Sucrose acetate isobutyrate based nanovesicles: A promising platform for drug delivery and bioavailability enhancement

• Published in: Journal of drug delivery science and technology 2020-08, Vol.58, p.101806, Article 101806
• Main Authors: Elshafeey, Ahmed Hassen, Zayed, Reham, Shukr, Marwa Hassan, Elsayed, Ibrahim
• Format: Article
• Language: English
• Subjects: Bioavailability enhancement; Lyophilization; Poloxamer; Sucrose acetate isobutyrate; Ticagrelor
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2020.101806

Sucrose acetate isobutyrate based nanovesicles (SBN) were designed to enhance the Ticagrelor poor bioavailability (36%). SBN were formulated with different ratios of sucrose acetate isobutyrate and Poloxamer 407 and tested for particle size, polydispersity index, zeta potential and entrapment efficiency. The desirable formula composed of 5.52:1 surfactant: drug ratio and 0.1:1 sucrose acetate isobutyrate: Poloxamer 407 ratio with 0.77 desirability value as determined by the Design-Expert® software. Then, the optimized formula was lyophilized and compressed into tablets to maintain its physical stability and facilitate the oral administration. The lyophilized formula and the compressed nanostructed tablets were tested for the in vitro drug release versus the pure drug powder and the marketed product (Brilique®), where a significant enhancement in the drug dissolution rate and extent was observed, either in the sink or non-sink conditions. Based on the pharmacokinetic study conducted on rabbits, the nanostructured tablets showed a significant increase in the drug absorption extent expressed by an area under the plasma concentration-time curve of 4163.52 ng h/mL where the latter for the marketed product was only 2824.16 ng h/mL. In conclusion, the prepared nanostructed tablets achieved 150% relative bioavailability assuring the enhancement of TR solubility and absorption after being loaded into the optimized SBN formula. [Display omitted]