Purpose

The objective of present work was to develop fibroin-sodium alginate floating microspheres of felodipine (FD) showing modified release.

Method

Binary polymer system of fibroin-sodium alginate was used to prepare microspheres by spray drying technique. Thus, FD loaded microspheres obtained were evaluated for % drug content, % entrapment efficacy, particle size, micromeritics, FT-IR, DSC, XRD, floatability profile, mucoadhesion, in vitro drug release, and accelerated stability studies.

Results

The drug content of FD-loaded microspheres (F1–F5) was in the range of 68.55 ± 1.20 to 78.21 ± 0.54 and entrapment efficacy 45.93 ± 0.41 to 61.60 ± 0.72%. The particle size varied from 60.33 ± 0.64 to 66.87 ± 0.85 μm. Acceptable Carr’s compressibility index and angle of repose demonstrated excellent flowability of microspheres (F1–F5). The FT-IR showed no chemical interactions between FD and polymers. The DSC and XRD indicated that FD was partially crystalline in microspheres. Floating parameters for optimized batch F2 were floating lag time10–15 s and floating time > 12 h. Floating buoyancy is 96.51 ± 0.66%. The in vitro drug dissolution kinetics of optimized F2 batch in 0.1NHCl and FSSGF demonstrated % drug release up to 80.42 ± 0.86% in 0.1NHCl and 84.64 ± 0.30% in FSSGF following Peppas model.

Conclusion

Electrostatic repulsion between polymers successfully enabled the design of FD-loaded floating microspheres by spray drying. Excellent floating profile and extended release for 12 h, as per USFDA guidelines, have been demonstrated by the fibroin-sodium alginate binary composite system. In the future, fibroin-sodium alginate scaffold can be successfully used for tailor-made floating and release profiles of drugs belonging to different solubility classes.

中文翻译：

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纤维蛋白-海藻酸盐支架用于设计含非洛地平的漂浮微球

目的

目前工作的目的是开发非洛地平的纤溶蛋白海藻酸钠漂浮微球（FD），其显示出缓释作用。

方法

用纤维蛋白-海藻酸钠的二元聚合物体系通过喷雾干燥技术制备微球。因此，评价了获得的FD负载的微球的％药物含量，％包封率，粒径，微聚合物，FT-IR，DSC，XRD，漂浮性，粘膜粘附性，体外药物释放和加速稳定性研究。

结果

FD载药微球（F1-F5）的药物含量在68.55±1.20至78.21±0.54之间，包封率在45.93±0.41至61.60±0.72％之间。粒度从60.33±0.64到66.87±0.85μm不等。可接受的Carr压缩系数和休止角表明，微球（F1-F5）具有出色的流动性。FT-IR表明FD与聚合物之间没有化学相互作用。DSC和XRD表明FD在微球中部分结晶。优化批次F2的浮动参数为浮动滞后时间10-15 s和浮动时间> 12 h。浮力为96.51±0.66％。在Peppas模型下，优化的F2批次在0.1NHCl和FSSGF中的体外药物溶解动力学表明，在0.1NHCl中的药物释放百分比高达80.42±0.86％，在FSSGF中的药物释放高达84.64±0.30％。

结论

聚合物之间的静电排斥通过喷雾干燥成功地设计了加载FD的浮动微球。纤维蛋白-海藻酸钠二元复合体系已证明，​​根据USFDA指南具有出色的漂浮性和可延长释放12小时。将来，血纤蛋白-海藻酸钠支架可以成功用于定制的不同溶解度类别药物的漂浮和释放特性。