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Formulation of silk fibroin-based single polymeric floating microspheres for sustained release of lafutidine

By: Pantwalawalkar, Jidnyasa.
Contributor(s): Nangare, Sopan.
Publisher: Karnataka Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(2), Apr-June.Description: 396-404p.Subject(s): PHARMACEUTICSOnline resources: Click here In: Indian journal of pharmaceutical education and researchSummary: Purpose: The present study was aimed at the formulation of lafutidine-loaded silk fibroin- based floating microspheres (LAFU-SF-Microspheres) for the site-specific sustained release of the drug. Materials and Methods: Briefly, the single polymeric system comprising SF was selected to prepare LAFU-SF-Microspheres by employing the emulsion solvent evaporation method. Subsequently, the obtained LAFU-SF-Microspheres were assessed for particle size, zeta potential, percent entrapment efficiency (%EE), percentage drug content (%DC), micromeritics, floating profile, in-vitro drug release, spectroscopical analysis, and accelerated stability study. Results: The particle size and zeta potential of the LAFU-SF-Microsphere were found to be 2.3-6.8μm and -21.93mV respectively whilst % EE and % DC of LAFU-SF-Microspheres were found to be 86.83±3.46% and 93.89±3.98% respectively. Moreover, it demonstrated the adequate angle of repose (26.50±1.06°) and Carr’s Compressibility Index (CI) confirming the excellent flow properties. In view of the floating profile, LAFU-SF-Microspheres showed floating lag time (FLT) between 9-13sec and total floating time (TFT) more than 12hr. Moreover, the % buoyancy was found to be 97.62± 4.78%. LAFU-SF-Microspheres showed in-vitro % drug release up to 92.41±4.29% adopting the first-order model. The FTIR indicated successful incorporation of LAFU in LAFU-SF-Microspheres. The DSC and PXRD indicated the disrupted crystallinity of LAFU in LAFU-SF-Microspheres. The SEM images of microspheres displayed spherical shapes with smooth textures. Conclusion: SF microspheres can be fruitfully applied for customized floating and release patterns of drugs with distinct solubility classes.
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Purpose: The present study was aimed at the formulation of lafutidine-loaded silk fibroin-
based floating microspheres (LAFU-SF-Microspheres) for the site-specific sustained
release of the drug. Materials and Methods: Briefly, the single polymeric system comprising
SF was selected to prepare LAFU-SF-Microspheres by employing the emulsion solvent
evaporation method. Subsequently, the obtained LAFU-SF-Microspheres were assessed
for particle size, zeta potential, percent entrapment efficiency (%EE), percentage drug
content (%DC), micromeritics, floating profile,
in-vitro drug release, spectroscopical
analysis, and accelerated stability study. Results: The particle size and zeta potential
of the LAFU-SF-Microsphere were found to be 2.3-6.8μm and -21.93mV respectively
whilst % EE and % DC of LAFU-SF-Microspheres were found to be 86.83±3.46% and
93.89±3.98% respectively. Moreover, it demonstrated the adequate angle of repose
(26.50±1.06°) and Carr’s Compressibility Index (CI) confirming the excellent flow
properties. In view of the floating profile, LAFU-SF-Microspheres showed floating lag
time (FLT) between 9-13sec and total floating time (TFT) more than 12hr. Moreover,
the % buoyancy was found to be 97.62± 4.78%. LAFU-SF-Microspheres showed
in-vitro % drug release up to 92.41±4.29% adopting the first-order model. The FTIR
indicated successful incorporation of LAFU in LAFU-SF-Microspheres. The DSC and
PXRD indicated the disrupted crystallinity of LAFU in LAFU-SF-Microspheres. The SEM
images of microspheres displayed spherical shapes with smooth textures. Conclusion:
SF microspheres can be fruitfully applied for customized floating and release patterns of
drugs with distinct solubility classes.

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