Development and characterization of oleic acid vesicles for the topical delivery of fluconazole

Abstract

Fatty acids have been widely used as adjuvant, vehicles in drug delivery viz penetration enhancers in topical delivery and in polymeric micelles to provide sustained release. However, the present investigation aims at exploring the potential of fatty acid vesicles for the topical delivery of fluconazole. Vesicles were prepared by film hydration method using oleic acid as a fatty acid principal component. Developed vesicles were characterized for size, size distribution, shape, in vitro release, pH dependent and storage stability, skin irritation study, and ex-vivo skin permeation. Penetration behavior of vesicles was further evaluated and elucidated using confocal microscopic study. Optical microscopy and TEM studies confirmed vesicular dispersion of fatty acid. The vesicles possessed higher entrapment efficiency (44.11%) with optimum vesicle size and homogeneity in regard to size distribution (PDI = 0.234 +/- 0.016) at 7:3 oleic acid-to-fluconazole ratio. In vitro drug release study suggested sustained release of drug from the vesicles. The release pattern followed Higuchian kinetics. The vesicles were fairly stable at refrigerated conditions. Ex-vivo skin permeation and confocal microscopic studies suggested that oleic acid vesicles penetrate the stratum corneum and retain the drug accumulated in the epidermal part of the skin. On the basis of sustained release behavior and skin retention it can be inferred that oleic acid vesicles can serve as a potential carrier for the topical localized delivery of bioactives.

Novel elastic membrane vesicles (EMVs) and ethosomes-mediated effective topical delivery of aceclofenac: a new therapeutic approach for pain and inflammation

“…Ltd., Mumbai, India) installed at Institute of Microbial Technology; IMTECH, Chandigarh, India. The mean value of three repeated measurements for each sample was reported as the final observation (Zakir et al, 2010;Negi et al, 2015b;Hussain et al, 2016).…”

Novel lecithin-integrated liquid crystalline nanogels for enhanced cutaneous targeting of terconazole: development, in vitro and in vivo studies

“…20 TEM demonstrated irregular and discrete microstructures for liquid crystalline organogel. The system showed liquid crystals of small particle size ,50 nm as shown in Figure 5.…”

“…Female Swiss albino mice of 20-25 g were selected for these studies. The negative control group was treated with normal saline 45 while formalin was used as a standard irritant 20,37 for the positive control group. The dorsal region of mice was shaved 24 h prior to the application of the formulations 52 using a hair remover cream (Veet ® , Reckitt Benchiser).…”

“…The test was carried out for both blank and medicated organogels. The negative control group was treated with normal saline 45 while formalin was used as a standard irritant 20,37 for the positive control group. The skin was observed for any visible change, such as erythema at 24, 48, and 72 h after the application of formulations.…”

“…The major drawback of these formulations is that most of them suffer from restricted drug delivery across the skin, resulting in therapeutic failure. 20 On the other hand, several excipients are often used in other formulations for enhancing drug permeation through stratum corneum (SC) such as Azone 21,22 and dimethyl sulfoxide. 23 These excipients cause disruption to the SC layers resulting in the penetration of antifungal drug into the deeper skin layers and, unfortunately, into blood circulation causing systemic side effects.…”