Multiunit floating drug delivery system of rosiglitazone maleate: development, characterization, statistical optimization of drug release and in vivo evaluation.
A multiunit floating drug delivery system of rosiglitazone maleate has been developed by encapsulating the drug into Eudragit RS100 through nonaqueous emulsification/solvent evaporation method. The in vitro performances of microspheres were evaluated by yield (%), particle size analysis, drug entrapment efficiency, in vitro floating behavior, surface topography, drug-polymer compatibility, crystallinity of the drug in the microspheres, and drug release studies. In vitro release was optimized by a {3, 3} simplex lattice mixture design to achieve predetermined target release. The in vivo performance of the optimized formulation was evaluated in streptozotocin-induced diabetic rats. The results showed that floating microspheres could be successfully prepared with good yields (69-75%), high entrapment (78-97%), narrow size distribution, and desired target release with the help of statistical design of experiments from very small number of formulations. In vivo evaluation in albino rats suggested that floating microspheres of rosiglitazone could be a promising approach for better glycemic control.
Mohan Kamila
Madan
M
Pharmaceutics Research Laboratory-II, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700 032, India. mmkamila@research.jdvu.ac.in
Mondal
Nita
N
Kanta Ghosh
Lakshmi
L
Kumar Gupta
Bijan
B
D000818:Animals; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005753:Gastric Mucosa / Q000378:metabolism; D041981:Gastrointestinal Tract / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D053758:Nanoparticles; D010316:Particle Size; D051381:Rats; D000077154:Rosiglitazone; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D045162:Thiazolidinediones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D014961:X-Ray Diffraction
D003692:Delayed-Action Preparations; D007004:Hypoglycemic Agents; D045162:Thiazolidinediones; D000077154:Rosiglitazone