Nanoparticles Based on Linear and Star-Shaped Poly(Ethylene Glycol)-Poly(ε-Caprolactone) Copolymers for the Delivery of Antitubulin Drug

Autor: Mahmoud E. S. Soliman, Giulia Bonacucina, Omaima A. Sammour, Lisbeth Illum, Giovanni Filippo Palmieri, Abdelhameed A. El Shamy, Karim S. Shalaby, Marco Cespi, Luca Casettari
Jazyk: angličtina
Rok vydání: 2016
Předmět:
Drug
Noscapine
Cell Survival
media_common.quotation_subject
Polyesters
Pharmaceutical Science
Nanoparticle
pH dependent release
passive targeting
polyethylene glycol-co-poly(ε-caprolactone) (PEG-co-PCL)
polymeric nanoparticles
02 engineering and technology
Polyethylene Glycols
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Drug Delivery Systems
Cell Line
Tumor

Polymer chemistry
medicine
Copolymer
Animals
Humans
Pharmacology (medical)
Solubility
Particle Size
Rats
Wistar

media_common
Pharmacology
Dose-Response Relationship
Drug

Organic Chemistry
technology
industry
and agriculture

Polyethylene
021001 nanoscience & nanotechnology
Polymeric nanoparticles
Combinatorial chemistry
Rats
chemistry
030220 oncology & carcinogenesis
MCF-7 Cells
Molecular Medicine
Nanoparticles
Female
0210 nano-technology
Caprolactone
Biotechnology
medicine.drug
Popis: Biodegradable polymeric nanoparticles of different architectures based on polyethylene glycol-co-poly(ε-caprolactone) block copolymers have been loaded with noscapine (NOS) to study their effect on its anticancer activity. It was intended to use solubility of NOS in an acidic environment and ability of the nanoparticles to passively target drugs into cancer tissue to modify the NOS pharmacokinetic properties and reduce the requirement for frequent injections.Linear and star-shaped copolymers were synthetized and used to formulate NOS loaded nanoparticles. Cytotoxicity was performed using a sulforhodamine B method on MCF-7 cells, while biocompatibility was determined on rats followed by hematological and histopathological investigations.Formulae with the smallest particle sizes and adequate entrapment efficiency revealed that NOS loaded nanoparticles showed higher extent of release at pH 4.5. Colloidal stability suggested that nanoparticles would be stable in blood when injected into the systemic circulation. Loaded nanoparticles had IC50 values lower than free drug. Hematological and histopathological studies showed no difference between treated and control groups. Pharmacokinetic analysis revealed that formulation P1 had a prolonged half-life and better bioavailability compared to drug solution.Formulation of NOS into biodegradable polymeric nanoparticles has increased its efficacy and residence on cancer cells while passively avoiding normal body tissues. Graphical Abstract ᅟ.
Databáze: OpenAIRE