Search

Abiraterone acetate is a novel antiandrogen drug indicated for prostate cancer. However, it suffers from low bioavailability owing to poor dissolution properties. The present work was aimed to develop abiraterone acetate nano-micelles to improve its dissolution properties and oral bioavailability. Film hydration method was employed to fabricate the abiraterone acetate nano-micelles. Impact of various variables on the formulation of abiraterone acetate nano-micelles were studied in the preliminary trials. Central composite design was employed with independent variables identified in the preliminary studies, viz. X1- Stirring speed and X2- Stirring time. Drug release studies were carried out to check the change in dissolution properties of abiraterone acetate nano-micelles as compared to pure drug. In vivo animal studies were carried out to check the pharmacokinetic parameters. Drug physical alterations caused by nano-micellization were analyzed by solid state characterization (FTIR, DSC, XRD and SEM) experiments. Accelerated stability studies for six months was carried out on the optimized formulation. Results demonstrated influence of various process variables on particle size of abiraterone acetate nano-micelles. In vitro dissolution showed an increase in drug release rate from nano-micelles as compared to pure drug dispersion. Abiraterone acetate nano-micelle's oral bioavailability significantly improved by 32-fold. Accelerated stability studies of the optimized formulation suggested stability of the nano-micelles for at least six-month time. Thus, dissolution properties and oral bioavailability of abiraterone acetate was enhanced by formulating nano-micelles. [ABSTRACT FROM AUTHOR]

The present work was focussed on the fabrication and development of folic acid conjugated mesoporous nanoparticulate system (FMSNs) of enzalutamide (EFMSNs) for the targeted dug delivery for the management of prostate cancer. Optimization was carried out using design of experiments at two stages i.e. preparation of MSNs and the drug loading employing Box–Behnken design and 23 Factorial design respectively. Batches were evaluated for various parameters including particle size, %yield, %EE, drug release studies. Further, optimized EFMSNs was subjected for characterization studies such as FT-IR and SEM analysis. In vitro cell viability assay demonstrated enhanced efficacy of the nanoparticulate system as compared to pure drug. Stability studies demonstrated pharmaceutical stable formulation for at least 6 month period. Thus, a stable and efficacious nanoparticulate targeted drug delivery system of enzalutamide was developed for the treatment of prostate cancer. [ABSTRACT FROM AUTHOR]

Zotepine is an atypical antipsychotic drug used in the treatment of schizophrenia. However, its poor dissolution properties limit its therapeutic efficacy. In this investigation, a series of nanosuspension-containing zotepine were prepared employing media milling method with an aim to improve its dissolution properties and oral bioavailability. Briefly, Box-Behnken design was applied to investigate the influence of various independent variables such as X1- amount of stabilizer, X2- amount of milling agent, and X3- milling time on the performance of the formulation. Dissolution studies revealed enhancement of dissolution rate as compared to pure drug. Solid state characterization (DSC, PXRD, and SEM) studies demonstrated no polymorphic changes in drug after lyophilization of media-milled nanosuspension. In vivo pharmacokinetic studies of lyophilized nanosuspension was carried out in rat and the results exhibited significant improvement in Cmax and AUC0-t, about 450.0 and 287.45%, respectively, suggesting amelioration in oral bioavailability by 2.87-fold higher as compared to pure drug. Accelerated stability studies of the optimized lyophilized formulation at 40°C and 75% RH suggested stability of the nanocrystals for at least a 6-month period. The obtained nanocrystals successfully showed dissolution enhancement and improved oral bioavailability of poorly water-soluble drug, zotepine. [ABSTRACT FROM AUTHOR]

Ezetimibe (EZE), a water insoluble drug, depicts variable bioavailability. The objective of the present investigation was to improve dissolution characteristics of EZE, which might offer improved bioavailability. The solid dispersions were prepared using poloxamer 407 (L 127) and polyvinyl pyrrolidone by melt and solvent method, respectively. Phase solubility studies indicated linear relationship between drug solubility and carrier concentration. In vitro release studies revealed improvement in the dissolution characteristics of EZE in solid dispersions. Solid dispersion with L 127 gave better rate and extent of dissolution. The best fit model indicating the probable mechanism of drug release from solid dispersions was found to be Korsemeyer-Peppas. The results of characterization of solid dispersions by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction revealed reduction in drug crystallinity which might be responsible for improved dissolution properties. The tablets of solid dispersion, containing L 127 prepared by direct compression, exhibited better drug release as compared to marketed formulation. [ABSTRACT FROM AUTHOR]