Next Generation Precision-Polyesters Enabling Optimization of Ligand–Receptor Stoichiometry for Modular Drug Delivery

The success of receptor-mediated drug delivery primarily depends on the ability to optimize ligand–receptor stoichiometry. Conventional polyesters such as polylactide (PLA) or its copolymer, polylactide-co-glycolide (PLGA), do not allow such optimization due to their terminal functionality. We herei...

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Bibliographic Details
Published in:Journal of the American Chemical Society 2017-05, Vol.139 (21), p.7203-7216
Main Authors: Ganugula, Raghu, Arora, Meenakshi, Saini, Prabhjot, Guada, Melissa, Kumar, Majeti N. V. Ravi
Format: Article
Language:English
Subjects:
Caco-2 Cells
Drug Carriers - chemistry
Drug Delivery Systems
Humans
Lactic Acid - chemical synthesis
Lactic Acid - chemistry
Ligands
Molecular Structure
Nanoparticles - chemistry
Particle Size
Polyesters - chemical synthesis
Polyesters - chemistry
Polyglycolic Acid - chemical synthesis
Polyglycolic Acid - chemistry
Receptors, Transferrin - chemistry
Xanthones - chemistry
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Summary:The success of receptor-mediated drug delivery primarily depends on the ability to optimize ligand–receptor stoichiometry. Conventional polyesters such as polylactide (PLA) or its copolymer, polylactide-co-glycolide (PLGA), do not allow such optimization due to their terminal functionality. We herein report the synthesis of 12 variations of the PLA–poly­(ethylene glycol) (PEG) based precision-polyester (P2s) platform, permitting 5–12 periodically spaced carboxyl functional groups on the polymer backbone. These carboxyl groups were utilized to achieve variable degrees of gambogic acid (GA) conjugation to facilitate ligand–receptor stoichiometry optimization. These P2s-GA combined with fluorescent P2s upon emulsification form nanosystems (P2Ns) of size
ISSN:0002-7863
1520-5126
DOI:10.1021/jacs.6b13231