A Novel Stabilizing Approach to Improve the Manufacturing of Biodegradable Microparticles Entrapping Plasticizing Active Molecules: the Case of 4-Methoxychalcone View Full Text


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Article Info

DATE

2018-09-07

AUTHORS

Danyela Francine Benvenutti, Tania Mari Bellé Bresolin, Rogerio Corrêa, Stefano Giovagnoli, Riccardo Vivani, Maurizio Ricci

ABSTRACT

The microencapsulation of plasticizing molecules, such as 4-methoxy chalcone (4MC), can raise serious stability issues in microparticle (MP) manufacturing and storage, especially when employing low glassy pseudo-plastic polymers, such as polylactides (PLA) and polylactide-co-glycolides (PLGA). In this work, two distinct steps were undertaken: (1) the study of the effect on manufacturing and storage of 4MC loading in polyester MP and (2) the investigation of a new stabilization strategy based on 4MC intercalation into a stearate-modified hydrotalcite (sHTC). 4MC was loaded up to 20% w/w in PLA and PLGA MP by a W/O emulsion solvent extraction/evaporation method. Likewise, the 4MC-sHTC intercalation compound was prepared and loaded in the MP in the same conditions using a W/O/W double-emulsion method. All preparations were characterized by spectrophotometry, thermal analysis, x-ray powder diffraction (XRPD), scanning electron microscopy (SEM), and energy-dispersive x-ray spectroscopy (EDX) and for their particle size, in vitro drug release profile and kinetics. Storage stability was assessed over 8 months of incubation at room temperature (rt) and 30% relative humidity (RH). The obtained 4MC-loaded MP showed a non-straightforward loading-dependent change of size, morphology, and release behavior. 4MC loading caused extensive clumping and poor MP recovery. Thermal and XRPD analyses confirmed a strong plasticizing effect of 4MC that, in some cases, segregated as crystals on the particle surface. Plasticization was inversely related to drug release. The loading of 4MC as a sHTC intercalation compound granted increased stability upon manufacturing and SEM-EDX evidenced a loading effect on porosity and the 4MC-sHTC distribution inside the MP. A remarkable stability increase was observed over 8 months storage at rt and 30% RH with no changes in the outer and inner MP morphology and compound distribution. The use of sHTC could be a useful stabilization strategy to improve manufacturing of biodegradable MP, surely worthy of further investigation in order to be extended to other MP drug delivery systems. More... »

PAGES

1-17

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s12247-018-9346-9

DOI

http://dx.doi.org/10.1007/s12247-018-9346-9

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1106855855


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Download the RDF metadata as:  json-ld nt turtle xml License info

HOW TO GET THIS DATA PROGRAMMATICALLY:

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curl -H 'Accept: application/ld+json' 'https://scigraph.springernature.com/pub.10.1007/s12247-018-9346-9'

N-Triples is a line-based linked data format ideal for batch operations.

curl -H 'Accept: application/n-triples' 'https://scigraph.springernature.com/pub.10.1007/s12247-018-9346-9'

Turtle is a human-readable linked data format.

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RDF/XML is a standard XML format for linked data.

curl -H 'Accept: application/rdf+xml' 'https://scigraph.springernature.com/pub.10.1007/s12247-018-9346-9'


 

This table displays all metadata directly associated to this object as RDF triples.

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