Background: Glimepiride is a third-generation, oral anti-diabetic sulfonylurea drug, generally
recommended for the treatment of type–II diabetes. A biocompatible polymer, Eudragit RS 100 is
widely used for the preparation of targeted and time-controlled release of drugs. Glimepiride is encapsulated
using Eudragit RS 100 for sustained release delivery.
Objective: To develop sustained release microparticles of Glimepiride using microreactor technology
to reduce the dosing frequency.
Methods: Microreactor precipitation method was used to develop sustained release microparticles of
Glimepiride. Plackett-Burman design was employed for the optimization of all the parameters including
the inner diameter of silicon tubing, the flow rate of solvent as well as antisolvent, length of tubing
and concentration of polymer, etc. Microparticles prepared were characterized by Fourier transform infrared
spectroscopy, X-ray diffraction, Scanning electron microscopy and in vitro drug release as well
as release kinetics study.
Results: Placket Burman design was found to be effective for comparing more than two parameters at a
time and showed the effect of parameters on design. The parameters A, B, C, D, E and J synergistically
affected the encapsulation efficiency. FE-SEM demonstrated the smooth and spherical nature of particles.
Fourier transformed infrared spectroscopy showed the absence of chemical interaction between
polymer and drug; X-ray diffraction results showed the decrease in crystallinity of pure drug when it
was transformed into encapsulated drug-loaded microparticles. The sustained drug release was observed
for 12 h.
Conclusion: Prepared Glimepiride loaded sustained release microparticles followed the first-order release
kinetics. The developed formulation could reduce dose frequency and improve patient compliance.