Title
Amorphous binary dispersions of chloramphenicol in enantiomeric pure and racemic poly-lactic acid: Morphology, molecular relaxations, and controlled drug release
Date Issued
10 September 2019
Access level
open access
Resource Type
journal article
Author(s)
Valenti S.
Diaz A.
Romanini M.
Puiggalí J.
Tamarit J.L.
Macovez R.
Universitat Politècnica de Catalunya
Publisher(s)
Elsevier B.V.
Abstract
We characterize amorphous solid dispersions (ASDs) of the Chloramphenicol antibiotic in two biodegradable polylactic acid polymers, namely a commercial sample of enantiomeric pure PLLA and a home-synthesized PDLLA copolymer, investigating in particular the effect of polylactic acid in stabilizing the amorphous form of the drug and controlling its release (e.g. for antitumoral purposes). Broadband dielectric spectroscopy and differential scanning calorimetry are employed to study the homogeneity, glass transition temperature and relaxation dynamics of solvent-casted ASD membranes with different drug concentrations. We observe improved physical stability of the ASDs with respect to the pure drug, as well as a plasticizing effect of the antibiotic on the polymer, well described by the Gordon-Taylor equation. The release of the active pharmaceutical ingredient from the films in a simulated body fluid is studied by UV/vis spectroscopy at two different drug concentrations (5 and 20% in weight). The amount of released drug is found to be proportional to the square root of time, with proportionality constant that is almost the same in both dispersions, despite the fact that the relaxation time and thus the viscosity of the two samples differ by four orders of magnitude at body temperature. Since the drug release kinetics does not display a significant dependence on the drug content in the carrier, it may be expected to remain roughly constant during longer release times.
Volume
568
Language
English
OCDE Knowledge area
Química medicinal
Scopus EID
2-s2.0-85069967494
PubMed ID
Source
International Journal of Pharmaceutics
ISSN of the container
03785173
Sponsor(s)
This work has been partially supported by the Spanish Ministry of Economy and Competitiveness MINECO through the projects FIS2017-82625-P and RTI2018-101827-B-I00 , and by the Generalitat de Catalunya under the project 2017SGR-42 .
Sources of information: Directorio de Producción Científica Scopus