title: Liquid crystalline systems for transdermal delivery of celecoxib: in vitro drug release and skin permeation studies.
abstract: Liquid crystalline systems of monoolein/water could be a promising approach for the delivery of celecoxib (CXB) to the skin because these systems can sustain drug release, improve drug penetration into the skin layers and minimize side effects. This study evaluated the potential of these systems for the delivery of CXB into the skin based on in vitro drug release and skin permeation studies. The amount of CXB that permeated into and/or was retained in the skin was assayed using an HPLC method. Polarizing light microscopy studies showed that liquid crystalline systems of monoolein/water were formed in the presence of CXB, without any changes in the mesophases. The liquid crystalline systems decreased drug release when compared to control solution. Drug release was independent of the initial water content of the systems and CXB was released from cubic phase systems, irrespective of the initial water content. The systems released the CXB following zero-order release kinetics. In vitro drug permeation studies showed that cubic phase systems allowed drug permeation and retention in the skin layers. Cubic phase systems of monoolein/water may be promising vehicles for the delivery of CXB in/through the skin because it improved CXB skin permeation compared with the control solution.
authors: School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, São Paulo, Brazil.
authors: Eder André
authors: EA
authors: Estracanholli
authors: Fabíola Silva Garcia
authors: FS
authors: Praça
authors: Ana Beatriz
authors: AB
authors: Cintra
authors: Maria Bernadete Riemma
authors: MB
authors: Pierre
authors: Marilisa Guimarães
authors: MG
authors: Lara
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000068579:Celecoxib; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005989:Glycerides / Q000737:chemistry*; D007700:Kinetics; D050866:Liquid Crystals; D008859:Microscopy, Polarization; D010539:Permeability; D011720:Pyrazoles / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism*; D013552:Swine; D013678:Technology, Pharmaceutical / Q000379:methods; D014867:Water / Q000737:chemistry*
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005989:Glycerides; D011720:Pyrazoles; D013449:Sulfonamides; D014867:Water; C005953:monoolein; D000068579:Celecoxib