A Comparison between Use of Spray and Freeze Drying Techniques for Preparation of Solid Self-Microemulsifying Formulation of Valsartan andIn VitroandIn VivoEvaluation

Abstract

The objective of the present study was to develop self micro emulsifying formulation (SMEF) of valsartan to improve its oral bioavailability. The formulations were screened on the basis of solubility, stability, emulsification efficiency, particle size and zeta potential. The optimized liquid SMEF contains valsartan (20% w/w), Capmul MCM C8 (16% w/w), Tween 80 (42.66% w/w) and PEG 400 (21.33% w/w) as drug, oil, surfactant and co-surfactant, respectively. Further, Liquid SMEF was adsorbed on Aerosol 200 by spray and freeze drying methods in the ratio of 2 : 1 and transformed into free flowing powder. Both the optimized liquid and solid SMEF had the particle size <200 nm with rapid reconstitution properties. Both drying methods are equally capable for producing stable solid SMEF and immediate release of drug in in vitro and in vivo conditions. However, the solid SMEF produced by spray drying method showed high flowability and compressibility. The solid state characterization employing the FTIR, DSC and XRD studies indicated insignificant interaction of drug with lipid and adsorbed excipient. The relative bioavailability of solid SMEF was approximately 1.5 to 3.0 folds higher than marketed formulation and pure drug. Thus, the developed solid SMEF illustrates an alternative delivery of valsartan as compared to existing formulations with improved bioavailability.

Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

“…This method enables entrapment of both hydrophilic and hydrophobic drugs in polymer matrix and compared to other techniques (emulsificationprecipitation, emulsification-cross-linking, ionotropic gelation, solvent evaporation, and coacervation) it might be used in both laboratory and industrial scale. Moreover, it is characterized by the possibility of precisely controlling production parameters, high production yield (40-80%), and encapsulation efficiency (up to 100%) [37][38][39][40]. It was shown that formulated microspheres were characterized by relatively narrow size distribution and MF loading in all formulations was in the range between 37.3±3.8% and 75.6±1.4% (Table 1).…”

Solid-Nanoemulsion Preconcentrate for Oral Delivery of Paclitaxel: Formulation Design, Biodistribution, andγScintigraphy Imaging

“…The samples included pure PAC, solid carrier (POE 4000), and the PAC loaded solid-nanoemulsion preconcentrate. The samples were placed in standard aluminum pans and then scanned at constant heating rate of 10°C/min between 20 and 450°C under a nitrogen gas flow of 20 mL/min [ 29 ].…”

“…The IR spectra were recorded on the FTIR (Jasco FT/IR-410, Japan) by using a potassium bromide pressed disc method. The spectrum was scanned over the frequency range of 4000–400 cm −1 [ 29 ].…”

Proniosomal powders of natural canthaxanthin: Preparation and characterization

“…Particles with high internal friction or cohesion increase the value of angle of repose. Moreover, Carr's index and Hausner's ratio should be less than 20% and 1.25, respectively, to ensure optimal flowability for proniosome powders (Singh, Vuddanda, Singh, & Srivastava, 2013). MDPP showed the lowest angle of repose (25±3°), Carr's index (21±4%) and Hausner's ratio (1.27±0.07) providing the best micromeritics properties among all.…”