ReviewMolecules (Basel, Switzerland)2015
Polymorph Impact on the Bioavailability and Stability of Poorly Soluble Drugs.
Review in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 113 papers.
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Who cites it
113 citing papers in PubMed.
- Systematic Scale-Up of Mechanochemical Paracetamol-Oxalic Acid Cocrystal Synthesis across Multiple Milling Technologies.Organic process research & development · 2026Article
- Form (III) of artemisinin: discovery and crystallographic characterization of a new high-pressure polymorph.Acta crystallographica Section B, Structural science, crystal engineering and materials · 2026Article
- In situ ptychographic x-ray nanotomography of temperature-controlled crystallization processes.Nature communications · 2026Article
- Mechanistic Insights into Molecular Modifiers That Promote Urate Crystallization through Solute Assembly Regulation.JACS Au · 2026Article
- Formulation of Metformin-Loaded Chitosan Nanoparticles and In Vivo Evaluation of Its Hypoglycemic Effects.Molecules (Basel, Switzerland) · 2026Article
- Assessment and Optimization of Force Fields for Glycine Polymorphism and Solution Properties.Journal of chemical theory and computation · 2026Article
- A study on the stability of ritonavir form III processed in orbit and returned to Earth.NPJ microgravity · 2026Article
- Crystal engineering for poorly water-soluble drugs: From design to applications.Acta pharmaceutica Sinica. B · 2026Review
- Multicomponent Salts of the Antidiabetic Agent Saxagliptin: Hydration-Assisted Assembly and Lipophilic Aggregation with Carboxylic Acids.ACS omega · 2026Article
- Comparative pharmacoinformatic and quantum descriptor insights from BFM/GBTLI guidelines to phase I/II compounds for acute lymphoblastic leukemia (ALL).Scientific reports · 2026Article
- Article
- Influence of Drying Methods on Redispersibility and Dissolution of Canagliflozin Nanocrystals: A Comparative Approach.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Investigation of Transdermal Drug Delivery and In Vivo Pharmacokinetics of Choline Ketoprofen Ionic Liquid.ACS materials Au · 2026Article
- Study on Dual-Targeted Liposomes Containing Curcumin-Copper Chelate in the Treatment of Triple-Negative Breast Cancer.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Duality of Simplicity and Accuracy in QSPR: A Machine Learning Framework for Predicting Solubility of Selected Pharmaceutical Acids in Deep Eutectic Solvents.Molecules (Basel, Switzerland) · 2025Article
- Genarris 3.0: Generating Close-Packed Molecular Crystal Structures with Rigid Press.Journal of chemical theory and computation · 2025Article
- 3D conformation and crystal interaction insights into drug development challenges for HCV drug analogues via molecular simulations.Communications chemistry · 2025Article
- NMR Crystallographic Investigation Coupled with Molecular Dynamics Simulations Reveals the Nature of Disorder in Chlorpromazine Hydrochloride Solvatomorphs.Molecular pharmaceutics · 2025Article
- Polymorphism and Phase-Transition Thermodynamic Properties of Phenazone (Antipyrine).Molecules (Basel, Switzerland) · 2025Article
- Article
53 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
2 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Drugs with low water solubility are predisposed to poor and variable oral bioavailability and, therefore, to variability in clinical response, that might be overcome through an appropriate formulation of the drug. Polymorphs (anhydrous and solvate/hydrate forms) may resolve these bioavailability problems, but they can be a challenge to ensure physicochemical stability for the entire shelf life of the drug product. Since clinical failures of polymorph drugs have not been uncommon, and some of them have been entirely unexpected, the Food and Drug Administration (FDA) and the International Conference on Harmonization (ICH) has required preliminary and exhaustive screening studies to identify and characterize all the polymorph crystal forms for each drug. In the past, the polymorphism of many drugs was detected fortuitously or through manual time consuming methods; today, drug crystal engineering, in particular, combinatorial chemistry and high-throughput screening, makes it possible to easily and exhaustively identify stable polymorphic and/or hydrate/dehydrate forms of poorly soluble drugs, in order to overcome bioavailability related problems or clinical failures. This review describes the concepts involved, provides examples of drugs characterized by poor solubility for which polymorphism has proven important, outlines the state-of-the-art technologies and discusses the pertinent regulations.
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