Assessment of Physical, Mechanical, Biopharmaceutical Properties of Emulgels and Bigel Containing Ciclopirox Olamine

Abstract

Emulsions are thermodynamically unstable systems and it is difficult to produce biphasic formulations with large amounts of oil. The aim of our study was to prepare biphasic formulations containing 1% ciclopirox olamine and to determine the influence of the method of oil incorporation (without and with emulsifier and gelifier) on the physical (pH, particle size, rheological properties), mechanical, and biopharmaceutical properties of the formulations. It was found that the use of a poloxamer 407 gel as the hydrophase could result in a stable formulation when an oil with (EPG) or without an emulsifier (APG) or oleogel (OPG) was used as the oily phase. The results of the studies showed that the addition of an emulsifier (polysorbate 80) led to a decrease in the sol-gel temperature, a slower release of ciclopirox olamine, and a higher stability in the freeze–thaw test. However, regardless of the way the oil is incorporated, the particles are distributed in the same range and the antifungal activity against T. rubrum is the same. It is possible to create a biphasic formulation with a large amount of oil and poloxamer gel, but for greater stability, it is recommended to include an emulsifier in the composition.

Development and Evaluation of Two-Phase Gel Formulations for Enhanced Delivery of Active Ingredients: Sodium Diclofenac and Camphor

“…The higher consistency values tend to result in the sample having a thicker and harder form. From a biopharmaceutical perspective, products with a low consistency can be more thoroughly applied on the skin and more easily absorbed [ 74 ]. The lowest consistency was determined in the 5/95 sample (315.54 g·s), and the bigels with ratios 10/90, 15/85, 20/80, 25/75, 30/70 had similar values (324.03–331.69 g·s).…”

“…Many authors have described index of viscosity as the extrusion energy or work of adhesion when it becomes higher [ 74 , 77 , 78 ]. In this study, it was observed that the higher the cohesiveness, the stronger the inner intermolecular bonds in the sample of the bigel and the lower the adhesion to the tool of the device.…”

“…Analysis of the results given in Table 5 shows that for the investigated samples, the structural viscosity gradually decreases with an increase in the shear rate gradient. This dependence is typical for systems with a plastic type of flow and characterizes the studied bigels as structured dispersed systems, which will ensure their easy and uniform distribution on the skin [ 74 , 79 ]. The viscosity of both tested samples at storage (25 °C) and application (32 °C) temperatures changes slightly—no more than 1.2 times.…”

Statistical modeling, optimization and characterization of andrographolide loaded emulgel for its therapeutic application on skin cancer through enhancing its skin permeability

“…In brief, 2 g of sample (ANG 12) was stored at −20 °C for 24 h into a 5 ml Eppendorf tube. After 24 h, the Eppendorf tube was kept at 22 °C and thawed for 5 h. The freeze-thawing process was repeated in triplicate and analysed for any change in appearance at the end of every cycle ( Mazurkeviciute et al, 2022 ).…”

The effect of preparation temperature and composition on bigel performance as fat replacers

“…20 Various bigel systems have recently been reported in the literature aiming to explore the general characteristics of bigels or to provide comprehensive knowledge of bigels as fat mimetics. Bigels were formulated using GMS, [20][21][22][23][24][25][26] waxes, 15,[27][28][29] ethyl cellulose 25,30 and a lecithin-stearic acid mix 31 as the oleogelators, while gelatin, 20,25,28,29 gums, 21,32 κ-carrageenan, 23,24 alginate 15,33 and others were used as the hydrogelators. The bigels' mixing procedure is commonly achieved by mixing two hot phases at temperatures higher than 70 °C (ref.…”