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AAPS PharmSciTech

, Volume 13, Issue 4, pp 1416–1427 | Cite as

Development, Optimization, and Characterization of Solid Self-Nanoemulsifying Drug Delivery Systems of Valsartan Using Porous Carriers

  • Sarwar Beg
  • Suryakanta Swain
  • Harendra Pratap Singh
  • Ch Niranjan Patra
  • ME Bhanoji Rao
Research Article

Abstract

The present studies entail formulation development of novel solid self-nanoemulsifying drug delivery systems (S-SNEDDS) of valsartan with improved oral bioavailability, and evaluation of their in vitro and in vivo performance. Preliminary solubility studies were carried out and pseudoternary phase diagrams were constructed using blends of oil (Capmul MCM), surfactant (Labrasol), and cosurfactant (Tween 20). The SNEDDS were systematically optimized by response surface methodology employing 33-Box–Behnken design. The prepared SNEDDS were characterized for viscocity, refractive index, globule size, zeta potential, and TEM. Optimized liquid SNEDDS were formulated into free flowing granules by adsorption on the porous carriers like Aerosil 200, Sylysia (350, 550, and 730) and Neusilin US2, and compressed into tablets. In vitro dissolution studies of S-SNEDDS revealed 3–3.5-fold increased in dissolution rate of the drug due to enhanced solubility. In vivo pharmacodynamic studies in Wistar rats showed significant reduction in mean systolic BP by S-SNEDDS vis-à-vis oral suspension (p < 0.05) owing to the drug absorption through lymphatic pathways. Solid-state characterization of S-SNEDDS using FT-IR and powder XRD studies confirmed lack of any significant interaction of drug with lipidic excipients and porous carriers. Further, the accelerated stability studies for 6 months revealed that S-SNEDDS are found to be stable without any change in physiochemical properties. Thus, the present studies demonstrated the bioavailability enhancement potential of porous carriers based S-SNEDDS for a BCS class II drug, valsartan.

KEY WORDS

BCS bioavailability in vitro dissolution porous carriers XRD 

Notes

ACKNOWLEDGMENTS

The authors are highly thankful to SAIF Panjab University, Chandigarh for carrying out the powder X-ray diffraction study and also thankful to Institute of Life Sciences, Bhubaneswar for providing the facility to determine the globule size and AIIMS, New Delhi for TEM study.

Conflict of Interest

Authors declare no conflict(s) of interest.

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Copyright information

© American Association of Pharmaceutical Scientists 2012

Authors and Affiliations

  • Sarwar Beg
    • 1
  • Suryakanta Swain
    • 1
  • Harendra Pratap Singh
    • 1
  • Ch Niranjan Patra
    • 1
  • ME Bhanoji Rao
    • 1
  1. 1.Department of PharmaceuticsRoland Institute of Pharmaceutical SciencesBerhampurIndia

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