Vasorelaxant effect of standardized extract of Cecropia glaziovii Snethl encapsulated in PLGA microparticles: In vitro activity, formulation development and release studies

In this study, the standardized dry extract of C. glaziovii (SDE) provided a significant vasorelaxant effect after contractions induced by phenylephrine in rat aortic rings in an endothelium-dependent manner, confirming that endothelial factors are needed to stimulate this response. A vasorelaxation...

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Bibliographic Details
Published in:Materials Science & Engineering C 2018-11, Vol.92, p.228-235
Main Authors: dos Santos, Talitha Caldas, Battisti, Mariana Alves, Lobo, Kiuanne Lino, Caon, Thiago, Linder, Aurea Elizabeth, Sonaglio, Diva, de Campos, Angela Machado
Format: Article
Language:English
Subjects:
Acetylcholine
Analysis of Variance
Aorta
Cecropia glaziovii Snethl
Cecropia Plant - chemistry
Controlled release
Design of experiments
Drug Compounding
Drug Liberation
Encapsulation
Endothelium
Experimental design
External pressure
Extraction processes
Formulations
Herbal medicine
Materials science
Microparticles
Microspheres
Osmosis
Osmotic effect
Osmotic pressure
Particle Size
Particle size distribution
Pharmacology
Phenylephrine
Plant Extracts - pharmacology
Polylactic Acid-Polyglycolic Acid Copolymer
Polylactide-co-glycolide
Pressure effects
Reference Standards
Release studies
Response surface design
Size distribution
Sodium chloride
Sustained release
Vasodilation
Vasodilation - drug effects
Vasodilator Agents - pharmacology
Vasorelaxant activity
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Summary:In this study, the standardized dry extract of C. glaziovii (SDE) provided a significant vasorelaxant effect after contractions induced by phenylephrine in rat aortic rings in an endothelium-dependent manner, confirming that endothelial factors are needed to stimulate this response. A vasorelaxation close to that of acetylcholine was achieved, justifying the development of new formulations for this plant material. In this context, microparticles were selected to encapsulate SDE and the double emulsion technique was considered because of the hydrophilic nature of plant material. Two experimental designs were applied. Firstly, the effect of formulation parameters on particle size, size distribution and encapsulation efficiency (EE) was evaluated. As low EE was achieved, the effect of the osmotic pressure of the external phase was evaluated in a second experimental design. The presence of the osmotic agent (NaCl) impacted positively on the EE and slower in vitro release profile was obtained, which is desired in controlled release systems. The formation of denser and less porous particle surface, which was identified by SEM analysis, contributes to explain these findings. Microstructures showed to be a promising delivery system for the C. glaziovii SDE considering that a sustained release was achieved. •The standardized extract of C. glaziovii showed a significant vasorelaxation effect.•An endothelium-dependent vasorelaxation effect was observed for the extract.•Two experimental designs were applied to develop microparticles of C. glaziovii.•The presence of an osmotic agent impacted positively on the EE.•A denser and less porous particle surface led to a sustained release.
ISSN:0928-4931
1873-0191
DOI:10.1016/j.msec.2018.06.046