Liquids in Dishes in a Lab
Small Molecules

Small molecules make up the majority of current pharmaceuticals and are used to treat and manage symptoms of cancer, infections, and depression, among others.

 

Applications of nanomedicine for small molecule drugs include:

• Drug targeting
• Controlled release
• Improving solubility
• Combination therapy

     


Small molecule drugs can be formulated into numerous nanoparticle materials. On the market, there are several liposomal formulations of small molecules including Doxil and Visudyne.

 

 

Liposome
Liposomes
Polymeric Nanoparticle and Micelles
Polymer NPs and Micelles
Emulsion

Emulsions

There are however some challenges to producing small molecule-loaded nanoparticles that can be addressed with NanoAssemblr® technology.

Overcome Key Challenges in Making Drug Delivery Nanoparticles


Challenges with 
Conventional Methods
 Benefits of NanoAssemblr® Technology
Formulation affected by production conditionsorangeRightArrowPrecisely controlled formulation conditions
Production is complex and time-consumingorangeRightArrowRapid formulation development
Difficult to scale-up productionorangeRightArrowInherently scalable
Different formulations require different process and equipmentorangeRightArrowProduce a variety of formulations

Key Benefits



Precisely Controlled Formulation Conditions


Laminar flow microfluidic conditions with computer-controlled fluid flow allow conditions of particle precipitation to be precisely controlled.

 

Precisely Controlled ConditionsPEG-b-PLGA block copolymer micelles of identical size were produced on the NanoAssemblr® Benchtop from polymers of different PLGA block lengths. Typically changing block lengths affect particle size, making it difficult to compare the drug delivery performance of these materials.

 

With conventional methods, it is difficult to adjust the formulation conditions to produce uniform sizes with different polymers. By contrast, with NanoAssemblr® technology Total Flow Rate (TFR) was adjusted in software to equalize the size of these formulations. The size was determined by DLS of triplicate formulations.



Rapid Formulation Development


Drug loading and particle formation can be performed simultaneously in one step at flow rates typically greater than 10 mL/min. All NanoAssemblr® instruments are intuitive to use requiring no prior experience with microfluidics.

 

Rapid Formulation DevelopmentSimultaneous drug loading and liposome formation were performed for 4 liposome formulations at a Total Flow Rate of 12 ml/min using a model hydrophobic small molecule drug verteporfin. This enabled rapid identification and optimization of lead formulations.

 

 

 

 



Inherently Scalable


The NanoAssemblr® process is continuous and can be scaled by flowing more volume through the system, or by using multiple microfluidic mixers in parallel.

Small Molecule: ScaleableLiposome formulations were optimized on the Benchtop and scaled up on the Blaze using a single microfluidic mixer and on the GMP System employing 8 mixers in parallel with identical results. Size and PDI were measured by DLS of triplicate formulations.


Produce a Variety of Formulations


Over 100 papers have demonstrated production of liposomes, polymer NPs, block-co-polymer micelles, emulsions, and lipid nanoparticles.




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To learn how Precision NanoSystems accelerates nanomedicine development from an idea to clinical applications, contact our Technical Sales Team.

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Small Molecule Resources

Publication - Summary

February 07, 2019

Nano Research

Chemotherapy drugs derived nanoparticles encapsulating mRNA encoding tumor suppressor proteins to treat triple-negative breast can...

C. Zhang, X. Zhang, W. Zhao, C. Zeng, W. Li, B. Li, X. Luo, J. Li, J. Jiang, B. Deng, D.W. McComb, Y. Dong

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Publication - Abstract

February 27, 2019

Cell Chemical Biology

Imidazole Ketone Erastin Induces Ferroptosis and Slows Tumor Growth in a Mouse Lymphoma Model

Y. Zhang, H. Tan, J.D. Daniels, F. Zandkarimi, H. Liu, L.M. Borwn, K. Uchida, O.A. O'Connor. B.R. Stockwell

Read More

Publication - Summary

January 14, 2019

Cancer Immunology, Immunotherapy

STAT3 inhibition specifically in human monocytes and macrophages by CD163-targeted corosolic acid-containing liposomes

MN Andersen, A Etzerodt, JH Graversen, LC Holthof, SK Moestrup, M Hokland, HJ Møller

Read More

Publication - Abstract

December 09, 2018

Pharmaceutics

The Microfluidic Technique and the Manufacturing of Polysaccharide Nanoparticles

E. Chiesa, R. Dorati, S. Pisani, B. Conti, G. Bergamini, T. Modena and I. Genta

Read More

Publication - Abstract

October 10, 2018

Drug Delivery and Translational Research

Rapid optimization of liposome characteristics using a combined microfluidics and design-of-experiment approach

M. Sedighi, S. Sieber, F. Rahimi, M.A. Shahbazi, A.H. Rezayan, J. Huwyler, D. Witzigmann

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Poster

August 01, 2018

Microfluidics-based Manufacture of PEG-b-PLGA Block Copolymer Nanoparticles for the Delivery of Small Molecule Therapeutics

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