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Background <p>Ofloxacin has a shorter gastric residence time and poor solubility, which hinders its effectiveness. Using floating microspheres may enhance the solubility and gastric retention of ofloxacin, thus enhancing its therapeutic efficacy.</p> Objectives <p>This study aimed to formulate and evaluate Ofloxacin-loaded floating microspheres to address the limitations of conventional dosage forms. The microspheres were designed to enhance gastric retention, provide sustained drug release, and improve the bioavailability of Ofloxacin. Key objectives included assessing their physicochemical properties, buoyancy, drug release profile, and antibacterial activity to ensure effective and prolonged therapeutic action. This study uniquely couples a sodium-alginate/chitosan–CaCO₃ formulation strategy with mechanistic kinetic modelling, ex vivo porcine intestinal permeation, antimicrobial efficacy, and six-month stability data to explain why the F3 composition provides superior buoyancy and sustained release.</p> Methods <p>To formulate the microspheres, polymers such as sodium alginate and chitosan were used during the emulsion solvent diffusion process. Sodium alginate and chitosan were selected for their complementary gel-forming, mucoadhesive, and sustained-release properties, which enhance gastric retention and improve drug bioavailability. Before the floating microspheres were used for additional research, they were subjected to multiple inspections. Pre-formulation studies drug-excipient compatibility testing, rheological property evaluation, drug content quantification, and drug entrapment efficiency calculations, were a few of these. The form, swelling index, and in vitro buoyancy of the microspheres were also assessed using scanning electron microscopy. Drug release and diffusion studies were conducted in vitro, followed by ex vivo permeation and antibacterial trials. Next, the stability of the microspheres during storage was examined.</p> Results <p>The emulsion solvent diffusion technique was employed to prepare floating microspheres of ofloxacin using various polymers. FTIR spectroscopy and DSC results depicted no chemical interaction between the drug and polymers. The encapsulation index, drug content, and In vitro buoyancy studies were found to be 60.4 ± 1.8 for F1, 66 ± 2.1% for F2, 74 ± 2.56% for F3, while drug content readings were160 mg for F1, 180&#xa0;mg for F2 and 210&#xa0;mg for F3, and similarly in vitro buoyancy gave 37 ± 2.5% for F1, 50 ± 2.3% for F2 and 72 ± 1.67% for F3 respectively. The formulated microsphere exhibited good rheological properties with a swelling index ranging between 225% and 300%. SEM studies showed that floating microspheres were spherical with regular surfaces. In vitro, release studies revealed that the F3 formulation followed the Korsemeyer’s Peppas model with good ex vivo release of 72.7. The F3 formulation had good antimicrobial properties compared to other formulations.</p> Conclusion <p>The drug ofloxacin was subjected to Preformulation experiments to establish its physical and chemical characteristics, solubility, and compatibility with excipients. The drug encapsulation efficiency, in vitro and ex vivo release, micrometric characteristics, and storage stability of a floating microsphere formulation were all investigated, from which the F3 formulation proved to be the best. Also, antimicrobial test verified its effectiveness against Staphylococcus aureus and P. aeruginosa, among others.</p>

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Optimization and Characterization of Sodium Alginate–Chitosan Based Floating Microspheres of Ofloxacin: In Vitro Evaluation and Antibacterial Efficacy

  • 期刊论文

  • 发表日期：

    2025年12月20日

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  • Deepshi Arora,
  • Yugam Taneja,
  • Ashwani Dhingra,
  • Prerna Sharma,
  • Nidhi Rani,
  • Thakur Gurjeet Singh

摘要

Background

Ofloxacin has a shorter gastric residence time and poor solubility, which hinders its effectiveness. Using floating microspheres may enhance the solubility and gastric retention of ofloxacin, thus enhancing its therapeutic efficacy.

Objectives

This study aimed to formulate and evaluate Ofloxacin-loaded floating microspheres to address the limitations of conventional dosage forms. The microspheres were designed to enhance gastric retention, provide sustained drug release, and improve the bioavailability of Ofloxacin. Key objectives included assessing their physicochemical properties, buoyancy, drug release profile, and antibacterial activity to ensure effective and prolonged therapeutic action. This study uniquely couples a sodium-alginate/chitosan–CaCO₃ formulation strategy with mechanistic kinetic modelling, ex vivo porcine intestinal permeation, antimicrobial efficacy, and six-month stability data to explain why the F3 composition provides superior buoyancy and sustained release.

Methods

To formulate the microspheres, polymers such as sodium alginate and chitosan were used during the emulsion solvent diffusion process. Sodium alginate and chitosan were selected for their complementary gel-forming, mucoadhesive, and sustained-release properties, which enhance gastric retention and improve drug bioavailability. Before the floating microspheres were used for additional research, they were subjected to multiple inspections. Pre-formulation studies drug-excipient compatibility testing, rheological property evaluation, drug content quantification, and drug entrapment efficiency calculations, were a few of these. The form, swelling index, and in vitro buoyancy of the microspheres were also assessed using scanning electron microscopy. Drug release and diffusion studies were conducted in vitro, followed by ex vivo permeation and antibacterial trials. Next, the stability of the microspheres during storage was examined.

Results

The emulsion solvent diffusion technique was employed to prepare floating microspheres of ofloxacin using various polymers. FTIR spectroscopy and DSC results depicted no chemical interaction between the drug and polymers. The encapsulation index, drug content, and In vitro buoyancy studies were found to be 60.4 ± 1.8 for F1, 66 ± 2.1% for F2, 74 ± 2.56% for F3, while drug content readings were160 mg for F1, 180 mg for F2 and 210 mg for F3, and similarly in vitro buoyancy gave 37 ± 2.5% for F1, 50 ± 2.3% for F2 and 72 ± 1.67% for F3 respectively. The formulated microsphere exhibited good rheological properties with a swelling index ranging between 225% and 300%. SEM studies showed that floating microspheres were spherical with regular surfaces. In vitro, release studies revealed that the F3 formulation followed the Korsemeyer’s Peppas model with good ex vivo release of 72.7. The F3 formulation had good antimicrobial properties compared to other formulations.

Conclusion

The drug ofloxacin was subjected to Preformulation experiments to establish its physical and chemical characteristics, solubility, and compatibility with excipients. The drug encapsulation efficiency, in vitro and ex vivo release, micrometric characteristics, and storage stability of a floating microsphere formulation were all investigated, from which the F3 formulation proved to be the best. Also, antimicrobial test verified its effectiveness against Staphylococcus aureus and P. aeruginosa, among others.