Abstract
This paper reports on the development of nanoparticles aiming at the in vitro controlled release of simvastatin (SVT). The nanoparticles were prepared by the nanoprecipitation method with polymers Eudragit® FS30D (EDGFS) or Eudragit® NE30D (EDGNE). EDGFS+SVT nanoparticles showed mean size of 148.8 nm and entrapment efficiency of 76.4%, whereas EDGNE+SVT nanoparticles showed mean size of 105.0 nm and entrapment efficiency of 103.2%. Infrared absorption spectra demonstrated that SVT incorporated into the polymer matrix, especially EDGNE. Similarly, the differential scanning calorimeter (DSC) curve presented no endothermic peak of fusion, indicating that the system is amorphous and the drug is not in the crystalline state. The maintenance of SVT in the amorphous state may favors its solubilization in the target release sites. In the in vitro dissolution assay, the SVT incorporated into the EDGFS+SVT nanoparticles showed a rapid initial release, which may be related to the pH of the dissolution medium used. Regarding the EDGNE+SVT nanoparticles, the in vitro release occurred in a bimodal behavior, i.e., an initial “burst” followed by a sustained delivery, with the kinetics of drug release following Baker-Lonsdale’s mathematical model. All these features suggest the nanoparticulate system’s potential to modulate SVT delivery and enhance its bioavailability.
Highlights
Simvastatin (SVT) (Figure 1) is a drug that belongs to a class of substances called statins, commonly used to reduce the production of cholesterol
The method selected for preparing the polymeric nanoparticles i.e., nanoprecipitation, has been widely used by both the academic and industrial communities for the development of pharmaceutical and agricultural products as innovative and eco-friendly solutions
Nanoparticles were formed spontaneously when the organic phase containing one of the polymers (EDGFS or Eudragit® NE30D (EDGNE)) plus SVT dissolved in acetone is poured into the aqueous solution containing surfactant Polaxamer® 407 (P407), agitated by magnetic stirring, resulting in a milky-looking suspension
Summary
Simvastatin (SVT) (Figure 1) is a drug that belongs to a class of substances called statins, commonly used to reduce the production of cholesterol. It acts by suppressing the endogenous cholesterol biosynthesis as a function of the competitive inhibition of 3-hydroxy3-methylglutaryl coenzyme-A (HMG-CoA) reductase – an enzyme that catalyzes the initial and rate-limiting step of the production of cholesterol. This inhibition contributes to the control of hypercholesterolemia, which is one of the risk factors for the development of atherosclerosis (Stone et al, 2014; Da Cruz et al, 2017). In Class II, drug dissolution in the GIT is considered the rate-limiting step for oral bioavailability (Fattahi et al, 2016)
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