Tailoring structural properties of spray-dried methotrexate-loaded poly (lactic acid)/poloxamer microparticle blends

• Published in: Journal of materials science. Materials in medicine Vol. 30; no. 1; p. 12
• Main Authors: de Oliveira, Edilene Gadelha, Machado, Paula Renata Lima, Farias, Kleber Juvenal Silva, da Costa, Tiago R., Melo, Dulce Maria Araújo, Lacerda, Ariane Ferreira, de Freitas Fernandes-Pedrosa, Matheus, Cornélio, Alianda Maira, da Silva-Junior, Arnóbio Antônio
• Format: Journal Article
• Language: English
• Published: New York Springer US 01-01-2019; Springer Nature B.V
• Subjects: Aqueous solutions; Biocompatibility; Biomaterials; Biomaterials Synthesis and Characterization; Biomedical Engineering and Bioengineering; Biomedical materials; Calorimetry; Cancer; Ceramics; Chemistry and Materials Science; Chemotherapy; Composites; Cytology; Differential scanning calorimetry; Drug delivery; Drug delivery systems; Drug resistance; Formulations; Fourier transforms; Glass; Hydrophobicity; In vivo methods and tests; Leaching; Materials Science; Methotrexate; Micelles; Microparticles; Miscibility; Mixtures; Morphology; Natural Materials; Particle size; Poloxamers; Polylactic acid; Polymer Sciences; Regenerative Medicine/Tissue Engineering; Structure-function relationships; Surfaces and Interfaces; Thin Films; X-ray diffraction
• ISSN: 0957-4530; 1573-4838
• DOI: 10.1007/s10856-018-6214-6

Drug delivery systems can overcome cancer drug resistance, improving the efficacy of chemotherapy agents. Poly (lactic acid) (PLA) microparticles are an interesting alternative because their hydrophobic surface and small particle size could facilitate interactions with cells. In this study, two poloxamers (PLX 407 and 188) were applied to modulate the structural features, the drug release behavior and the cell viability from spray-dried microparticles. Five formulations with different PLA: PLX blend ratio (100:0, 75:25, 50:50, 25:50, and 0:100) were well-characterized by SEM, particle size analysis, FTIR spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction analysis (XRD). The spray-dried microparticles showed higher drug loading, spherical-shape, and smaller particle size. The type of poloxamer and blend ratio affected their structural and functional properties such as morphology, crystallinity, blend miscibility, drug release rate, and cell viability. The methotrexate (MTX), a model drug, was loaded in amorphous spray-dried microparticles. Moreover, the drug release studies demonstrated that PLX induced a leaching-effect of MTX from PLA: PLX blends, suggesting the formation of MTX/PLX micelles in aqueous medium. This finding was better established by cell viability assays. Therefore, biocompatible PLA: PLX blends showed promising in vitro results, and further in vivo studies will be performed to evaluate the performance of this chemotherapeutic agent.