TY - GEN
T1 - Thermodynamic limits on drug loading in nanopartiele cores
AU - Kumar, Varun
AU - Prud'homme, Robert K.
PY - 2007
Y1 - 2007
N2 - Recently, biodegradable nanoparticles based on block copolymers have attracted attention as effective drug delivery vehicles. Maximizing the amount of drug loaded into particle is the desired goal, but experimental results find loading only between 3 to about 25 wt% drug (for paclitaxel). The reasons for the low loading and variability in loading have not been fully explained. In this study, we present a model that quantitatively explains the observed phenomena. The thermodynamic model of drag loading is based on the molar free energy of the drug, which depends on the block copolymers size (entropic term), the interaction parameter between the drug and the hydrophobic core (enthalpic term), and the pressure-volume work to load the particle. The pressure-volume work, related directly to the interfacial tension between the core and the corona region, has not been previously considered with respect to drug loading. To validate the model, calculations were compared with experimental results for organic solutes, including paclitaxel, loaded into poly(ethylene glycol)-b-poly(ε-caprolactone), PEG-b-PCL block copolymer micelles. The model developed was found to predict the loading values in close agreement with experiments reported in literature.
AB - Recently, biodegradable nanoparticles based on block copolymers have attracted attention as effective drug delivery vehicles. Maximizing the amount of drug loaded into particle is the desired goal, but experimental results find loading only between 3 to about 25 wt% drug (for paclitaxel). The reasons for the low loading and variability in loading have not been fully explained. In this study, we present a model that quantitatively explains the observed phenomena. The thermodynamic model of drag loading is based on the molar free energy of the drug, which depends on the block copolymers size (entropic term), the interaction parameter between the drug and the hydrophobic core (enthalpic term), and the pressure-volume work to load the particle. The pressure-volume work, related directly to the interfacial tension between the core and the corona region, has not been previously considered with respect to drug loading. To validate the model, calculations were compared with experimental results for organic solutes, including paclitaxel, loaded into poly(ethylene glycol)-b-poly(ε-caprolactone), PEG-b-PCL block copolymer micelles. The model developed was found to predict the loading values in close agreement with experiments reported in literature.
KW - Aggregation number
KW - Blob size
KW - Drag delivery
KW - Interaction parameter
KW - Interfacial energy
KW - Micelle
KW - Nanoparticles
KW - Paclitaxel
KW - Particle size
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M3 - Conference contribution
AN - SCOPUS:80053655705
SN - 9780816910229
T3 - AIChE Annual Meeting, Conference Proceedings
BT - 2007 AIChE Annual Meeting
T2 - 2007 AIChE Annual Meeting
Y2 - 4 November 2007 through 9 November 2007
ER -