| Autor: |
Cruz-Zazueta, Isabel, Arias-Durán, Luis, Estrada-Soto, Samuel, Piñón-Segundo, Elizabeth, Herrera-Ruiz, Dea, Alcalá-Alcalá, Sergio |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
International Journal of Pharmaceutics. 628:122295 |
| ISSN: |
0378-5173 |
| DOI: |
10.1016/j.ijpharm.2022.122295 |
| Popis: |
Poly(latic-co-glycolic) acid (PLGA) nanoparticles loaded with felodipine (FEL) were embedded in a mucoadhesive matrix of poly (methyl vinyl ether-co-maleic anhydride) (PVM/MA) to prepare micro-nanoparticulate composites by particle engineering. Composites were characterized for physical and rheological properties and formulated with inhalable grade lactose. In-vitro characterization studies such as drug release kinetics, and mucoadhesive, and aerodynamic properties were performed. The in-vivo efficacy was evaluated by administering the optimized composites by nebulization in hypertensive rats. The obtained FEL-PLGA-PVM/MA composites of 1,069 ± 82 nm showed sustained drug release and mucoadhesive properties. Bulk and tapped densities of composites mixed with lactose were 0.08-0.13 g/mL and 0.18-0.30 g/mL, respectively, with mass median aerodynamic diameters (MMAD) in a range of 1.29-12.0 µm. After pulmonary administration of the composites, a decrease in systolic and diastolic blood pressure was observed within the first 3 h, of -9.0 ± 1.3 % and -13.9 ± 3.3 %, respectively, with a maximal effect at 12 h (sustained during 144 h), in contrast to pure FEL, which showed no significant decrease in blood pressure (1.6 ± 2.7 % and 4.1 ± 4.1 %). Findings suggest that novel mucoadhesive FEL-PLGA-PVM/MA composites are a promising strategy formulation to treat systemic diseases by pulmonary route. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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Full Text from ScienceDirect