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Formulation of Diblock Polymeric Nanoparticles through Nanoprecipitation Technique

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Precise engineering of targeted nanoparticles by using self-assembled biointegrated block copolymers.

Frank Gu¹, Liangfang Zhang, Benjamin A Teply

¹Department of Chemical Engineering, Harvard-MIT Center of Cancer Nanotechnology Excellence, Massachusetts Institute of Technology, 77 Massachusetts Avenue, Cambridge, MA 02139, USA.

Proceedings of the National Academy of Sciences of the United States of America

|February 15, 2008

Summary

Researchers developed targeted nanoparticles (NPs) for prostate cancer (PCa) therapy by precisely controlling their properties. This strategy enables reproducible formulation for enhanced drug delivery and treatment efficacy.

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Published on: August 11, 2018

Area of Science:

Biotechnology
Materials Science
Nanomedicine

Background:

Targeted nanoparticles (NPs) show promise for drug delivery but reproducible formulation with optimal properties remains a challenge.
Achieving molecular targeting, immune evasion, and controlled drug release simultaneously is crucial for *in vivo* efficacy.

Purpose of the Study:

To develop a reproducible strategy for formulating targeted NPs with tunable biophysicochemical properties.
To systematically screen optimally formulated drug-encapsulated NPs for enhanced prostate cancer (PCa) therapy.

Main Methods:

Formulation of NPs via self-assembly of amphiphilic triblock copolymers (PLGA-PEG-Aptamer).
Tuning NP size and drug release by controlling copolymer composition.
Varying ratios of triblock copolymer with diblock copolymer to modulate aptamer density and PEG exposure.

Main Results:

Developed a series of targeted NPs with controlled aptamer densities and PEG exposure.
Identified a narrow range of aptamer density for maximal targeting and immune evasion.
Demonstrated most efficient PCa cell uptake *in vitro* and *in vivo* within this optimal range.

Conclusions:

The reported strategy enables reproducible formulation of targeted NPs with fine-tuned properties.
This approach facilitates systematic screening for optimal NP design in nanomedicine.
Contributes to the development of highly selective and effective targeted NP therapeutics for PCa.