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chitosan and plga microspheres as drug delivery ... - UniCA Eprints

chitosan and plga microspheres as drug delivery ... - UniCA Eprints

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1. General Introductionsphere preparation temperature. The authors found that the highest encapsulation efficienciesoccurred at the lowest <strong>and</strong> highest formation temperatures tested (about 50% at 4 <strong>and</strong> 38°C,<strong>and</strong> about 19% at 22 <strong>and</strong> 29°C). The non-linear <strong>drug</strong> loading trend suggested that differentmechanisms governed the encapsulation process at different temperatures. When consideringthe relation of the polymer itself to encapsulation efficiency, Ghaderi et al. (138) found thatincre<strong>as</strong>ing the concentration of polymer in the organic ph<strong>as</strong>e incre<strong>as</strong>ed the encapsulationefficiency. An incre<strong>as</strong>e in E% from 1 to 25% w<strong>as</strong> observed depending on the concentration ofthe polymer.Microsphere size can be affected by the polymer concentration, temperature, viscosity, thestirring rate, <strong>and</strong> the amount of emulsifier employed. Considering the effect of polymerconcentration, it h<strong>as</strong> often been reported that incre<strong>as</strong>ing the concentration of polymerincre<strong>as</strong>es sphere size (138, 139, 140, 141, 142). Yang et al. (137) used scanning electronmicroscopy (SEM) to show that sphere size w<strong>as</strong> temperature dependent; lower <strong>and</strong> highertemperatures produced larger spheres where<strong>as</strong> intermediate temperatures produced smallerspheres. Once again, different mechanisms dominated microsphere formation at differenttemperatures. At lower temperatures, the solution’s higher viscosity resulted in the formationof larger spheres; this h<strong>as</strong> also been confirmed by other researchers (143). Larger sphereswere obtained at higher temperatures due to the higher rate of solvent evaporation whichresulted in higher solvent flow pressure moving more material from the sphere center outward(137).Jalil <strong>and</strong> Nixon (144) studied the variation of sphere size with respect to the stirring rate <strong>and</strong>the influence of the emulsifier in the second emulsion step. It w<strong>as</strong> shown that <strong>microspheres</strong>ize decre<strong>as</strong>ed with incre<strong>as</strong>ing stirring rate since incre<strong>as</strong>ed stirring results in the formation offiner emulsions. Little change in diameter size w<strong>as</strong> reported by varying emulsifierconcentration.Controlled rele<strong>as</strong>e is an attainable <strong>and</strong> desirable characteristic for DDS. The factors affectingthe <strong>drug</strong> rele<strong>as</strong>e rate revolve around the structure of the matrix where the <strong>drug</strong> is contained<strong>and</strong> the chemical properties <strong>as</strong>sociated with both the polymer <strong>and</strong> the <strong>drug</strong>. Conventional oral<strong>delivery</strong> is not rate controlled. A <strong>drug</strong> encapsulated in a slowly degrading matrix provides theopportunity for slower rele<strong>as</strong>e effects, but polymer degradation is not the only mechanism forthe rele<strong>as</strong>e of a <strong>drug</strong>. The <strong>drug</strong> rele<strong>as</strong>e is also diffusion controlled <strong>as</strong> the <strong>drug</strong> can travelthrough the pores formed during sphere hardening. In some c<strong>as</strong>es, <strong>drug</strong>s containingnucleophilic groups can cause incre<strong>as</strong>ed chain scission of the polymer matrix, which also28

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