Poor tumor accumulation and dose limiting side effects associated with the chemotherapeutic agent temozolomide (TMZ) reduce its potential impact on the life expectancy of those diagnosed with glioblastoma. Despite well-established TMZ treatment regimens, the average life expectancy for glioblastoma patients is 40 – 50 weeks. Improving the tumor accumulation and/ or tolerable dose would allow for increased tumor cell death and ultimately improve the prognosis of glioblastoma. Therefore, it is necessary to explore methods of improving the efficacy of TMZ. It is hypothesized that if TMZ is encapsulated in actively targeted polymeric nanoparticles, the tumor accumulation of TMZ can be improved and the dose limiting side effects can be reduced. To determine the impact of TMZ encapsulation on TMZ efficacy, a polymeric nanoformulation composed of poly (lactic-co-glycolic acid) (PLGA) and chitosan was developed. The particles were decorated with a novel small molecule epidermal growth factor receptor (EGFR) targeting agent. Co-encapsulation of TMZ and cyanine-5, a near-infra red (NIR) hydrophobic dye, offers fluorescence guided imaging options both in-vitro and in-vivo which provides a theranostic approach to treatment. Targeted chitosan coated PLGA nanoparticles were synthesized that demonstrated hydroscopic diameters ranging from 93 – 186 nm. The nanoparticles’ ability to permeate the blood-brain barrier (BBB), a physical barrier which presents a significant challenge in glioblastoma treatment, was analyzed using an in-vitro BBB model. The nanoparticles demonstrated the ability to cross the BBB with a maximum crossing of 7.4% observed after a 48-hour incubation. This initially suggests the nanoparticles are capable of delivering TMZ to the tumor site. Complete results including drug release profiling, targeting studies, and IC50 analysis will be presented.

Co-encapsulation of TMZ and Cy5 in EGFR targeted biodegradable nanoparticles for improved TMZ efficacy and glioblastoma theranostics

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.