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Purpose <p>To develop spiramycin lipid-based nano delivery systems for improved oral bioavailability (BA) and antibacterial action.</p> Significance <p>Spiramycin lipid nanoemulsions/solid lipid nanoparticles (LNEs/SLNs) are novel, not previously reported, and have the potential to be industrially produced for patient benefit.</p> Methods <p>LNEs/SLNs were prepared by using known methods and characterized for particle size, poly dispersity, charge, drug entrapment, drug content, and drug release. Bioavailability (BA) was found in rats. Next,<i> in vitro</i> antibacterial action was seen by the agar diffusion test. IVIVCs (<i>In vitro In vivo</i> correlations) of optimal LNE and SLN were analysed.</p> Results <p>The size, Polydispersity Index ( PDI), and Zeta potential (ZP) of LNEs varied in between 212.1 ± 0.95 and 269.7 ± 1.6&#xa0;nm, 0.12 ± 0.03 and 0.25 ± 0.03, and − 28.6 ± 1.8 and − 30.5 ± 1.1 mV, respectively. Drug content, entrapment efficiency (EE), and cumulative release of LNEs varied in between 98.1 ± 1.24 and 98.6 ± 0.2%, 97.5 ± 0.27 and 98.12 ± 0.12%, and 90.2 ± 0.85 and 96.06 ± 0.29%, respectively. The size, PDI, and ZP of SLNs varied in between 170.81 ± 1.64 and 194.46 ± 3.87&#xa0;nm, 0.23 ± 0.04 and 0.30 ± 0.12, and − 16.13 ± 1.1 and − 28.43 ± 0.25 mV, respectively. Drug content, EE, and cumulative release of SLNs varied in between 96.56 ± 1.18 and 99.67 ± 0.08%, 73.92 ± 0.36 and 84.21 ± 0.7%, and 92.27 ± 0.49 and 97.17 ± 0.21%, respectively. In pharmacokinetic (PK) studies, SLN-S2 showed a higher area under the curve (AUC) than that of LNE-F3. In IVIVC analysis, LNE-F3 showed an R<sup>2</sup> value of 0.977, while SLN-S2 showed 0.838.</p> Conclusions <p>Both formulations were found to be less bitter and stable at room and refrigerated temperatures. They showed superior antibacterial activity against <i>E. coli</i> when compared to the solution. In PK studies, SLN-S2 and LNE-F3 showed 2.95 and 2.70-fold increase in BA, respectively, when compared to the drug suspension. They exhibited no significant difference in BA. LNE-F3 showed level A IVIVC when compared to SLN-S2.</p>

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Spiramycin—A BCS Class III Drug: Comparative Studies On the Development of Lipid-based Nano Formulations for Improved Oral Bioavailability and Antibacterial Action

  • 期刊论文

  • 发表日期：

    2026年5月11日

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  • Mamatha Myakala,
  • Kishan Veerabrahma

摘要

Purpose

To develop spiramycin lipid-based nano delivery systems for improved oral bioavailability (BA) and antibacterial action.

Significance

Spiramycin lipid nanoemulsions/solid lipid nanoparticles (LNEs/SLNs) are novel, not previously reported, and have the potential to be industrially produced for patient benefit.

Methods

LNEs/SLNs were prepared by using known methods and characterized for particle size, poly dispersity, charge, drug entrapment, drug content, and drug release. Bioavailability (BA) was found in rats. Next, in vitro antibacterial action was seen by the agar diffusion test. IVIVCs (In vitro In vivo correlations) of optimal LNE and SLN were analysed.

Results

The size, Polydispersity Index ( PDI), and Zeta potential (ZP) of LNEs varied in between 212.1 ± 0.95 and 269.7 ± 1.6 nm, 0.12 ± 0.03 and 0.25 ± 0.03, and − 28.6 ± 1.8 and − 30.5 ± 1.1 mV, respectively. Drug content, entrapment efficiency (EE), and cumulative release of LNEs varied in between 98.1 ± 1.24 and 98.6 ± 0.2%, 97.5 ± 0.27 and 98.12 ± 0.12%, and 90.2 ± 0.85 and 96.06 ± 0.29%, respectively. The size, PDI, and ZP of SLNs varied in between 170.81 ± 1.64 and 194.46 ± 3.87 nm, 0.23 ± 0.04 and 0.30 ± 0.12, and − 16.13 ± 1.1 and − 28.43 ± 0.25 mV, respectively. Drug content, EE, and cumulative release of SLNs varied in between 96.56 ± 1.18 and 99.67 ± 0.08%, 73.92 ± 0.36 and 84.21 ± 0.7%, and 92.27 ± 0.49 and 97.17 ± 0.21%, respectively. In pharmacokinetic (PK) studies, SLN-S2 showed a higher area under the curve (AUC) than that of LNE-F3. In IVIVC analysis, LNE-F3 showed an R2 value of 0.977, while SLN-S2 showed 0.838.

Conclusions

Both formulations were found to be less bitter and stable at room and refrigerated temperatures. They showed superior antibacterial activity against E. coli when compared to the solution. In PK studies, SLN-S2 and LNE-F3 showed 2.95 and 2.70-fold increase in BA, respectively, when compared to the drug suspension. They exhibited no significant difference in BA. LNE-F3 showed level A IVIVC when compared to SLN-S2.