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Sci. Pharm. 2011, 79(3), 635-652; doi:10.3797/scipharm.1103-17

Enhanced Antihypertensive Activity of Candesartan Cilexetil Nanosuspension: Formulation, Characterization and Pharmacodynamic Study

Drug Delivery Laboratory, Centre of Relevance and Excellence in NDDS, G.H. Patel Building of Pharmacy, Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Vadodara-390002, India
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Received: 24 March 2011 / Accepted: 5 July 2011 / Published: 5 July 2011
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Abstract

The objective of the present investigation was to enhance the oral bioavailability of practically insoluble Candesartan cilexetil [CC] by preparing nanosuspension. The nanosuspension was prepared by media milling using zirconium oxide beads and converted to solid state by spray drying. The spray dried nanosuspension of CC [SDCN] was evaluated for particle size, zeta potential, saturation solubility, crystallanity, surface morphology and dissolution behavior. SDCN showed particle size of 223.5±5.4 nm and zeta potential of −32.2±0.6 mV while saturation solubility of bulk CC and SDCN were 125±6.9 μg/ml and 2805±29.5 μg/ml respectively, showing more than 20 times increase in solubility. Differential Scanning Calorimetry [DSC] and X-ray diffraction [XRD] analysis showed that crystalline state of CC remained unchanged in SDCN. Dissolution studies in phosphate buffer pH 6.5 containing 0.7% Tween 20 showed that 53±5% of bulk drug dissolved in 15 min whereas SDCN was almost completely dissolved exhibiting higher dissolution velocity and solubility. Transmission electron microscopy [TEM] revealed that nanocrystals were not of uniform size, and approximately of oval shape. Pharmacodynamic study based on deoxycorticosterone acetate [DOCA] salt model was performed in rats to evaluate in-vivo performance, which showed 26.75±0.33% decrease in systolic blood pressure for nanosuspension while plain drug suspension showed 16.0±0.38% reduction, indicating that increase in dissolution velocity and saturation solubility leads to enhancement of bioavailability of SDCN when compared to bulk CC suspension. Thus, the results conclusively demonstrated a significant enhancement in antihypertensive activity of candesartan when formulated as nanosuspension.
Keywords: Candesartan; Saturation solubility; Nanosuspension; Bioavailability; DOCA salt model Candesartan; Saturation solubility; Nanosuspension; Bioavailability; DOCA salt model
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

DETROJA, C.; CHAVHAN, S.; SAWANT, K. Enhanced Antihypertensive Activity of Candesartan Cilexetil Nanosuspension: Formulation, Characterization and Pharmacodynamic Study. Sci. Pharm. 2011, 79, 635-652.

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