Metformin loaded non-ionic surfactant vesicles: optimization of formulation, effect of process variables and characterization

Abstract

BackgroundMetformin an oral hypoglycemic has been widely used as a fist line of treatment of Type II Diabetes but in a very high dose 2–3 times a day and moreover suffers from a number of side effects like lactic acidosis, gastric discomfort, chest pain, allergic reactions being some of them. The present work was conducted with the aim of sustaining the release of metformin so as to decrease its side effects and also reduce its dosing frequency using a novel delivery system niosomes (non-ionic surfactant vesicles). Non-ionic surfactant vesicles of different surfactants were prepared using thin film hydration technique and were investigated for morphology, entrapment, in-vitro release, TEM (transmission electron microscopy) and physical stability. Optimized formulation was further studied for the effect of Surfactant concentration, DCP (Dicetyl phosphate), Surfactant: cholesterol ratio and volume of hydration. The release studies data was subjected to release kinetics models.ResultsThe prepared vesicles were uniform and spherical in size. Optimized formulation MN3 entrapped the drug with 84.50±0.184 efficiency in the vesicles of the size 487.60±2.646 and showed the most sustained release of 73.89±0.126. Also it was resulted that 100 molar concentration of cholesterol and surfactant, Presence of DCP, equimolar ratio of span 60: cholesterol and 15 ml of volume of hydration were found to be optimum for miosome preparation.ConclusionsThe present work concluded metformin loaded niosomes to be effective in sustaining the drug release leading to decreased side effects and increased patient compliance.

Design and optimization of topical methotrexate loaded niosomes for enhanced management of psoriasis: Application of Box–Behnken design, in-vitro evaluation and in-vivo skin deposition study

“…The lower volume of hydration medium may have led to incomplete or distorted formation of bilayer due to excess of material and low space. In order to accommodate the scarcity of water, the surface area of the produced vesicles was decreased and consequently the particle size increased (Sankhyan and Pawar, 2013).…”

Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

“…The equimolar CH-Span 1 60 mixture was selected since it proved to be very effective to give stable vesicles with good entrapment efficiency towards MTF (Sankhyan and Pawar, 2013). The presence of the charged surfactant enabled to obtain better results in terms of both smaller vesicle size (978.6 AE 51.9 nm), higher Zeta potential (À38.1 AE1.3 mV) and higher percent of entrapped drug (20.40%) compared to the simple CH-Span 1 60 mixture, that gives rise to vesicles of larger dimensions (1156.2 AE 86.1 nm) with lower Zeta potential (À26.0 AE 0.7 mV) and entrapment efficiency (16.46%) values.…”

“…Niosomal formulations resulted suitable also for oral delivery of hypoglycemic agents (Pardakhty et al, 2007), including metformin (Sankhyan and Pawar, 2013), and demonstrated their effectiveness in prolonging drug release and improving its therapeutic effect (Hasan et al, 2013).…”

Microparticulate and nanoparticulate drug delivery systems for metformin hydrochloride

“…However, recent studies demonstrated that metformin is effective on metabolic differences between normal and abnormal metabolic pathways (Grzybowska et al, 2011;Pernicova & Korbonits, 2014;Sankhyan & Pawar, 2013). The reductions in the hepatic glucose output and plasma-fasting insulin level, and also the reduction in insulin resistance contribute significantly to the glucose-lowering action of metformin (Zhou et al, 2001;Viollet et al, 2012;McCulloch, 2015).…”