Felodipine loaded PLGA nanoparticles: preparation, physicochemical characterization and in vivo toxicity study

Abstract

Felodipine, a calcium channel blocker has been widely used for the treatment of hypertension and cardiovascular diseases; but the frequent dosing is needed for its poor solubility and variable bioavailability. In present study an attempt has been made to overcome the problems through nanoparticulate delivery system using poly (D, L-lactic-co-glycolic acid) polymer keeping in the view to get better sustainability of the formulation. The nanoparticles were prepared by single emulsion solvent evaporation technique and the physico-chemical characterization of prepared nanoparticles confirmed the particles were nanosize range with smooth and spherical morphology. Further, the compatibility of drug-polymer combination was analyzed by FTIR and DSC study. The in vitro drug release study of PLGA nanoparticles showed longer duration of drug release with reduced burst release compared with pure felodipine. The in vitro drug release data were fitted with various mathematical models to establish the drug release mechanism from the nanoparticles and found to follow mixed order kinetics. The in vivo toxicity study in albino mice showed no noticeable change in biochemical parameters and histopathology of organs. Hence, the developed felodipine nanoparticles were prepared, characterized and could possibly be advantageous for prolonged drug release and improving the antihypertensive effect.

Ciprofloxacin HCl-loaded calcium carbonate nanoparticles: preparation, solid state characterization, and evaluation of antimicrobial effect against Staphylococcus aureus

“…The average diameters of the blank CaCO 3 nanoparticles and ciprofloxacin HCl-loaded CaCO 3 nanoparticles were 89.64 nm and 116.09 nm, respectively. The particle size distributions were relatively monodisperse in both formulations with the polydispersity index (PDI) values of 0.246 and 0.216 for the blank CaCO 3 nanoparticles and drug-loaded CaCO 3 nanoparticles, respectively (Adibkia et al 2012, Jana et al 2014). The diameters obtained by the DLS for the prepared nanoparticles were larger than the size observed by the SEM.…”

In Vitro Performance Testing of Nanoparticulate Drug Products for Parenteral Administration

“…Compared to the use of dialysis membranes as a separator inside the dissolution vessel, sample and separate methods require separation of the released drug from the bound fraction after the sampling. Separation of the two fractions, bound and unbound drug, can be done by means of filtration, ultracentrifugation, ultrafiltration, SPE, or asymmetrical flow field flow fractionation (AF4) (50,54). Filtration is a common technique, easy to perform and reproducible; however, special attention must be paid to the filtering material.…”

“…Preparative ultra-centrifugation uses high centrifugal forces over a long period of time, which determines the sedimentation of the nanoparticles. Limitations of this method have been mentioned by Wallace et al and Beyer et al for nanoparticles smaller than 100 nm, among which incomplete separation and the potential to create artifacts by continuing release from the carrier after sampling, due to the high shear forces applied (50,55). SPE uses a solid (stationary) phase and a liquid (mobile) phase to separate the dissolved drug substance from the nano carrier.…”

“…The versatility of the sample and separate method is represented by the possibility to choose between different setups: USP 1, USP 2, or vials; different volumes of dissolution/release medium: from 1 to 900 mL; or type of agitation of the medium: orbital shakers or magnetic stirrers (27,50).…”

“…When assessing drug release from nanoparticulate dosage forms, the main concern is to quantify the released moiety of drug substance in the presence of the carrier bound moiety, which may require physical separation. Physical separation methods based on filtration and centrifugation are used besides physicochemical methods (solid phase extraction [SPE]) (26,(50)(51)(52).…”