Simvastatin is a poorly water-soluble drug, and bioavailability from its crystalline form is very low. The purpose of this investigation was to increase the solubility and dissolution rate of simvastatin by the preparation of nanosuspensions with Pluronic F127 and zirconium oxide (ZrO 2 ) beads using a wet-milling technique at the laboratory scale. Prepared nanosuspensions were evaluated for particle size and in vitro dissolution. A 3 2 central composite design was employed to study the effect of the independent variables (i.e., amount of Pluronic F127, X 1 , and amount of ZrO 2 , X 2 ) on the dependent variables (i.e., particle size [nm] and percentage of drug released after 10 min, Q 10 ). The relationship between the dependent and independent variables was further elucidated using multiple liner regression analysis (MLRA) and contour plots. The results show that nanosuspensions prepared with the higher concentrations of Pluronic F127 and the higher quantities of ZrO 2 (up to 8 g) reduced the particle size and enhanced the dissolution rate of the formulation. The dissolution rate of the optimized nanosuspension was enhanced (64% in 10 min) relative to that of a micronized suspension of simvastatin (3.5% in 10 min), mainly because of the formation of nanosized particles. These results show that the preparation of simvastatin-loaded nanosuspensions significantly improved the in vitro dissolution rate, thus possibly enhancing the fast onset of therapeutic drug effect.
Celecoxib is a poorly water-soluble drug, and bioavailability from its crystalline form is very low. The purpose of the present investigation was to increase the solubility and dissolution rate of celecoxib by preparing a solid dispersion with polyvinyl pyrrolidone K30 (PVP-K30) using a solvent-evaporation method. The dissolution profiles of developed formulations in distilled water containing 1% SLS were studied. Drug-polymer interactions were investigated using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). For the preparation of celecoxib fast-dissolve tablets, a 1:2 solid dispersion with PVP-K30 was used with croscarmellose sodium as a superdisintegrant and Pearlitol 200SD (pearlitol) as a pore-forming agent. A 3 2 full-factorial design was employed to study the effect of independent variables, the amounts of croscarmellose sodium (X 1 ) and pearlitol (X 2 ), on dependent variables, disintegration time, percentage friability, wettability, and percentage of drug released after 20 min (Q 20 ). The results show that a dispersion of the drug in polymer considerably enhanced the dissolution rate. The drug-to-carrier ratio is the controlling factor for dissolution improvement. FTIR spectra show no chemical incompatibility between the drug and PVP-K30. FTIR and DSC data indicate that celecoxib was in the amorphous form, which explains the faster dissolution rate of the drug from its solid dispersions. Concerning the optimization study, multiple regression analysis reveals that an optimum concentration of croscarmellose sodium and a higher percentage of pearlitol are required for obtaining rapidly disintegrating tablets.
Low oral bioavailability of poorly water-soluble drugs poses a great challenge during drug development. Poorly water-soluble compounds are difficult to develop as drug products using conventional formulation techniques and are frequently abandoned early in discovery. The aim of the this study was to improve the dissolution rate of a poorly water-soluble drug famotidine, by a nanoprecipitation technique. Selected parameters of the nanoprecipitation method, such as the amount of Lutrol F-68 and stirring speed were varied so as to obtain drug nanoparticles. The combination of lowest amount of stabilizer with low speed yield bluish white transparent nanosuspensions with the smallest average particle size (566 nm). In contrast to the very slow dissolution rate of pure famotidine, the nanosuspension of the drug considerably enhanced the dissolution rate. Nanosuspension prepared with 0.25% Lutrol F-68 with 1000 rpm showed the most improvement in dissolution rate of famotidine. The formulation of famotidine as a nanosuspension was very successful in enhancing dissolution rate, more than 42% of the drug being dissolved in the first 10 min (batch F1) compared to less than 2.5% of the micronized drug (batch F7).
Nanoparticles have unique properties as compared to micro or macro particles. Different types of nanoparticulate material use in electronic, magnetic, pharmaceutical, cosmetic, energy, catalytic and materials industries. Nanoparticles can be produced by biological, chemical or physical processes. Several of these processes have been known for a long time, while others are new technologies. Nanoparticles are also used in the medical field to aid in drug delivery and medical imaging. Nanoparticles are solid colloidal drug carriers, typically made of a single material, in which a drug is entrapped, encapsulated or adsorbed onto the surface. In pharmaceutical field, it is estimated that about 40% of newly developed drugs will be poorly soluble in future. The poor solubility even makes it very difficult to perform the pharmacological screening of compounds for potential drug effects. With help of nanoparticle technology, this can be solving. Nanoparticle technology is currently taking prominence in the market. This review presents the production process of nanoparticles, characterization techniques & its clinical aspects
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