Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation

Abstract

<jats:p>Nebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formulas with the absence or presence of four different polymers were prepared and evaluated. In-vitro precipitation assay was performed to assess the precipitation inhibition capacity of polymers. The ex-vivo permeation through rat intestinal mucosa was also conducted for determination of permeability parameters. Results revealed that (Su-SNA formula SAS1) containing 5% soluplus could effectively retard the nebivolol precipitation. There was no statistical difference between formula A and SAS1; both maintained a higher apparent NBH concentra­tion for approximately 240 min in 0.1N HCl. The permeation rate of conventional (formula A) and soluplus-based Su-SNE (formula SAS1) was significantly improved, and the permeation enhancement ratio was found 2.7 and 3.2, respectively, as compared with non-formulated NBH. Consequently, it is concluded that developing soluplus-based nebivolol SNE is a promising alternative approach. It can enhance nebivolol stability and permeability with half the amount of conventional SNE components.</jats:p>

Study the Variables Affecting Formulation of Ethylcellulose-based Microsponges Loaded with Clobetasol

“…The IR spectrum was recorded using FTIR (FTIR600; Shimadzu, Japan). The sample was directly placed onto a modified crystal on FTIR instrument without any previous sample preparation, and the FTIR spectra were collected in the range of 4000-400 cm − 1 (14,15) .…”

Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

“…Each stable formula was diluted with deionized water 100 times while being stirred with a magnetic stirrer at 37 °C to create fine nanoemulsion. The resulting particle size of each nanoemulsion was examined using the dynamic light scattering method utilizing a particle size analyzer device (Malvern zetasizer, USA), and the PDI was subsequently determined (14) .…”