Application of Central Composite Design in Optimization of Valsartan Nanosuspension to Enhance its Solubility and Stability.

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.

journal_name

Curr Drug Deliv

journal_title

Current drug delivery

authors

Vuppalapati L,Cherukuri S,Neeli V,Yeragamreddy PR,Kesavan BR

doi

10.2174/1567201812666150724094358

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

143-57

issue

1

eissn

1567-2018

issn

1875-5704

pii

CDD-EPUB-69027

journal_volume

13

pub_type

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