This study indicates that owing to nanosize, SNEDDS and S-SNEDDS of FLD have potential to enhance its absorption and may serve an efficient oral delivery.

In this investigation, multivariate design approach was employed to develop self-nanoemulsifying drug delivery system (SNEDDS) of loratadine and to exploit its potential for intestinal permeability. Drug solubility was determined in various vehicles and existence of self-nanoemulsifying region was evaluated by phase diagram studies. The influence of formulation variables X1 (Capmul MCM C8) and X2 (Solutol HS15) on SNEDDS was assessed for mean globule sizes in different media (Y1-Y3), emulsification time (Y4) and drug-release parameters (Y5-Y6), to improve quality attributes of SNEDDS. Significant models were generated, statistically analyzed by analysis of variance and validated using the residual and leverage plots. The interaction, contour and response plots explicitly demonstrated the influence of one factor on the other and displayed trend of factor-effect on responses. The pH-independent optimized formulation was obtained with appreciable global desirability (0.9266). The strenuous act of determining emulsification time is innovatively replaced by the use of oil-soluble dye to produce visibly distinct globules that otherwise may be deceiving. TEM images displayed non-aggregated state of spherical globules (size < 25 nm) and also revealed the structural transitions occurring during emulsification. Optimized formulation exhibited non-Newtonian flow justified by the model-fit and also presented the stability to dilution effects and thermodynamic stress testing. The ex vivo permeation study using confocal laser scanning microscopy indicate strong potential of rhodamine 123-loaded loratadine-SNEDDS to inhibit P-gp efflux and facilitate intestinal permeation. To conclude, the effectiveness of design yields a stable optimized SNEDDS with enhanced permeation potential, which is expected to improve oral bioavailability of loratadine.

(2013) Crystalline and amorphous carvedilolloaded nanoemulsions: formulation optimisation using response surface methodology, Journal of Experimental Nanoscience, 8:7-8, 971-992, DOI: 10.1080/17458080.2011 This study aimed to evaluate the crystalline and amorphous carvedilol along with their lipidic mixtures using various instrumental techniques and to use response surface methodology in conjunction with factorial design to establish the functional relationships between operating variables (capmul GMS 50 K and cremophor RH 40). The response variables selected are spectroscopic absorbance (Y 1 ), mean particle size in distilled water (Y 2 ) and in phosphate buffer pH 6.8 (Y 3 ), polydispersibility index (PDI) (Y 4 ) and zeta potential (Y 5 ). The optimal formulations of crystalline and amorphous carvedilol-loaded nanoemulsions were composed of fixed levels, À0.41 and À0.42, of capmul GMS 50 K and cremophor RH 40, respectively. The predicted and observed values of Y 1 -Y 5 for blank nanoemulsions showed the percentage bias error of À12.12%, À10.25%, À18.47%, þ14.81 and À2.89, respectively. The bias percent ranged between À2.70% and À29.41% for the responses Y 1 -Y 4 for both crystalline and amorphous carvedilol-loaded nanoemulsions, indicating high degree of prognosis. However, the bias percent values for the response variable Y 5 were 294.2% and 262.6%, for the crystalline and amorphous carvedilol-loaded nanoemulsions, respectively, possibly due to cationisation of emulsion droplets. The transmission electron microscopy of selected optimal nanoemulsions showed the spherical shape of globules with no signs of coalescence and precipitation of drug. This study demonstrates the use of factorial design for the preparation of nanoemulsions of crystalline and amorphous carvedilol. The desirable goals can be obtained by systematic formulation approach in the shortest possible time.

Hydrophilic and hydrophobic grades of Aerosil® were employed to develop solid-SNEDDS of loratadine and evaluated for their influence on powder, physicochemical and biopharmaceutical properties.