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.

Development of Metronidazole Loaded Chitosan Nanoparticles Using QbD Approach—A Novel and Potential Antibacterial Formulation

“…The hydrodynamic PS of MetNp were analyzed after subjecting samples to dynamic light scattering in Zetasizer Nano ZS 90 (Malvern instruments, Royston, UK) analogous to an earlier study performed by our group [ 16 , 26 , 27 , 28 ]. Samples were diluted (10-times) with deionized water at 25 ± 0.5 °C and were sonicated before examination.…”

HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

“…Moreover, they help to improve the bioavailability of medications by protecting them from exposure to stomach acid and pepsin. The literature signifies that studies have also been carried out to enhance the therapeutic efficacy of various drugs by formulating mucoadhesive nanoparticles intended for oral therapy [8][9][10]. During the past few decades, various sitagliptin-loaded polymeric nano formulations for oral drug delivery have been developed to enhance bioavailability [2,11,12].…”

Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics

“…For this reason, the drug should remain in the upper part of the gastrointestinal tract or in the stomach for longer periods of time. This can only be achieved by sustaining the drug's release until all of the drug is completely released over a desired period of time [6–8]. Existing drugs with prolonged gastric residence times can reveal greater insights into new therapeutic options.…”