Supramolecular Assembly of Pharmaceuticals and
23rd IUPAC Conference on Physical Organic Chemistry (ICPOC23) 3rd – 8th July 2016 • Sydney • Australia
Supramolecular Assembly of Pharmaceuticals and Polymers A. Rawal,a* M. Callari, M. Stenzel, Vikram J. Pansarec, Robert K. Prud’hommec, Aaron Goodwind a
NMR Facility, UNSW, Sydney, Australia School of Chemistry, UNSW, Sydney, Australia c Department of Chemical and Biological Engineering, Princeton University, Princeton, USA d Bend Research, a Division of Capsugel’s Dosage Form Solution, Bend , USA *[email protected] b
Supramolecular-assembly of pharmaceutical drugs and excipient polymers provides a key technological tool for nano-dispersion, targeted delivery and controlled release of drug molecules. Understanding the specific drug-polymer interactions within the supramolecular assemblies is crucial for designing drug-delivery systems with engineered properties. Here we demonstrate investigations into the architecture of two systems: a) Where the polymer-excipient matrix controls precipitation and nano-crystallinity of a drug molecule; and b) Where the amount of drug binding to the polymer controls the morphology of the resulting drug-polymer micellar structure. In the first case, millisecond co-precipitation of the drug molecule with an excipient polymer matrix, allows for kinetic trapping of drug within the polymer matrix. By choosing an appropriate polymer matrix, the drug molecule is either undergoes molecular level dispersion or forms nano-crystals within the polymer. In the second case, conjugation of a drug to the polymer, results in self-assembly of polymer encapsulated micelles. In this case, controlling the level of drug conjugation, enables control of drug aggregation and release from the micellar structure. For both cases we demonstrate specific and resolvable interactions between the drug-and the polymer and discuss how these interactions guide the supramolecular assembly and the resultant pharmacological properties of the materials. Multinuclear solid-state NMR is the key technique that enables the necessary resolution to identify the specific interactions and with complimentary techniques such as XRD and EM, develop the all-important structure-property relationship in these systems.
CLC4
Supramolecular Assembly of Pharmaceuticals and Polymers A. Rawal,a* M. Callari, M. Stenzel, Vikram J. Pansarec, Robert K. Prud’hommec, Aaron Goodwind a
NMR Facility, UNSW, Sydney, Australia School of Chemistry, UNSW, Sydney, Australia c Department of Chemical and Biological Engineering, Princeton University, Princeton, USA d Bend Research, a Division of Capsugel’s Dosage Form Solution, Bend , USA *[email protected] b
Supramolecular-assembly of pharmaceutical drugs and excipient polymers provides a key technological tool for nano-dispersion, targeted delivery and controlled release of drug molecules. Understanding the specific drug-polymer interactions within the supramolecular assemblies is crucial for designing drug-delivery systems with engineered properties. Here we demonstrate investigations into the architecture of two systems: a) Where the polymer-excipient matrix controls precipitation and nano-crystallinity of a drug molecule; and b) Where the amount of drug binding to the polymer controls the morphology of the resulting drug-polymer micellar structure. In the first case, millisecond co-precipitation of the drug molecule with an excipient polymer matrix, allows for kinetic trapping of drug within the polymer matrix. By choosing an appropriate polymer matrix, the drug molecule is either undergoes molecular level dispersion or forms nano-crystals within the polymer. In the second case, conjugation of a drug to the polymer, results in self-assembly of polymer encapsulated micelles. In this case, controlling the level of drug conjugation, enables control of drug aggregation and release from the micellar structure. For both cases we demonstrate specific and resolvable interactions between the drug-and the polymer and discuss how these interactions guide the supramolecular assembly and the resultant pharmacological properties of the materials. Multinuclear solid-state NMR is the key technique that enables the necessary resolution to identify the specific interactions and with complimentary techniques such as XRD and EM, develop the all-important structure-property relationship in these systems.
CLC4
