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AAPS PharmSciTech

, 20:45 | Cite as

Quality by Design Approach for Developing Lipid-Based Nanoformulations of Gliclazide to Improve Oral Bioavailability and Anti-Diabetic Activity

  • Pravin Patel
  • Sravanthi Reddy Pailla
  • Nagarjun Rangaraj
  • Hanumanth Srikanth Cheruvu
  • Sujatha Dodoala
  • Sunitha SampathiEmail author
Research Article

Abstract

The aim of the current investigation was to generate a self-nanoemulsifying drug delivery system (SNEDDS) of gliclazide (GCZ) to address the poor solubility and bioavailability. Ternary phase diagram was created with Capmul MCM C8 NF (oil), Cremophor RH 40 (surfactant), and Transcutol HP (co-surfactant) to distinguish the self-emulsifying region. A D-optimal design was employed with three variables, such as oil, surfactant, and co-surfactant, for further optimization of liquid (L)-SNEDDS. GCZ-loaded L-SNEDDs were analyzed for globule size, polydispersity index (PDI), and solubility. In vitro dissolution of optimized L-SNEDDS exhibited (F5) faster drug release (97.84%) within 30 min as compared to plain drug (15.99%). The optimized L-SNEDDS was converted to solid (S)-SNEDDS as a self-nanoemulsifying powder (SNEP) and pellets by extrusion-spheronization. Optimized S-SNEDDS were characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). In vitro dissolution of SNEP (S3) and pellet were 90.54 and 73.76%, respectively, at 30 min. In vivo studies showed a twofold rise in bioavailability through SNEDDS with a significant decline in blood glucose levels compared to plain drug suspension suggesting a lipid-based system as an alternative approach for treating diabetes.

KEY WORDS

D-optimal design extrusion spheronization SNEDDS pharmacokinetics single-pass intestinal perfusion self-nanoemulsifying powder 

Notes

Acknowledgments

The authors would like to acknowledge NIPER Hyderabad for providing facilities for the research work.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that there are no conflicts of interest.

Supplementary material

12249_2018_1214_MOESM1_ESM.docx (345 kb)
ESM 1 (DOCX 345 kb)

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Pravin Patel
    • 1
  • Sravanthi Reddy Pailla
    • 1
  • Nagarjun Rangaraj
    • 1
  • Hanumanth Srikanth Cheruvu
    • 1
  • Sujatha Dodoala
    • 2
  • Sunitha Sampathi
    • 1
    Email author
  1. 1.Department of PharmaceuticsNational Institute of Pharmaceutical Education and Research (NIPER-HYD)BalanagarIndia
  2. 2.Institute of Pharmaceutical TechnologySri Padmavathi Mahila VisvavidyalayamTirupatiIndia

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