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Purpose <p>Microspheres have emerged as promising carriers for site-specific and modulated delivery of poorly water-soluble drugs, especially in chronic conditions such as schizophrenia. This study focuses on the design and characterization of functionalized graphene oxide (FGO) sodium alginate–based microspheres for the effective delivery of quetiapine fumarate (QF), aiming to enhance mucoadhesion and sustain drug release for prolonged central nervous system (CNS) targeting.</p> Methods <p>In line with the purpose of the present study, microspheres were prepared by the ionic gelation technique and categorized as: blank alginate microspheres (AM), drug-loaded microspheres (QF@AM), and graphene oxide–functionalized drug-loaded microspheres (FGO/QF@AM). The formulations were characterized for particle size and morphology and further examined using FTIR, DSC, P–XRD, zeta potential, and SEM. Microspheres were evaluated for mucoadhesion studies and in vitro drug release profiling.</p> Results <p>Findings of FTIR and DSC confirmed successful QF encapsulation and GO functionalization without significant chemical interaction. SEM revealed spherical shapes for AM and QF@AM, and a wrinkled morphology for FGO/QF@AM. Encapsulation efficiency and drug loading were 78.13 ± 1.14% and 19.53 ± 1.08%, respectively. Notably, FGO/QF@AM demonstrated enhanced mucoadhesion 54 ± 1.18% at 6&#xa0;h vs. 18 ± 1.02% for AM. Drug release from FGO/QF@AM was sustained (66.25 ± 2.27% over 24&#xa0;h) in contrast to pure QF, which released 92.48 ± 1.74% within 12&#xa0;h. The drug&#xa0;release profile&#xa0;is&#xa0;best fitted&#xa0;to the Higuchi model (<i>R</i><sup>2</sup> = 0.997), indicating diffusion-controlled transport.</p> Conclusion <p>In summary, the&#xa0;FGO/QF@AM showed potential for sustained oral delivery of QF with improved mucoadhesion and controlled in vitro release, necessitating further in vivo evaluation.</p> Lay Summary <p>Treating chronic brain disorders like schizophrenia often requires long-term use of medications such as quetiapine fumarate. However, this drug does not dissolve easily in water and needs frequent doses, which can reduce patient compliance and increase drug related side effects. Our research intended to solve this by designing tiny carriers called microspheres that can gradually release the drug in the body over time. We used two natural and innovative materials to make these microspheres: sodium alginate, a gel-like substance from seaweed, and graphene oxide, a modern nanomaterial with a high surface area that helps improve drug delivery. The microspheres were made in three versions: empty (for comparison), with the drug, and with both the drug and graphene oxide. We tested the structure, drug content, surface appearance, and how the drug is released from these microspheres. The version containing graphene oxide showed a wrinkled surface, which helped it stick better to the intestinal walls. This improves the chances of the drug staying longer in the body and releasing slowly. In lab tests, the graphene oxide-enhanced microspheres released the drug steadily over 24 h, while the regular ones released most of it in just 12 h. Also, these improved microspheres stayed attached to the intestinal membrane for much longer, which can help the drug be absorbed more efficiently. In summary, our study developed a smart, natural-material-based system for slow and effective oral delivery of schizophrenia medication, which may reduce dosing frequency and improve patient outcomes.</p>

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Design and Characterization of Graphene Oxide Functionalized Alginate Microspheres for Oral Delivery of Quetiapine Fumarate

  • 期刊论文

  • 发表日期：

    2025年9月23日

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  • Bhushan P. Sonar,
  • Gaurav S. Patil,
  • Kalpeshkumar S. Wagh,
  • Pushpraj V. Kuwar,
  • Vikas P. Patil

摘要

Purpose

Microspheres have emerged as promising carriers for site-specific and modulated delivery of poorly water-soluble drugs, especially in chronic conditions such as schizophrenia. This study focuses on the design and characterization of functionalized graphene oxide (FGO) sodium alginate–based microspheres for the effective delivery of quetiapine fumarate (QF), aiming to enhance mucoadhesion and sustain drug release for prolonged central nervous system (CNS) targeting.

Methods

In line with the purpose of the present study, microspheres were prepared by the ionic gelation technique and categorized as: blank alginate microspheres (AM), drug-loaded microspheres (QF@AM), and graphene oxide–functionalized drug-loaded microspheres (FGO/QF@AM). The formulations were characterized for particle size and morphology and further examined using FTIR, DSC, P–XRD, zeta potential, and SEM. Microspheres were evaluated for mucoadhesion studies and in vitro drug release profiling.

Results

Findings of FTIR and DSC confirmed successful QF encapsulation and GO functionalization without significant chemical interaction. SEM revealed spherical shapes for AM and QF@AM, and a wrinkled morphology for FGO/QF@AM. Encapsulation efficiency and drug loading were 78.13 ± 1.14% and 19.53 ± 1.08%, respectively. Notably, FGO/QF@AM demonstrated enhanced mucoadhesion 54 ± 1.18% at 6 h vs. 18 ± 1.02% for AM. Drug release from FGO/QF@AM was sustained (66.25 ± 2.27% over 24 h) in contrast to pure QF, which released 92.48 ± 1.74% within 12 h. The drug release profile is best fitted to the Higuchi model (R2 = 0.997), indicating diffusion-controlled transport.

Conclusion

In summary, the FGO/QF@AM showed potential for sustained oral delivery of QF with improved mucoadhesion and controlled in vitro release, necessitating further in vivo evaluation.

Lay Summary

Treating chronic brain disorders like schizophrenia often requires long-term use of medications such as quetiapine fumarate. However, this drug does not dissolve easily in water and needs frequent doses, which can reduce patient compliance and increase drug related side effects. Our research intended to solve this by designing tiny carriers called microspheres that can gradually release the drug in the body over time. We used two natural and innovative materials to make these microspheres: sodium alginate, a gel-like substance from seaweed, and graphene oxide, a modern nanomaterial with a high surface area that helps improve drug delivery. The microspheres were made in three versions: empty (for comparison), with the drug, and with both the drug and graphene oxide. We tested the structure, drug content, surface appearance, and how the drug is released from these microspheres. The version containing graphene oxide showed a wrinkled surface, which helped it stick better to the intestinal walls. This improves the chances of the drug staying longer in the body and releasing slowly. In lab tests, the graphene oxide-enhanced microspheres released the drug steadily over 24 h, while the regular ones released most of it in just 12 h. Also, these improved microspheres stayed attached to the intestinal membrane for much longer, which can help the drug be absorbed more efficiently. In summary, our study developed a smart, natural-material-based system for slow and effective oral delivery of schizophrenia medication, which may reduce dosing frequency and improve patient outcomes.