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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.

 

 

Lipid nanoparticle image
Liposomes
Lipid nanoparticle image
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.

sm_mol - 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 affects 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. 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.



sm_mol - Rapid formulation developmentSimultaneous drug loading and liposome formation was 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.



sm-mol - ScalableLiposome formulations were optimized on the Benchtop and scaled up on the Blaze using a single microfluidic mixer and on the 8x Scale-Up 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

Application Note

July 01, 2018

Seamless scale up of liposomal verteporfin formulations using the NanoAssemblr™ Platform

Read More PDF

Publication - Abstract

April 26, 2018

Small Methods

State‐of‐the‐Art Design and Rapid‐Mixing Production Techniques of Lipid Nanoparticles for Nucleic Acid Delivery

Evers, M. J. W., Kulkarni, J. A., van der Meel, R., Cullis, P. R., Vader, P., & Schiffelers, R. M.

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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

Read More PDF

Publication - Abstract

July 04, 2018

Nature communications

Rapid transport of deformation-tuned nanoparticles across biological hydrogels and cellular barriers

M Yu, L Xu, F Tian, Q Su, N Zheng, Y Yang

Read More

Publication - Abstract

June 01, 2018

Biological and Pharmaceutical Bulletin

The Use of an Efficient Microfluidic Mixing System for Generating Stabilized Polymeric Nanoparticles for Controlled Drug Release

Y Morikawa, T Tagami, A Hoshikawa, T Ozeki

Read More

Publication - Abstract

May 25, 2018

Multiple Myeloma

Microfluidic Assembly of Liposomes with Tunable Size and Coloading Capabilities

JR Hoffman, E Tasciotti, R Molinaro

Read More
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