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<p>A biocompatible nanoporous calcium tartrate (CaT)-based bio-metal–organic framework (bioMOF) was successfully synthesized via a one-pot aqueous method in the presence of glutamine (Glu) and palbociclib (PAL), acting as a structure-directing agent and therapeutic cargo, respectively. The synthesis was performed under mild alkaline conditions at room temperature using ligand: metal molar ratios of 1:1 and 2:1. Morphological and structural analyses confirmed the formation of well-defined crystalline frameworks with Glu-mediated size reduction and improved particle dispersion. The system exhibited high PAL loading efficiency, approaching ~ 100% within 15&#xa0;min of synthesis. In vitro drug release studies demonstrated a pronounced pH-responsive behavior, with approximately 100% PAL release achieved within 24&#xa0;h at pH 5.5, while only ~ 60% release was observed at pH 7.4 over the same period. Kinetic modeling using multiple mathematical models revealed that the Korsmeyer–Peppas model provided the best fit, indicating anomalous transport at physiological pH and diffusion-dominated release under acidic conditions. Cytotoxicity evaluation using the MTT assay revealed minimal toxicity of the carrier (CaT and Glu@CaT) toward NIH/3T3 fibroblast cells up to high concentrations, confirming its biocompatibility. In contrast, free PAL exhibited cytotoxic effects on B16 melanoma cells starting from low concentrations (~ 13.9&#xa0;µg/mL), whereas Glu/PAL@CaT formulations showed a controlled and concentration-dependent cytotoxic profile. Notably, the 2:1 formulation maintained low toxicity toward normal cells even at higher concentrations (up to 500&#xa0;µg/mL), while preserving anticancer activity. The enhanced selectivity of the nanoformulation compared to free drug is attributed to its controlled release behavior and improved drug dispersion within the MOF matrix. Overall, the developed Glu/PAL@CaT system demonstrates a combination of high drug loading, pH-responsive release, and selective cytotoxicity, highlighting its potential as a non-invasive platform for localized skin cancer therapy. The micrometer-scale particle size further supports its suitability for topical delivery systems such as transdermal patches, enabling site-specific drug activation in the tumor microenvironment.</p>

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One-pot green synthesis of a glutamine-modified calcium tartrate bio-metal-organic framework for pH-responsive delivery of palbociclib in skin cancer therapy

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年6月21日

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  • Mergan Haghshenas,
  • Maryam Tohidi,
  • Banafsheh Rastegari

摘要

A biocompatible nanoporous calcium tartrate (CaT)-based bio-metal–organic framework (bioMOF) was successfully synthesized via a one-pot aqueous method in the presence of glutamine (Glu) and palbociclib (PAL), acting as a structure-directing agent and therapeutic cargo, respectively. The synthesis was performed under mild alkaline conditions at room temperature using ligand: metal molar ratios of 1:1 and 2:1. Morphological and structural analyses confirmed the formation of well-defined crystalline frameworks with Glu-mediated size reduction and improved particle dispersion. The system exhibited high PAL loading efficiency, approaching ~ 100% within 15 min of synthesis. In vitro drug release studies demonstrated a pronounced pH-responsive behavior, with approximately 100% PAL release achieved within 24 h at pH 5.5, while only ~ 60% release was observed at pH 7.4 over the same period. Kinetic modeling using multiple mathematical models revealed that the Korsmeyer–Peppas model provided the best fit, indicating anomalous transport at physiological pH and diffusion-dominated release under acidic conditions. Cytotoxicity evaluation using the MTT assay revealed minimal toxicity of the carrier (CaT and Glu@CaT) toward NIH/3T3 fibroblast cells up to high concentrations, confirming its biocompatibility. In contrast, free PAL exhibited cytotoxic effects on B16 melanoma cells starting from low concentrations (~ 13.9 µg/mL), whereas Glu/PAL@CaT formulations showed a controlled and concentration-dependent cytotoxic profile. Notably, the 2:1 formulation maintained low toxicity toward normal cells even at higher concentrations (up to 500 µg/mL), while preserving anticancer activity. The enhanced selectivity of the nanoformulation compared to free drug is attributed to its controlled release behavior and improved drug dispersion within the MOF matrix. Overall, the developed Glu/PAL@CaT system demonstrates a combination of high drug loading, pH-responsive release, and selective cytotoxicity, highlighting its potential as a non-invasive platform for localized skin cancer therapy. The micrometer-scale particle size further supports its suitability for topical delivery systems such as transdermal patches, enabling site-specific drug activation in the tumor microenvironment.