Flurbiprofen-loaded niosomes-in-gel system improves the ocular bioavailability of flurbiprofen in the aqueous humor

Abstract

The present work aimed to prolong the contact time of flurbiprofen (FBP) in the ocular tissue to improve the drug anti-inflammatory activity. Different niosome systems were fabricated adopting thin-film hydration technique and using the nonionic surfactant Span 60. The morphology of the prepared niosomes was characterized by scanning electron microscopy (SEM). Physical characterization by differential scanning calorimetry, X-ray powder diffraction and Fourier transform infrared spectroscopy were conducted for the optimized formula (F5) that was selected on the basis of percent entrapment efficiency, vesicular size and total lipid content. F5 was formulated as 1% w/w Carpobol 934 gel. Pharmacokinetic parameters of FBP were investigated following ocular administration of F5-loaded gel system, F5 niosome dispersion or the corresponding FBP ocular drops to albino rabbits dispersion. Anti-inflamatory effect of F5-loaded carbopol gel was investigated by histopathological examination of the corneal tissue before and after the treatment of inflamed rabbit eye with the system. Results showed that cholesterol content, surfactant type. and total lipid contents had an apparent impact on the vesicle size of the formulated niosomes. Physical characterization revealed reduced drug crystallinity and incidence of interaction with other niosome contents. F5-loaded gel showed higher C, area under the curve (AUC), and thus higher ocular bioavailability than those of the corresponding FBP ocular solution. F5-loaded gel showed a promising rapid anti-inflammatory effect in the inflamed rabbit eye. These findings will eradicate the necessity for frequent ocular drug instillation and thus, improve patient compliance.

Enhancement of Dissolution Characteristics of Clopidogrel Bisulphate by Proniosomes

“…FTIR spectrum of the selected proniosomal formula exhibited the characteristics peaks of clopidogrel that con firmed the absence of any chemical interactions between clopidogrel and other excipients [12]. Reduced-intensity and minor shifting of the characteristic peaks of clopidogrel may be explained on the basis of formation of Van der Wall forces, hydrogen bonds or dipole-dipole interactions between clopidogrel and other proniosome contents leading to the formation of stable proniosomal vesicles with high entrapment efficiency of the drug [49].…”

“…The characteristic peaks of cholesterol appeared at 3400 cm -1 (OH stretching) and the observed bands between 2800-3000 cm −1 are due to asymmetric and symmetric stretching vibrations of CH2 and CH3 groups. [49]. FTIR spectrum of maltodextrin showed an absorption band at 3399 cm -1 for OH group, a strong broadband between 980 cm -1 and 1200 cm -1 which is the most characteristic band for polysaccharides.…”

“…The plain proniosomes exhibited an appearance of a new endothermic peak at 191.1 °C. That may be explained on the basis of interaction of the proniosome components during the formation of the lipid bilayer [49]. The chosen proniosomal formula (F1) showed the shift of the endothermic peak of the lipid bilayer to 199 °C and disappearance of the endothermic peak of clopidogrel.…”

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

“…The gel network probably creates a diffusion barrier for the drug, which results in lowering the drug release rate. Previous reports showed that vesicular carriers dispersed in gel preparations had slower drug release rates compared with the vesicular dispersions [52,53].…”

Niosomes: a review of their structure, properties, methods of preparation, and medical applications

“…Therefore, to enhance the ocular bioavailability of flurbiprofen, the drug was encapsulated in niosomes consisting of nonionic surfactant Span 60 using the thin-film hydration technique. The encapsulated flurbiprofen was found to rapidly reduce eye inflammation of New Zealand albino rabbits, with a higher ocular bioavailability than that of a flurbiprofen solution [99].…”