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Fibroin-Alginate Scaffold for Design of Floating Microspheres Containing Felodipine

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Abstract

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.

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Abbreviations

EE:

Entrapment efficiency

FT-IR:

Fourier transforms-infrared

UV-Vis:

Ultraviolet–visible

DSC:

Differential scanning calorimetry

PXRD:

Powder X-ray diffraction

SF:

Silk fibroin

FD:

Felodipine

DC:

Drug content

FSSGF:

Fasted-state simulated gastric fluid

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Authors and Affiliations

  1. Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur, Maharashtra, 416013, India

    Prashant Rathod, Harinath More, Shailesh Dugam, Pallavi Velapure & Namdeo Jadhav

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  1. Prashant Rathod
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  2. Harinath More
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  3. Shailesh Dugam
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Correspondence to Namdeo Jadhav.

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Rathod, P., More, H., Dugam, S. et al. Fibroin-Alginate Scaffold for Design of Floating Microspheres Containing Felodipine. J Pharm Innov 16, 226–236 (2021). https://doi.org/10.1007/s12247-020-09440-6

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