Fabrication of ticagrelor bioadhesive solid dispersion based on coaxial electrostatic spray to improve drug release and enhance oral bioavailability

Due to the low solubility and poor bioavailability of Ticagrelor (TIC), the current study developed a structured bioadhesive core-shell drug delivery system to address it. Ticagreior solid dispersion (T-SD) was fabricated using the uniaxial electrostatic spray method. Ticagrelor bio adhesive solid d...

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Bibliographic Details
Published in:Pakistan journal of pharmaceutical sciences 2023-01, Vol.36 (1), p.121-127
Main Authors: Liu, Hongfei, Zhang, Hui, Gu, Chunguang, Chen, Xiaoyan, Feng, Yingshu, Kesse Firempong, Caleb, He, Haibing, Sun, Changshan
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Bioavailability
Biological Availability
Chemical properties
Dosage and administration
Drug delivery systems
Drug Liberation
Drugs
Electrostatics
Methods
Pharmaceutical research
Rats
Rats, Sprague-Dawley
Solubility
Spraying
Static Electricity
Ticagrelor
Vehicles
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Summary:Due to the low solubility and poor bioavailability of Ticagrelor (TIC), the current study developed a structured bioadhesive core-shell drug delivery system to address it. Ticagreior solid dispersion (T-SD) was fabricated using the uniaxial electrostatic spray method. Ticagrelor bio adhesive solid dispersion (T-BSD) was also prepared using the coaxial electrostatic spray technique. The adhesion of T-BSD to each intestinal segment was determined using biological adhesion test. The compartment model was used to study the plasma concentration-time curve and related pharmacokinetic parameters. The results of bioadhesion tests showed a positive adhesion effect of T-BSD in each intestinal segment. The maximum plasma concentration (C ) of T-BSD was increased to 777.08ng/mL compared with the free drug (367ng/mL). Similarly, t , MRT and T of T-BSD (12.1h, 9.4h, 4h) were higher than the free drug (11.2h, 8.6h, 1h), respectively. The relative bioavailability of T-BSD was further increased to 430% compared with the free drug. The findings collectively revealed that the coaxial-electrospray technique could be a promising way to improve the bioavailability of TIC.
ISSN:1011-601X
DOI:10.36721/PJPS.2023.36.1.REG.121-127.1