Inflammation is a complex pathophysiological process mediated by a variety of signaling molecules and can be classified as either acute or chronic. Anti inflammatory drugs are broadly classified into two categories: Steroidal and Non steroidal anti-inflammatory agents (NSAIDs) some of them are no longer used due to their severe adverse effects. Traditionally, people have been using powerful anti-inflammatory plants for thousands of years as part of their diet and pharmaceutical arsenal, and secondary compounds derived from these plants may offer important sources of anti-inflammatory agents.
Objective: The objective of the present study was to improve the aqueous solubility and dissolution characteristics of the loop diuretic furosemide (FUR); a class IV drug in the Biopharmaceutical Classification System (BCS) using solid dispersion technique.
Methods: Solvent evaporation and kneading methods were used to produce solid dispersions of FUR in different ratios with the hydrophilic carrier polyvinylpyrrolidone K-30 (PVP-K30). The prepared solid dispersions were evaluated in terms of solubility study, percentage yield, drug content and Fourier transform infrared spectroscopic study (FT-IR). Tablets containing the optimized formula of solid dispersions ( were formulated and their dissolution characteristics were compared with commercial furosemide tablets.
Results: The prepared solid dispersions showed an increase in aqueous solubility, especially those formulated in a 1:2 drug: carrier ratio using solvent evaporation method ( it showed a four-fold increase in solubility compared to the parent drug. The absence of drug-carrier chemical interactions that could affect the dissolution was proved by FT-IR. Solid dispersion tablets exhibited a better dissolution profile in simulated gastric fluid pH 1.2 at 37°C ± 0.5 than the commercial FUR tablets in terms of mean dissolution time (8.44 min) and dissolution efficiency in 30 min (42.54%). Both FUR solid dispersions and commercial tablets followed Weibull and Krosmeyer models as the two best models of drug release kinetics proving that they were immediate release.
Conclusion: According to the results obtained in this study, solid dispersion techniques could be successfully used for the enhancement of aqueous solubility and dissolution rate of FUR.
Objective: The aim of this study was to explore the individual and joint effects of drug: ethylcellulose ratio, content of tween 80 and chloroform: water volume ratio on particles' size and size distribution of artemether loaded ethyl cellulose nanosuspension formulations, aiming to achieve nanosuspension with desired particles properties, stability and drug release profile.Methods: Mixed levels design was used to generate a series of artemether loaded ethylcellulose nanosuspensions that produced by emulsificationsolvent evaporation technique. Formulations were qualified for particle size and size distribution using dynamic light scattering technique. Best ranked formulation was then evaluated for stability and drug release rate and kinetics.Results: Drug: polymer ratio, content of surfactant and organic: water volume ratio were found to exert considerable influences (p<0.05) on particle size of produced nanosuspensions, either individually or as joint variables. Peak intensity property of nanosuspensions was found to be influenced by drug: polymer ratio (p<0.05) whereas the influences of different variables on the polydisperse index property appear inconsequential (p>0.05). Best ranked (optimal) artemether nanosuspension proved stable and capable to improve and maintain the release of loaded drug over 24 h, at least under the setting conditions of this study.
Conclusion:Focusing on both the individual and joint influences of formulation variables assist in achieving nanosuspension with desired particles characteristics, stability and drug release profile.
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