SOLID DISPERSION TECHNIQUE TO ENHANCE THE SOLUBILITY AND DISSOLUTION OF FEBUXOSTAT AN BCS CLASS II DRUG

Objective: The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers.Methods: Pre-formulation studies like drug excipient compatibility studies by Fourier-transform infrared spectroscopyDifferential scanning calorimetry and determination of saturation solubility of drug individually in various media like distilled water and pH 7.4 phosphate buffer. Solid dispersions of Febuxostat was prepared using Polyethylene glycol (PEG 6000) (fusion method) and Polyvinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies.Results: From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 54-78 %, and drug content was in the range of 43-78 mg. The solid dispersion containing polyvinylpyrrolidone K 30 in 1:4 ratio showed the highest amount of drug release at the end of 30 min than other formulations.Conclusion: Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method

Comparative in vitro evaluation of glimepiride containing nanosuspension drug delivery system developed by different techniques

The present study was aimed to develop the Glimepiride (GLM) loaded nanosuspension by different methods for increasing the solubility of GLM. Twelve formulations were prepared by combination method (FG), which included antisolvent precipitation method followed by sonication (Method 1) selecting drug and polymer in ratio of 1:10, 1:20 and 1:30. Further 6 formulations were prepared by nanoprecipitation method (Fg) (Method 2) selecting drug and polymer in ratio of 1:10, 1:20 by using different polymers like polyvinyl pyrolidone (PVP K30), and poly(ethylene glycol) (PEG) such as PEG 6000 and PEG 400. The GLM nanosuspensions prepared by different techniques were evaluated by optical microscopy, percent entrapment efficiency (%EE), particle size analysis, zeta potential, transmission electron microscopy (TEM) and in vitro dissolution. FG1 formulation was found to be better formulation showing 82.04% EE, 129–180 nm particle size range, 30.16 mV zeta potential, 0.253 polydispersity index (PDI) and 86.76% drug release as compared to Fgii formulation having %EE, average particle size, zeta potential, PDI value and drug release as 80.03%, 72–383 nm, -22.19 mV, 0.358 and 74.77%, respectively. On the basis of results obtained from different studies, it can be concluded that GLM nanosuspension prepared by combination technique (FG) shows good solubility and dissolution than those prepared by nanoprecipitation technique (Fg), hence the combination technique is found to be a preferred technique to prepare GLM nanosuspension over nanoprecipitation technique

A simple desolvation method for production of cationic albumin nanoparticles with improved drug loading and cell uptake

The transport protein albumin has been used as a drug nanocarrier for a long time due to its versatility. Albumin is negatively charged at physiological conditions limiting its anionic drug loading capacity. However, loading of anionic drugs in the albumin nanoparticles (NPs), can be facilitated by albumin cationization. Here, we postulate a simple desolvation method for preparation of cationic albumin NPs with improved anionic drug loading. First, bovine serum albumin was cationized with ethylenediamine. Next, salicylic acid (SA) was added to the cationic bovine serum albumin (cBSA) solution prior to the desolvation. Among different desolvating agents tested, acetonitrile allowed the highest nanoparticle formation yield. The SEM analyses showed that the average size of cBSA NPs decreased from similar to 200 nm to similar to 100 nm upon SA loading. Moreover, the drug loading capacity of cBSA NPs was found to increase similar to 2 fold, and drug release was slower compared to BSA NPs. Finally, a significant increase in cellular uptake of cBSA NPs compared to that of native BSA NPs showed the potential for improved drug delivery