Formulation and Evaluation of Nanosuspension of Simvastatin

Abstract

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

Factors affecting the preparation of Cilnidipine nanoparticles

“…AFM done for optimum formula N4,its surface was found to be smooth with no aggregation which indicated particle size distribution and stability of formula. As shown in figure (4).…”

“…Nanoparticles can be prepared using two methods: bottom-up and top-down. These methods are used to synthesize nanoparticles that yield more physically stable products (4) . Particle-size reduction is one of the most commonly used processes in the formulation development.…”

Physical stability and dissolution of ketoprofen nanosuspension formulation: Polyvinylpyrrolidone and Tween 80 as stabilizers

“…Rank of the amount of ketoprofen dissolved in decreasing order was: nanosuspension of F2 > F3 > F4 > F5. This finding was caused by the increase in the particle size and polymer concentration which could affect the dissolution rates of the nanosuspensions (Shid et al 2013). The high concentration of stabilizers in the formulation is most likely due to the formation of micelles that solubilizes the drug, resulting in Ostwald ripening and further destabilizing nanosuspensions (Shariare et al 2018).…”

“…Micronization alone is not sufficient to increase the bioavailability of insoluble drugs. Therefore, this problem is a challenge to motivate researchers to develop nano-size pharmaceutical preparations (< 1 µm) that could increase the dissolution rates of the drugs as well as their bioavailabilities (Shid et al 2013;Yadollahi et al 2015;Gadhari et al 2022). Nanosuspension is a colloidal submicron dispersion of pure drug particles in a liquid phase stabilized by surfactants and polymers.…”

Nanosizing Approaches: Current Trends in the Solubility Enhancement of Poorly Water-soluble Drugs

“…[60][61][62] Albendazole nanosuspension prepared by High-pressure homogenization technique using different stabilizers shown promising drug action in comparison to pure drug products. 63 Ibuprofen nanosuspensions were prepared using the ultra-homogenization method. It was shown in the study data that the drug particles were significantly reduced by adding Tween and Polyvinylpyrrolidone.…”