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In vitro and in vivo evaluation of β-cyclodextrin-based nanosponges of telmisartan

  • Monica RaoEmail author
  • Amrita Bajaj
  • Ishwar Khole
  • Ghanshyam Munjapara
  • Francesco Trotta
Original Article

Abstract

Telmisartan (TEL) is a BCS Class II drug having dissolution rate limited bioavailability. The aim of work was to enhance the solubility of TEL so that bioavailability problems are solved. β-Cyclodextrin (β-CD) based nanosponges (NSs) were formed by cross-linking β-CD with carbonate bonds, which were porous as well as nanosized. Drug was incorporated by solvent evaporation method. The effect of ternary component alkalizer (NaHCO3) on solubility of TEL was studied. In order to find out the solubilization efficiency of NS, phase solubility study was carried out. Saturation solubility and in vitro dissolution study of β-CD complex of TEL was compared with plain TEL and NS complexes of TEL. The NS and NS complexes of TEL were characterized by differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy, nuclear magnetic resonance and scanning electron microscope. It was found that solubility of TEL was increased by 8.53-fold in distilled water; 3.35-fold in 0.1 N HCl and 4.66-fold in phosphate buffer pH 6.8 by incorporating NaHCO3 in drug–NS complex than TEL. It was found that the NaHCO3 in NS based complex synergistically enhanced dissolution of TEL by modulating microenvironmental pH and by changing amorphization of the drug. The highest solubility and in vitro drug release was observed in inclusion complex prepared from NS and NaHCO3. An increase of 54.4 % in AUC was seen in case the ternary NS complex whereas β-CD ternary complex exhibited an increase of 79.65 %.

Keywords

Nanosponge Telmisartan β-Cyclodextrin Sodium bicarbonate 

Notes

Conflicts of interest

The author reports no conflicts of interest financial or otherwise.

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Copyright information

© Springer Science+Business Media B.V. 2012

Authors and Affiliations

  • Monica Rao
    • 1
    Email author
  • Amrita Bajaj
    • 2
  • Ishwar Khole
    • 1
  • Ghanshyam Munjapara
    • 1
  • Francesco Trotta
    • 3
  1. 1.Department of PharmaceuticsAISSMS College of PharmacyPuneIndia
  2. 2.Head of Department (Pharmaceutics)SVKM’s B. N. College of PharmacyMumbaiIndia
  3. 3.Department of Chemistry IFMUniversity of TorinoTorinoItaly

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