Preparation of 5‐Fluorouracil‐Poly(L‐lactide) Microparticles Using Solution‐Enhanced Dispersion by Supercritical CO₂

Abstract

Summary: 5‐Fluorouracil‐poly(L‐lactide) (5‐Fu‐PLLA) microparticles have been prepared by an SEDS process. First, the 5‐Fu is successfully micronized and is then used to produce the 5‐Fu‐PLLA microparticles. The 5‐Fu‐PLLA microparticles synthesized by the SEDS process exhibit a rather spherical shape and a narrow particle size distribution, where it ranges from 615 to 1 990 nm, with a mean particle size of 980 nm. The dichloromethane residue in the 5‐Fu‐PLLA microparticles without any further treatment is 46 ppm. The average drug load and encapsulation efficiency of the 5‐Fu‐PLLA microparticles are 3.05 and 17.8%, respectively. The rate of drug release from the 5‐Fu‐PLLA microparticles shows mainly first‐order kinetics.Scanning electron spectroscopy image of 5‐Fu‐PLLA microparticles.magnified imageScanning electron spectroscopy image of 5‐Fu‐PLLA microparticles.

Fabrication of hydrophilic paclitaxel-loaded PLA-PEG-PLA microparticles via SEDS process

“…The research groups of Ghaderi, Lee, and Rantakyla, had reported their findings on the preparation of PLA and copolymer microparticles via SAS process separately [13,22,25]. In our previous studies [36,37], we had succeeded in micronizing PLLA with various molecular weight using different processing conditions, and loading 5-Fluorouracil into PLLA microparticles, via SEDS process. However, to our knowledge, few researchers reported that paclitaxel was encapsulated into PLA-PEG-PLA triblock copolymer microparticles by scCO 2 technique in the SEDS process.…”

Self-assembled silk fibroin nanoparticles loaded with binary drugs in the treatment of breast carcinoma

“…25,26 Curcumin is widely used as an anticancer agent in preclinical and clinical trials, probably due to their capability of generating intracellular ROS. However, this drug is poorly soluble in water, which restricts it from being directly used in aqueous solutions.…”

“…24 5-Fluorouracil (5-FU) is another highly efficient chemotherapeutic agent that inhibits the methylation reaction of deoxyuridylic acid to thymidylic acid. 25,26 This chemical drug can cause intense thymine deficit in the cells by interfering with the synthesis of deoxyribonucleic acid and ribonucleic acid, which eventually results in an imbalanced growth and death of cancer cells. To increase their water solubility and biocompatibility, several drug carriers are developed based on nanotechnology, 27 ranging from liposome, 28 proteins, 29 saccharides, 30 phospholipids, 31 to inorganic silica particles 32,33 and polymeric organic nanoparticles.…”

Preparation of Emodin‐Polyethylene Glycol Composite Microparticles Using a Supercritical Antisolvent Process

“…Solution-enhanced dispersion by supercritical fluids (SEDS) is one of the SFP processes that have attracted high attention in producing high-quality drug composite microparticles. Some successful examples include: composite crystals of acetaminophen and p-acetoxyacetanilide [6], budesonide-b-cyclodextrin complexes [7], microencapsulation of amoxicillin in poly(L-lactic acid) [8], 5-fluorouracil-poly-(L-lactide) microparticles [9], budesonide-c-cyclodextrin complexes [10], etc. In our previous works, the SEDS-prefilming atomization (PA) process has been also successfully applied to deposit the composite microparticles of polyethylene glycol (PEG) loaded with natural carotene [2] and caroteneproanthocyanidin composite microparticles [11].…”