Poor aqueous solubility and bioavailability of drugs are one of the important factors affecting the absorption of drugs and consequently their therapeutic effectiveness. Celecoxib is a widely used anti-inflammatory agent, with special use in rheumatoid arthritis. It belongs to biopharmaceutical classification system (BCS) class II drug with low solubility and high permeability. The present study was aimed to prepare and characterize the microcrystals of celecoxib, employing in situ micronization technique by rapid solvent change approach to enhance the solubility and dissolution rate and to optimize the solvent and anti-solvent ratio (v/v) using hydrophilic stabilizers such as guar gum, maltodextrin and PVP K30. The prepared formulations were evaluated for percentage crystal yield, mean particle size, drug content and in vitro dissolution studies. Amongst the formulations prepared (F1-F9), F6 formulation containing maltodextrin as stabilizing agent at 0.1% w/v concentration with 1:6 ratio of solvent to anti-solvent (v/v) respectively was considered as optimized formulation in which percentage drug release was found to be 89.33% within 60 minutes in comparison with that of the pure drug dissolution of 30.26% only within 60 minutes. Characterization studies like SEM, DSC and XRD indicate the solubility enhancement of celecoxib microcrystals due to decrease in particle size when compared to that of pure drug. FT-IR spectroscopy studies revealed that there is no chemical interaction between the drug and stabilizer and crystalline habit modification occurs in the microcrystals without any polymorphic changes.
The aim of the present study was an attempt to prepare tablets containing inclusion complexes of meloxicam with β-cyclodextrins and hydroxypropyl-β-cyclodextrin to improve the aqueous solubility of the drug, thus enhances its dissolution rate to show a faster onset of action. Complexation with cyclodextrins has been used as novel approach for designing drug delivery system because of ability for the non-covalent inclusion complexes formation and it has the ability to molecular encapsulate meloxicam into their hydrophobic cavity without the formation of any covalent bonds. Meloxicam complexation with cyclodextrin enhance the drug solubility and dissolution rate. Also cyclodextrins enhance the bioavailability of insoluble drugs by increasing the drug solubility, dissolution and permeability. The carriers used in this study are β-cyclodextrin and hydroxypropyl-β-cyclodextrin. Solid complexes of meloxicam with β-cyclodextrin and hydroxypropyl-β-cyclodextrin were prepared by two different methods namely, Kneading and Co-evaporation techniques. For kneading method, water-methanol-dichloromethane at 2 : 5 : 3 ratio was used as a solvent blend and for co-evaporation techniques, methanol-dichloromethane was used as solvent blend at 2 : 3 ratio. In each case different proportions of drug and carriers at 90 : 10, 75 : 25, 50 : 50, 25 : 75, 10 : 90 were used in the preparation of solid complexes to evaluate the effect of carrier concentrations on the dissolution characteristics. A total of 20 meloxicam solid complexes with different carriers were prepared, found to be fine and free flowing powders. The estimated drug content of the prepared complexes were in the range of 100 ± 5%. The dissolution parameters of T50 and dissolution rate indicated rapid dissolution of meloxicam from the solid complexes when compared with the pure drug and physical mixture. Meloxicam-β-CD (10 : 90) complex gave the highest dissolution rate.
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