Abstract
The objective of the present research is to prepare stable nano suspensions of Valsartan (VAL) with high solubility and dissolution. VAL is an orally administered anti-hypertensive drug with lower bio-availability of 25%, this is attributed to its lower aqueous solubility (0.082 mg/ml). VAL nano suspensions were prepared by using a bottom-up precipitation technique using five level full factorial central composite design (CCD). The optimized nano formulations NS21, NS22, NS23 showed the particle size of 268.42±8.99, 288.3±11.32, 293.46±6.92 nm, zeta potential of 20.89±0.79, 26.01 ±1.02, 21.34±0.43 mVs and the dissolution efficiency of 93.10±1.459, 91.84±1.419, 89.47±0.644 % respectively. SEM & AFM studies represent the formation of fine irregularly shaped particles with smooth surfaces on nanosization. X-rd studies confirmed the physical state conversion of crystalline drug into amorphous form. Drug excipient compatibility was studied using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The investigation pragmatic the solubility and dissolution efficiency of VAL in nanosuspension was significantly higher when compared with its pure form. Finally, it is concluded that, nanosuspension approach could be an ideal, promising approach to increase the solubility and dissolution of BCS-II drugs like Valsartan.
Keywords: Valsartan, central composite design, nanosuspension, anti-solvent precipitation technique, bio-pharmaceutics classification system, dissolution efficiency.
Current Drug Delivery
Title:Application of Central Composite Design in Optimization of Valsartan Nanosuspension to Enhance its Solubility and Stability
Volume: 13 Issue: 1
Author(s): Lavakumar Vuppalapati, Sowmya Cherukuri, Vijaykumar Neeli, Padmanabha Reddy Yeragamreddy and Bhaskar Reddy Kesavan
Affiliation:
Keywords: Valsartan, central composite design, nanosuspension, anti-solvent precipitation technique, bio-pharmaceutics classification system, dissolution efficiency.
Abstract: The objective of the present research is to prepare stable nano suspensions of Valsartan (VAL) with high solubility and dissolution. VAL is an orally administered anti-hypertensive drug with lower bio-availability of 25%, this is attributed to its lower aqueous solubility (0.082 mg/ml). VAL nano suspensions were prepared by using a bottom-up precipitation technique using five level full factorial central composite design (CCD). The optimized nano formulations NS21, NS22, NS23 showed the particle size of 268.42±8.99, 288.3±11.32, 293.46±6.92 nm, zeta potential of 20.89±0.79, 26.01 ±1.02, 21.34±0.43 mVs and the dissolution efficiency of 93.10±1.459, 91.84±1.419, 89.47±0.644 % respectively. SEM & AFM studies represent the formation of fine irregularly shaped particles with smooth surfaces on nanosization. X-rd studies confirmed the physical state conversion of crystalline drug into amorphous form. Drug excipient compatibility was studied using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The investigation pragmatic the solubility and dissolution efficiency of VAL in nanosuspension was significantly higher when compared with its pure form. Finally, it is concluded that, nanosuspension approach could be an ideal, promising approach to increase the solubility and dissolution of BCS-II drugs like Valsartan.
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Vuppalapati Lavakumar, Cherukuri Sowmya, Neeli Vijaykumar, Yeragamreddy Reddy Padmanabha and Kesavan Reddy Bhaskar, Application of Central Composite Design in Optimization of Valsartan Nanosuspension to Enhance its Solubility and Stability, Current Drug Delivery 2016; 13 (1) . https://dx.doi.org/10.2174/1567201812666150724094358
DOI https://dx.doi.org/10.2174/1567201812666150724094358 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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