Enhanced corneal permeation and antimycotic activity of itraconazole against Candida albicans via a novel nanosystem vesicle

Abstract

The objective of this study was to investigate the potential of spanlastics as an ophthalmic delivery system to improve the corneal permeability and antimycotic activity of itraconazole (ITZ). Spanlastics containing edge activators, including Tween 20 or 80, were produced by modified ethanol injection method and exhibited a particle size of approximately 287 nm and an entrapment efficiency of more than 88%. Less than 13% ITZ was released from spanlastics over 6 h compared to 35% from conventional niosomes. Spanlastics exerted a 1.34-fold increase in the amount of ITZ permeated through excised bovine cornea after 24 h compared to conventional niosomes. Antimycotic study revealed a significant (p < 0.05) increase in the zone of inhibition of Candida albicans culture demonstrated by spanlastics compared to ITZ powder at the same concentration level (10 mg). In vivo Draize test showed no signs of acute ocular toxicity upon application of the selected spanlastic formulation to the rabbit eye. Results revealed that spanlastics loaded with itraconazole could be a potential nanosystem in ocular drug delivery systems.

Carbamazepine Loaded Vesicular Structures for Enhanced Brain Targeting via Intranasal Route: Optimization, in Vitro Evaluation, and in Vivo Study

“…It is calculated through the ratio of the standard deviation to the mean vesicle size. The higher of the PDI, the lower of the vesicle size's uniformity [32]. The PDI for the prepared formulation ranged from 0.594-0.99 as shown in table 1.…”

“…While after 90 min the release showed almost the same profile and no significant difference was noticed at the end of the release profile (p>0.05), while for the CBZ suspension the release profile showed the release of 61.11% after 180 min. This might be due to the vesicular structure of spanlastics and the incorporation of span 60 and polyvinyl alcohol which can improve the release of the CBZ from the vesicles [12,32]. Both formulations were found to fit the Higuchi diffusion equation with ''r'' values of 0.976 and 0.992 for the optimized spanlastics formulation and CBZ suspension, respectively.…”

“…EE is an important parameter in the vesicular formulation's design. The more the EE, the more drug's bioavailability and also the higher the drug's concentration will be targeted to the specific site leading to decrease in the required dose [32]. The EE ranges for all prepared formulations was ranged from 44%-97.6%.…”

“…According to equations (13) and (14), the positive coefficient of XA reveals that the EE increased as the drug amount which is used to load the niosomes or the spanlastics increased. This is may be due to the increase in the medium's saturation with the drug which will then be available to be encapsulated into the vesicles [32].…”

<p>Mitigation of Rheumatic Arthritis in a Rat Model via Transdermal Delivery of Dapoxetine HCl Amalgamated as a Nanoplatform: In vitro and in vivo Assessment</p>

“…This suggests that DH interacts with the bilayer components, causing numerous lattice defects, with DH residing in amorphous regions; this may account for the enhanced entrapment of DH in the TENVs in an amorphous state. 89 Physical Stability of the Optimized DH-TENV…”