Abstract
The main aim of the study was to develop and statistically optimize the proniosomal gel for enhanced transdermal delivery using 32 factorial designs to investigate the influence of both non-ionic surfactant and cholesterol to maximize the entrapment efficiency and flux. The concentration of non-ionic surfactant and cholesterol were taken as independent variables, while entrapment efficiency and flux were taken as dependent variables. The study showed that the entrapment efficiency depends on both cholesterol and surfactant, whereas permeation flux depends only on the surfactant. Proniosomal gel showed a significantly enhanced drug permeation through the skin, with an enhancement ratio 3.81±1.85 when compared to the drug solution. Comparative evaluation of permeation studies and the in vitro release study of optimized proniosomal gel (F5) with that of marketed gel and carbopol gel showed that the penetration of the optimized formulation was enhanced 1.75 times in comparison with that of the marketed formulation, and the release was in a controlled manner. Similarly, the anticandidial activity showed a significantly higher activity (p<0.05) than the marketed and carbopol gel. This may be due to the enhanced penetration of noisome-containing drug through the fungal cell wall, inhibiting the ergo sterol synthesis, thereby causing the fungal cell death due to the presence of penetration enhancer. The stability study at two different temperatures (30 ± 2°C and 4 ± 2°C) confirmed that the formulations were stable even at the end of 45 days. Hence, proniosomal gel is an efficient carrier for the delivery of clotrimazole, thereby prolonging the action.
Highlights
The main obstacle for the delivery of drug through the skin is the "dead, impermeable barrier devoid of biological activity“ i.e., the stratum cornea; various approaches were put forward for overcoming it [1]
The non-ionic surfactant selected for the study is span 60 because of high transition temperature (53°C) and the chemical structure(long alkyl chain), which is reported for the higher entrapment efficiency
The entrapment efficiency and permeation are largely dependent upon the concentration of non-ionic surfactant and cholesterol, and any alteration in their concentration may lead to the leakiness of the vesicles that result in the leakage of free drug before drug diffusion and fusion of vesicles
Summary
The main obstacle for the delivery of drug through the skin is the "dead, impermeable barrier devoid of biological activity“ i.e., the stratum cornea; various approaches were put forward for overcoming it [1]. Among the various colloidal carriers, liposome and niosome were the popular ones as they can efficiently encapsulate both hydrophilic and hydrophobic drugs. These carriers encountered stability problems, and this led to the discovery of proniosomes. Proniosomes are a liquid crystalline compact niosomal hybrid, which upon hydration will be converted to niosomes and thereby considered the versatile carrier for transdermal delivery [3]. It provides additional convenience of storage, transport and dosing. The key ingredients used in its preparation are Generally Regarded as Safe [4]
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