Folate Engineered Microbeads Loaded with Anticancer Drug for Targeted Delivery as Cancer Targeted Vector

Background: Sulforaphane (SFN) is an isothiocyanate obtained from Brassicaceae vegetables. SFN is an anticarcinogenic
drug used in the treatment of breast cancer. Microbeads have various properties such as high stability,
sustained release, acceptability, small particle size and controlled release of the drug molecules. A drug delivery
system releases the drug in the particular body compartment at the controlled rate required for a specific treatment,
especially in the study of controlled-release and slow release.

Methods: The present study aimed at the development and optimization of multiparticulate system consisting of
Folate-alginate beads containing SFN for extended delivery using design of experiments by employing Box-Behnken
statistical design (BBD).

Results: The result showed that QbD approach was successfully used in the development of Folate–alginate beads for
the extended-release of SFN with predictable encapsulation efficiency, particle size and drug release properties. The
quality of SFN loaded Folate-alginate beads were presented using Box–Behnken design.

Conclusion: The result showed that QbD approach was successfully used in the development of Folate–alginate beads
for the extended-release of SFN with predictable encapsulation efficiency, particle size and drug release properties.
The quality of SFN loaded Folate-alginate beads were presented using Box– Behnken design. All the independent
variables, the concentration of sodium alginate (X1) 3.5-6.5 % w/v, folic-acid(X2) 0.8-2 % w/v and CaCl2 (X3) 4.5-9.5 %
w/v were found to affect the time for 75% of the drug to be released (T75% ), particle size and encapsulation efficiency
either through linear, quadratic or interaction effects. The results revealed that polymer amount is a major factor
affecting the drug release, particle size and encapsulation efficiency. The optimized formulation prepared using the
predicted levels of factors provided the desired observed responses with T75% (Y1), particle size (Y2) and DEE (Y3)
values of 17.2h, 1389.43μm and 82.6% respectively. In vitro release studies showed that the drug is released from the
optimized formulation throughout 24 h in a sustained release manner.