title: 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.
authors.forename: Lavakumar
authors.initials: L
authors.lastname: Vuppalapati
authors.affiliation: Department of Pharmaceutics, Faculty Raghavendra Institute of Pharmaceutical Education and Research, Anantapuram-515721, AP, India. drsowmyariper@gmail.com.
authors.forename: Sowmya
authors.initials: S
authors.lastname: Cherukuri
authors.forename: Vijaykumar
authors.initials: V
authors.lastname: Neeli
authors.forename: Padmanabha Reddy
authors.initials: PR
authors.lastname: Yeragamreddy
authors.forename: Bhaskar Reddy
authors.initials: BR
authors.lastname: Kesavan
mesh_terms: D000284:Administration, Oral; D000959:Antihypertensive Agents / Q000737:chemistry; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D008855:Microscopy, Electron, Scanning / Q000379:methods; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013535:Suspensions / Q000737:chemistry*; D000068756:Valsartan / Q000737:chemistry*; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D000959:Antihypertensive Agents; D005079:Excipients; D013535:Suspensions; D000068756:Valsartan