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Polylactic-co-glycolic acid (PLGA) 50:50 and Eudragit RS 100 nanoparticles entrapping glipizide along with excipients were prepared using single emulsion solvent evaporation method. The objective was to develop single oral dose glipizide nano particles for reducing blood sugar level in diabetes induced experimental animals. Incorporation of Polyethylene glycol (PEG) (0.5%), Hydroxypropyl methylcellulose (HPMC) (0.5%) and Tween 20 (0.5%) in the organic phase during particle formulation improved release profile of glipizide from the polymer particles. Entrapment efficiency of glipizide in all the polymeric formulations was around ~70 %. Around 80 % of glipizide was released from both PLGA and Eudragit RS 100 nanoparticles when 0.5% of PEG and Tween 20 were added during preparation. Incorporation of amphiphilic polymer during particle formulation not only improved entrapment efficiency of glipizide but also resulted in uniform stabilized nanoparticles having desired control release characteristics. Both PLGA and Eudragit nanoparticles were biocompatible to SW 480 adenocarcinoma human cell line at concentration ranges from 12.5 to 500 µg/ml. The efficacy of glipizide loaded particle formulations were evaluated in female out breed Wistar rats. Significant reduction of blood glucose level was observed (p ≤ 0.05) for 24 hours from a single oral dose using stabilized nanoparticles formulations.
Pratap C. Naha, Hugh J. Byrne, and Amulya K. Panda, Role of polymeric excipients on controlled release profile of Glipizide from PLGA and Eudragit RS 100 Nanoparticles, Journal of Nanopharmaceutics and Drug Delivery, 1, 74-81 (2013)