Novel Preparation and Effective Delivery of Mucoadeshive Nanoparticles Containing Anti-diabetic Drug

Abstract:

Background: Vildagliptin is an extensively studied DPP-4 inhibitors (anti-diabetic drug) which has contributed greatly to the understnading of molecular interatcion with the DPP-4 enzyme. However, Vildagliptin exerts glucose- lowering effect transiently due to short elimination half-life of 2- 3 hrs. Consequently, strict adherence to the dosing schedule strongly emphasised to the diabetic patients. In order to sustain therapeutic effects of a drug at site of absorption, recent efforts have focused on development of mucoadhesive delivery systems using nanoparticles. Methods: Spray-drying method was used to prepare nanoparticles. The drug vildagliptin was incorporated into the nanoparticles and percentage yield, drug content, surface morphology studies, particle size, swelling rate, ex vivo, drug release, drug distribution, histopathology studies were carried out. Results: The yield percentage and drug loading were determined as 95.8 ± 0.5% and 69 ± 0.3%, respectively. SEM microphotographs further revealed nanoparticles with smooth-surfaced spherical forms and particle size were typically about 450 nm with 375 - 525 range of scattering and swelling rate was found to be 171.5±12%. The ex vivo studies revealed superior mucoadhesive properties of Vildagliptin nanoparticles (8.02 ± 05 hr). The formulation prolonged the release of Vildagliptin to about 12 hrs (98.5 ± 2.5). Vildagliptin prolonged retention in GIT (~12 h) further suggests benefit associated with oral delivery of nanoparticles with higher efficiency than single dose administration. Conclusion: The mucoadhesive nanoparticles optimized in this study may potentially serve as the ideal technology for the effective Vildagliptin delivery specially for diabetes treatment.

Key words: Burst release, Diabetes mellitus, Nanoparticle, Muoadhesive, Vildagliptin, Spray drying.