In Vitro and In Vivo Evaluation of Nanoparticles Prepared by Nano Spray Drying for Stomach Mucoadhesive Drug Delivery

Abstract

According to a World Health Organization report published in 2010, 346 million people worldwide have diabetes; in Saudi Arabia, 16.8% of the population has been diagnosed with type 2 diabetes. Many patients with type 2 diabetes are unable to maintain adequate glycemic control even after receiving recent antidiabetic drugs. A combination of vildagliptin and metformin hydrochloride tablets is available; however, both conventional drugs have a short half-life. The formulation of mucoadhesive nanoparticles for these classes of drugs can be most beneficial, because they release the drug slowly into the gastrointestinal tract and maintain the therapeutic drug concentration. Vildagliptin and metformin hydrochloride were prepared with Carbopol (VMCN) using a Buchi Nano Spray Dryer B-90. The surface morphology was found to be shriveled (due to surface folding), and the average particle size was 437 nm. The percentage drug yield for vildagliptin and metformin hydrochloride in the nanoparticles was 71 ± 0.5% and 74 ± 0.3%, respectively, and the drug content was 84 ± 0.4% and 89 ± 0.4%, respectively. Ex vivo studies of mucoadhesion were 6.9 ± 0.3 h. The percentage of swelling was recorded as 162 ± 4%. In vivo studies of nanoparticles containing vildagliptin and metformin hydrochloride showed that these values were 3.9 and 4.1% at 12 h, respectively.

Keywords:

• Encapsulation
• Pharmaceuticals
• Powder technology
• Spray drying

ACKNOWLEDGMENTS

I thank Bandar E. Al-Dhubiab for contributions and Journal Prep for English-language editing.