RESUMO
OBJECTIVE: A number of natural polymer-based drug delivery systems targeting the colon are reported for different applications. Most of the research is based on the class of natural polymers such as polysaccharides. This study compares the anti-inflammatory effect of different polysaccharide based tablets on IBD when a drug carrier is targeted to the colon as matrix and coated systems. METHODS: The TNBS induced IBD Wistar rats were used as a model for the study. The microscopic and macroscopic parameters were studied in detail. Almost all the important IBD parameters were reported in this work. RESULTS: The results demonstrated that the polysaccharides are efficient in carrying the drugs to the colon. Reduction in the level of ulcer index (UI), Myeloperoxidase (MPO), and Malondialdehyde MDA, confirmed the inhibitory activity on the development of Reactive oxygen species (ROS). The increased level of Tumor necrosis factor (TNFα) an expression of colonic inducible nitric oxide synthase (iNOS) was lowered in treatments as compared to TNBS control. CONCLUSION: The different polymer-based mesalamine (DPBM) confirmed the efficient anti- inflammatory activity on IBD induced rats. The increased level of glutathione (GSH), and superoxide dismutase (SOD) also confirmed the effective anti-inflammatory effect. A significant decrease in the ulcer score and ulcer area was reported. The investigation revealed that chitosan is superior to pectin in IBD treatment likewise polysaccharide-based matrix systems are superior to the coated system.
Assuntos
Anti-Inflamatórios/uso terapêutico , Colo/patologia , Sistemas de Liberação de Medicamentos/métodos , Doenças Inflamatórias Intestinais/tratamento farmacológico , Mesalamina/química , Pectinas/química , Úlcera/tratamento farmacológico , Animais , Anti-Inflamatórios/química , Quitosana/química , Modelos Animais de Doenças , Humanos , Ratos , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo , Ácido TrinitrobenzenossulfônicoRESUMO
The study was designed to investigate the in vitro dissolution profile and compression characteristics of colon targeted matrix tablets prepared with HPMC E15 LV in combination with pectin and Chitosan. The matrix tablets were subjected to two dissolution models in various simulated fluids such as pH 1.2, 6, 6.8, 7.2, 5.5. The fluctuations in colonic pH conditions during IBD (inflammatory bowel disease) and the nature of less fluid content in the colon may limit the expected drug release in the polysaccharide-based matrices when used alone. The Hydrophilic hydroxyl propyl methylcellulose ether premium polymer (HPMC E15 LV) of low viscosity grade was used in the formulation design, which made an excellent modification in physical and compression characteristics of the granules. The release studies indicated that the prepared matrices could control the drug release until the dosage form reaches the colon and the addition HPMC E15 LV showed the desirable changes in the dissolution profile by its hydrophilic nature since the colon is known for its less fluid content. The hydrophilic HPMC E15 LV allowed the colonic fluids to enter into the matrix and confirmed the drug release at the target site from a poorly water soluble polymer such as Chitosan and also from water soluble Pectin. The dramatic changes occurred in the drug release profile and physicochemical characteristics of the Pectin, Chitosan matrix tablets when a premium polymer HPMC E15 LV added in the formulation design in the optimized concentration. Various drug release mechanisms used for the examination of drug release characteristics. Drug release followed the combined mechanism of diffusion, erosion, swelling and polymer entanglement. In recent decade, IBD attracts many patents in novel treatment methods by using novel drug delivery systems.
Assuntos
Quitosana/administração & dosagem , Colo/efeitos dos fármacos , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos , Mesalamina/administração & dosagem , Pectinas/administração & dosagem , Animais , Quitosana/química , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/química , Concentração de Íons de Hidrogênio , Mesalamina/química , Metilcelulose/administração & dosagem , Metilcelulose/química , Patentes como Assunto , Pectinas/química , Polímeros , Ratos , Comprimidos/químicaRESUMO
A melt dispersion technique was employed to prepare ofloxacin lipospheres, by using cetyl alcohol (polar lipid). Effects of various process parameters such as selection of surfactants (gelatin, Tween 40 and poly vinyl alcohol) and selection of stirring speed were studied. Lipospheres were evaluated for morphology, drug entrapment and in vitro drug release profiles. The optimized liposphere batch was selected and formulated as tablets and evaluated the in vitro drug release profile. These studies showed that ofloxacin loaded lipospheres were able to control the drug release for a period of 16h.
