narrow constriction from 5 to times less than their own diameter. These are the biocompatible and biodegradable carrier for low and high molecular weight drugs e. g. analgesic, anesthetic, corticosteroids, hormones, anticancer, insulin, gap junction protein, and albumin [8]
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