Production of polycaprolactone nanoparticles with hydrodynamic diameters below 100 nm

Abstract

Cancer is a worldwide increasing burden and its therapy is often challenging and causes severe side effects in healthy tissue. If drugs are loaded into nanoparticles, side effects can be reduced, and efficiency can be increased via the enhanced permeability and retention effect. This effect is based on the fact that nanoparticles with sizes from 10 to 200 nm can accumulate in tumor tissue due to their leaky vasculature. In this work, we produced polycaprolactone (PCL) in the sizes 1.8, 5.4, and 13.6 kDa and were able to produce spherical shaped nanoparticles with mean diameters of 64 ± 19 nm out of the PCL5.4 and 45 ± 8 nm out of the PCL13.6 reproducibly. By encapsulation of paclitaxel the diameter of that nanoparticles did not increase, and we were able to encapsulate 73 ± 7 fmol paclitaxel per 1000 particles in the PCL5.4‐nanoparticles and 35 ± 8 fmol PTX per 1000 PCL13.6‐nanoparticles. Furthermore, we coupled the aptamer S15 to preformed PCL5.4‐nanoparticles resulting in particles with a hydrodynamic diameter of 153 nm. This offers the opportunity to use these nanoparticles for targeted drug delivery.

Poly(caprolactone)-Based Coatings on 3D-Printed Biodegradable Implants: A Novel Strategy to Prolong Delivery of Hydrophilic Drugs

“… 12 , 40 The main applications of this type of polymer have been the preparation of nanoparticles for drug delivery or its use as scaffold for tissue regeneration. 37 , 38 PCL has previously been used as a rate-controlling membrane. 13 However, we propose a novel approach where the properties of the membrane, including its drug permeation, will be tailored by adjusting the coating composition.…”

Biodegradable Polymeric Nanoparticles for Drug Delivery to Solid Tumors

“…Among polylactone-based polymers, poly(Ɛ-caprolactone) (PCL) is the most studied polymer for anticancer drug development. It is a semicrystalline compound obtained by the ring-opening polymerization of ε-caprolactone ( Witt et al, 2019 ). PCL exhibits slower ester bond hydrolysis at physiological pH and has a less acidic character than poly-hydroxy acids; in addition, the slower degradation rate of PCL prolongs the release of encapsulated drugs ( Doppalapudi et al, 2016 ).…”

Polymeric Nanoparticles for Nasal Drug Delivery to the Brain: Relevance to Alzheimer's Disease

“…PEGylated PCL-NPs play an important role in improving biodistribution and their penetration into the brain. [229] In this study, the size of the synthesized NPs was about 100 nm. Cur alone was able to be transported via the olfactory bulb, but the intact NPs were not.…”