ArticlePharmaceutical research2025
Development of a Melting Point Depression Method to Measure the Solubility of a Small-Molecule Drug in Poly-Lactic-co-Glycolic Acid (PLGA).
Article in Pharmaceutical research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed.
- Tabletting of single-screw hot melt extruded itraconazole: HPMC-AS amorphous solid dispersion by 3D printing and direct compression.Drug delivery and translational research · 2026Article
- Application of PLCL as a biodegradable polymer in biomedical engineering.Journal of materials science. Materials in medicine · 2026Review
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Authors and funding
2 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe solubility of a crystalline drug in a polymer is commonly determined by measuring melting point depression with differential scanning calorimetry (DSC). The accuracy of this measurement depends on rapid dissolution of the drug into the molten polymer during the DSC heating scan. A preferred method of accelerating this dissolution process is to preblend the drug and polymer by cryo-milling. However, cryo-milling may be unsuitable for water-sensitive drugs or polymers such as poly(lactic-co-glycolic acid) (PLGA). The purpose of this study was to develop a PLGA-specific melting point depression method that did not require a cryo-milling operation.
methodsA three-step DSC method was used to measure the solubility of a small-molecule drug, voriconazole, in amorphous PLGA (Resomer ® RG 502H). First, drug/PLGA powder mixtures of multiple drug loadings were melted and rapidly cooled to form glassy solid solutions. Second, these solid solutions were heated above their T
resultsThe crystallization procedure generated the desired drug polymorph and likely generated small, well-mixed crystalline drug particles, as the drug dissolved rapidly into the molten polymer during melting point depression scans. Drug/PLGA solubility temperatures were determined with confidence between 40 - 100% drug loading. The solubility curve was extrapolated to lower drug loadings using the Flory-Huggins model.
conclusionThis technique can assist product development of high-drug-loaded PLGA products, particularly those manufactured by melt extrusion.
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