ArticlePharmaceutical research2018
Surface Enrichment and Depletion of the Active Ingredient in Spray Dried Amorphous Solid Dispersions.
Article in Pharmaceutical research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
10 citing papers in PubMed.
- Crystallization Inhibition and Solid-State Stability in High Drug Loaded Amorphous Drug-Polymer Dispersions Above the Overlap Concentration.Pharmaceutical research · 2026Review
- Ultrahigh-concentration biologic therapeutics enabled by spray drying with a glassy surfactant excipient.Science translational medicine · 2025Article
- Advances in the development of amorphous solid dispersions: The role of polymeric carriers.Asian journal of pharmaceutical sciences · 2023Review
- Pulmonary Drug Delivery of Antimicrobials and Anticancer Drugs Using Solid Dispersions.Pharmaceutics · 2021Review
- Hierarchical Particle Approach for Co-Precipitated Amorphous Solid Dispersions for Use in Preclinical In Vivo Studies.Pharmaceutics · 2021Article
- Water-Induced Phase Separation of Spray-Dried Amorphous Solid Dispersions.Molecular pharmaceutics · 2020Article
- A Single Hydrogen to Fluorine Substitution Reverses the Trend of Surface Composition Enrichment of Sorafenib Amorphous Solid Dispersion upon Moisture Exposure.Pharmaceutical research · 2019Article
- Advances in coamorphous drug delivery systems.Acta pharmaceutica Sinica. B · 2019Article
- Formulation and Manufacturing of Solid Dosage Forms.Pharmaceutical research · 2018Article
- Qualitative and Quantitative Characterization of Composition Heterogeneity on the Surface of Spray Dried Amorphous Solid Dispersion Particles by an Advanced Surface Analysis Platform with High Surface Sensitivity and Superior Spatial Resolution.Molecular pharmaceutics · 2018Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
purposeTo study the effects of physicochemical properties of drug and polymer, as well as the drug-polymer interactions, on the surface composition of SDDs.
methodsEthanol solutions containing a model drug (IMC, NMP or FCZ) and a model polymer (PVPK12, PVPK30 or PVP-VA) were spray dried, and the surface composition of SDDs was analyzed by XPS. The surface tensions of pure components and their solutions were measured using Wilhelmy plate and/or calculated using ACD/Labs. NMR and DLS were used to obtain the diffusion coefficients of IMC, NMP, PVPK12 and PVPK30 in solvents. Flory-Huggins interaction parameters for selected drug-polymer pairs were obtained using a melting point depression method.
resultsSignificant surface enrichment or depletion of the drug was observed in SDDs depending on the particular drug-polymer combination. With PVP as the dispersion polymer, IMC and NMP were surface enriched; whereas FCZ, a hydrophilic drug, was surface depleted. With increasing PVP molecular weight, the surface drug concentration increased, and the effect was greater in the NMP/PVP and FCZ/PVP systems than in the IMC/PVP system where strong drug-polymer interaction existed. Changing the polymer from PVP to PVP-VA reduced the surface concentration of the drug.
conclusionsThe surface concentration of a SDD can be significantly different from the bulk concentration. The main results of this work are consistent with the notion that the relative surface tensions control surface enrichment or depletion. Besides, the relative diffusion rates of the components and the strength of their interactions may also affect the surface composition of the SDDs.
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Registered trials
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