Objective:
The aim of this study is to prepare floating hollow
microspheres encapsulating Sorafenib (SFN) to enha
nce its oral bioavailability.
Methods:
Gastro-floating hollow adhesive microspheres contai
ning SFN were produced by using an emulsion solvent
evaporation technique with
ether and ethanol as solvents. Ethyl cellulose and
carbopol 934P were used as the encapsulating carrie
rs. The effects of formulation parameters like,
solvent volume ratio, and drug to polymer ratio (D:
P ratio), encapsulation efficiency percentage EE%, f
loating percentage, and release of SFN after
12 h (Rel
12
) were investigated and analyzed using a (3
2
) full factorial design.
Results:
The floating percentage of the microspheres was fou
nd to be 76.5%. The
in vitro
drug release from these hollow microspheres follow
ed the
Higuchi model equation. The
in vivo
results showed that approximately 1.96-fold improv
ement in the relative bioavailability of the micros
pheres
compared with that of the commercial tablet.
Conclusion:
The results demonstrate that the hollow microsphere
s with good gastro-floating ability are a promising
delivery system to enhance
SFN bioavailability