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...

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

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Publication - Abstract

December 16, 2020

pharmaceutics

Applying Microfluidics for the Production of the Cationic Liposome-Based Vaccine Adjuvant CAF09b

S.T. Schmidt, D. Christensen and Y. Perrie

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Publication - Abstract

December 16, 2020

Advanced Therapeutics

Quantification of Cellular Drug Biodistribution Addresses Challenges in Evaluating In Vitro and In Vivo Encaps...

C.B. Rodell, P. Baldwin, B. Fernandez, R. Weissleder, S. Sridhar and J.M. Dubach

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Publication - Abstract

December 10, 2020

Journal of Orthopaedic Research

Diflunisal‐loaded Poly(propylene sulfide) Nanoparticles Decrease S. aureus‐mediated Bone Destruction During Os...

C.A. Ford, T.J. Spoonmore, M.K. Gupta, C.L. Duvall, S.A. Guelcher and J.E. Cassat

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Publication - Abstract

November 20, 2020

nanomaterials

Biomimetic Nanoparticles Potentiate the Anti-Inflammatory Properties of Dexamethasone and Reduce the Cytokine ...

R. Molinaro, A. Pasto, F. Taraballi, F. Giordano, J.A. Azzi, E. Tasciotti and C. Corbo

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Publication - Abstract

August 30, 2020

International Journal of Pharmaceutics

Rapid Scale-up and Production of Active-loaded PEGylated Liposomes

C.B. Roces, E.C. Port, N.N. Daskalakis, J.A. Watts, J.W. Aylott, G.W. Halbert and Y. Perri...

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