Encapsulation of Anticancer Drugs (5-Fluorouracil and Paclitaxel) into Polycaprolactone (PCL) Nanofibers and In Vitro Testing for Sustained and Targeted Therapy

Abstract

We report a continuous nanoscale encapsulation of cancer drugs 5-Fluorouracil (FU) and Paclitaxel into biocompatible polycaprolactone (PCL) nanofibers (NFs) using core-sheath electrospinning process. A high potential electric field of 19–23.2 kV was used to draw a compound solution jet from a specialized coaxial spinneret. Using of DMF in both core and Sheath resulted in NFs within 50–160 nm along with large beaded structures. Addition of Trichloromethane (TCM) or Trifluoroethanol (TFE) in sheath turned NFs in more uniform and thin fiber structure. The diameter range for paclitaxel encapsulated fibers was 22–90 nm with encapsulation efficiency of 77.5% and the amount of drug was only 4 to 5% of sheath polymer. Addition of PVA within core resulted drug nanocrystal formation outside of sheath and poor encapsulation efficiency (52%) with rapid initial release (52–53%) in first 3 days. Drug release test of NFs in different pH exhibited increase of release rate with the decrease of media pH. In-vitro cell viability test with FU encapsulated NFs in human prostatic cancer PC3 cells exhibited 38% alive cells at 5 μM concentration while in pristine FU 43% cells were alive. Paclitaxel encapsulated NFs with breast cancer cells also exhibited increased efficacy in comparison to pristine anticancer drugs. Continuous decrease of cell density indicated the slow release of cancer drugs from the NFs. Both PCL+Paclitaxel and PCL+5FU treated conditions caused breast cancer cell death between 40% to 50%.

Bioimaging of Intact Polycaprolactone Nanoparticles Using Aggregation‐Caused Quenching Probes: Size‐Dependent Translocation via Oral Delivery

“…Polycaprolactone (PCL) is a biocompatible and biodegradable polymer frequently used for the preparation of nanoparticles . PCL degradation is slower than poly(lactic‐co‐glycolic acid) (PLGA), making it more appropriate for delivery of biologics.…”

Polycaprolactone as Drug Carrier for an Antifungal Agent

“…This is shown in particular for formulations with lower % DL. The initial burst could be due to the dissolution of drug molecules that are present at the surface of microspheres 14,19 .…”

Superior antitumor effect of self-assembly supramolecular paclitaxel nanoparticles

“…Compared with polymeric nanosphere systems, these compositions could self-assemble into nanoparticles with drugs themselves as carriers (also referred to as "carrier-free"), which have higher drug loading efficiency and offer more stable drug release. 20,21 Previous studies have demonstrated that Ptx is a widely used model drug to achieve the "carrier-free" goal. 19,[22][23][24] As our previous study reported, Ptx loaded nanoparticles can be designed by the conjugation of Ptx and a small molecule compound, succinic acid (SA), with a very high drug loading content (90%).…”