Formulation and optimization of nonionic surfactants emulsified nimesulide-loaded PLGA-based nanoparticles by design of experiments.
This investigation aimed to develop nimesulide (NMS)-loaded poly(lactic-co-glycolic acid) (PLGA)-based nanoparticulate formulations as a biodegradable polymeric drug carrier to treat rheumatoid arthritis. Polymeric nanoparticles (NPs) were prepared with two different nonionic surfactants, vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) and poly(vinyl alcohol) (PVA), using an ultrasonication solvent evaporation technique. Nine batches were formulated for each surfactant using a 3(2) factorial design for optimal concentration of the emulsifying agents, 0.03-0.09% for vitamin E TPGS and 2-4% for PVA. The surfactant percentage and the drug/polymer ratio (1:10, 1:15, 1:20) of the NMS-loaded NPs were investigated based on four responses: encapsulation efficiency, particle size, the polydispersity index, and the surface charge. The response surface plots and linearity curves indicated a relationship between the experiment's responses and a set of independent variables. The NPs produced with both surfactants exhibited a negative surface charge, and scanning electron micrographs revealed that all of the NPs were spherical in shape. A narrower size distribution and higher drug loadings were achieved in PVA-emulsified PLGA NPs than in the vitamin E TPGS emulsified. Decreasing amounts of both nonionic surfactants resulted in a reduction in the emulsion's viscosity, which led to a decrease in the particle size of NPs. According to the ANOVA results obtained in this present research, vitamin E TPGS exhibited the best correlation between the independent variables, namely drug/polymer ratio and the surfactant percentage, and the dependent variables (encapsulation efficiency R(2) = 0.9603, particle size R(2) = 0.9965, size distribution R(2) = 0.9899, and surface charge R(2) = 0.8969) compared with PVA.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, 06100, Tandogan, Ankara, Turkey.
Ceyda Tuba Sengel
CT
Turk
Umut Can
UC
Oz
Tugrul Mert
TM
Serim
Canan
C
Hascicek
D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D004655:Emulsions / Q000737:chemistry*; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry; D011142:Polyvinyl Alcohol / Q000737:chemistry; D013449:Sulfonamides / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry*; D014810:Vitamin E / Q000031:analogs & derivatives / Q000737:chemistry
D004337:Drug Carriers; D004655:Emulsions; D011108:Polymers; D013449:Sulfonamides; D013501:Surface-Active Agents; D014810:Vitamin E; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D011142:Polyvinyl Alcohol; C014225:tocophersolan; C012655:nimesulide