Copolymers in Formulations: Improving Solubility, Bioavailability, and Anticancer Activity of Molecules

Hydrophobicity remains a major barrier for many bioactive natural products and small molecules in medicinal and pharmaceutical chemistry. Poor aqueous solubility can limit dissolution, permeability, formulation options, and ultimately bioavailability, slowing translation from promising in vitro activity to clinically relevant outcomes. Several polymers, such as Pluronic (poloxamer) triblock copolymers, offer a biocompatible platform that can self-assemble into micelles, vesicles, and other nanostructures, improving the apparent solubility and stability of hydrophobic compounds. Recent examples, such as phthalocyanines, porphyrins, and natural compounds, were prepared via the solid dispersion method and characterized by morphological, spectroscopic, and thermal analysis. The results reveal that formulations can enhance biological performance, including increased cytotoxicity in cancer cell models (e.g., MCF-7). This RT addresses this translational gap.

This Research Topic aims to bring together formulation scientists, medicinal chemists, and translational researchers working on copolymer-based carriers for hydrophobic molecules and drug candidates. We seek contributions that connect formulation design (polymer selection, loading strategy) with quality attributes (encapsulation efficiency, size distribution, stability, release behavior and stability) and pharmacologically relevant outcomes (cellular uptake, cytotoxicity, mechanism, safety). Submissions should go beyond “it dissolves better” and clarify why a formulation works, including drug–polymer interactions and performance under biologically realistic conditions (serum, dilution, storage). We also encourage manuscripts that address reproducibility and translation, such as scale-up readiness, long-term stability, and standardized reporting. The overall goal is to accelerate practical, defensible delivery strategies that improve the developability of hydrophobic bioactives.

We welcome Original Research, Review, Mini Review and Perspective articles on themes including, but not limited to:
• Copolymers for hydrophobic molecules and natural products
• Methods for copolymers-based drug incorporation
• Encapsulation efficiency and drug loading optimization strategies
• Drug–polymer interactions via FTIR, DSC, TGA, and spectroscopy
• DLS and complementary methods for size, PDI, and stability
• Release kinetics modeling and in vitro–relevant dissolution testing
• Cytotoxicity studies in cancer cell models, including MCF-7
• Mechanistic assays: apoptosis, cell cycle, ROS, and signalling
• Cellular uptake and permeability impacts of micellar formulations
• Serum, dilution, and storage stability of copolymeric systems
• Safety profiling: hemocompatibility and off-target cytotoxicity assessment
• Scale-up, reproducibility, and quality attributes for translation

Article types and fees

This Research Topic accepts the following article types, unless otherwise specified in the Research Topic description:

• Editorial
• FAIR² Data
• FAIR² DATA Direct Submission
• Mini Review
• Opinion
• Original Research
• Perspective
• Review

Articles that are accepted for publication by our external editors following rigorous peer review incur a publishing fee charged to Authors, institutions, or funders.

Article types

This Research Topic accepts the following article types, unless otherwise specified in the Research Topic description:

• Editorial
• FAIR² Data
• FAIR² DATA Direct Submission
• Mini Review
• Opinion
• Original Research
• Perspective
• Review

Keywords: Copolymers, hydrophobic molecules, solubility enhancement, bioavailability, anticancer activity synthesis

Important note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.