title: Comparing various techniques to produce micro/nanoparticles for enhancing the dissolution of celecoxib containing PVP.
abstract: One of the major challenges in pharmaceutical development is the poor dissolution performance of drugs. Celecoxib (CLX) is a poorly water soluble drug with its bioavailability being limited by its poor dissolution. In this study several particle engineering methods were employed on CLX using various ratios of CLX:PVP-K30. Micro/nanoparticles of CLX:PVP were prepared by using spray drying (SD), antisolvent crystallization followed by freeze drying (CRS-FD) and spray drying (CRS-SD) techniques. The suspension obtained through antisolvent crystallization was also subjected to high pressure homogenization followed by freeze drying (HPH-FD). Particle size measurements, saturation solubility, optical and scanning electron microscopy, DSC, XRPD, FT-IR and dissolution test were performed to characterize the physicochemical and pharmaceutical properties of the samples. The results showed that spray dried samples in the presence of (50%) PVP produced spherical particles and exhibited a high dissolution rate. Interestingly in the antisolvent crystallization technique, spherical nanoparticles of drug-PVP were obtained in the range of 291-442 nm. The average particle size was dependent on the concentration of the PVP used during the crystallization process. Solid state analysis showed that these particles were completely amorphous in nature. Also interesting to note was that at concentration of 5% PVP, when the suspension of nanoparticles was subjected to the high pressure homogenization process, the crystallinity of CLX increased. Despite the partial crystallinity of particles produced, they showed excellent dissolution behavior. It can thus be concluded that the method of preparation of CLX micro/nanoparticles had a big impact on the dissolution rate when the concentration of PVP was low (e.g., 5%). At high PVP concentration (e.g., 50%) all methods used to prepare engineered CLX particles showed better dissolution with no significant differences in their dissolution efficiency.
authors: Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
authors: Alireza
authors: A
authors: Homayouni
authors: Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran; Targeted Drug Delivery Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
authors: Fatemeh
authors: F
authors: Sadeghi
authors: School of Pharmacy, Esfahan University of Medical Sciences, Esfahan, Iran.
authors: Jaleh
authors: J
authors: Varshosaz
authors: Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran; Pharmaceutical Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address: hadiafrasiabi@yahoo.com.
authors: Hadi Afrasiabi
authors: HA
authors: Garekani
authors: Medway School of Pharmacy, University of Kent, Chatham Maritime, ME4 4TB Kent, UK; Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. Electronic address: a.nokhodchi@kent.ac.uk.
authors: Ali
authors: A
authors: Nokhodchi
mesh_terms: D002152:Calorimetry, Differential Scanning; D000068579:Celecoxib; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003460:Crystallization; D004337:Drug Carriers; D005612:Freeze Drying; D008863:Microspheres; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011205:Povidone / Q000737:chemistry*; D011312:Pressure; D011720:Pyrazoles / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013449:Sulfonamides / Q000008:administration & dosage* / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D011720:Pyrazoles; D012997:Solvents; D013449:Sulfonamides; D011205:Povidone; D000068579:Celecoxib
keywords: Crystallization; Dissolution rate; High pressure homogenization; Nanoparticles; Solid state; Spray drying