Enhancement of the dissolution and permeation rates of meloxicam by formation of its freeze-dried solid dispersions in polyvinylpyrrolidone K-30.
Freeze-drying (FD) and solvent evaporation (SE) were used to prepare solid dispersions (SDs) of meloxicam (MX) in polyvinylpyrrolidone K-30 (PVP). The SDs were prepared at different ratios, namely 1:1, 1:3, and 1:5 MX:PVP weight ratio. Differential scanning calorimetry (DSC), infrared absorption spectroscopy (IR), and x-ray powder diffractometry (XPD) were utilized to characterize the physicochemical properties of the SDs. Meloxicam (MX) in the solid dispersions appeared with less crystallinity form and was present in a complete amorphous form at higher PVP ratio. Dissolution rates of MX as a pure drug, physical mixtures (PMs), and SDs indicated a marked increase of the dissolution rate of MX in presence of PVP. The increase in the dissolution rate was dependent on the ratio of PVP and the method of preparation. In addition, the permeability of the drug through standard cellophane membrane and hairless mouse skin was also evaluated. The permeation rate of MX was significantly increased in the case of SDs and was dependent on the ratio of PVP. The results were primarily due to increase wettability, the solubilization of the drug by the carrier, and formation of MX amorphous form.
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, 71526, Assiut, Egypt.
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El-Badry
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Fathy
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D005260:Female; D005612:Freeze Drying; D066298:In Vitro Techniques; D000077239:Meloxicam; D051379:Mice; D010539:Permeability; D011205:Povidone / Q000737:chemistry*; D012869:Skin Absorption; D012995:Solubility; D013055:Spectrophotometry, Infrared; D013843:Thiazines / Q000737:chemistry* / Q000493:pharmacokinetics; D013844:Thiazoles / Q000737:chemistry* / Q000493:pharmacokinetics; D014961:X-Ray Diffraction
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013843:Thiazines; D013844:Thiazoles; D011205:Povidone; D000077239:Meloxicam