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Preparation of biocompatible copolymeric micelles as a carrier of atorvastatin and rosuvastatin for potential anticancer activity study
- Source :
- Pharmaceutical development and technology. 24(3)
- Publication Year :
- 2018
-
Abstract
- Statins are widely used for the treatment of hypercholesterolemia. However, their inhibitory action on HMG-CoA reductase also results in the depletion of intermediate biosynthetic products, which importantly contribute to cell proliferation. The aim of the present study was to compare the effects of the individual commercially available statins on investigational breast cancer. Thus, in this study, biodegradable polymeric micelles as carrier of statins were prepared using biodegradable copolymers (PCL-PEG-PCL). These nanoparticles were prepared with two statins (atorvastatin and rosuvastatin) and drug loading, release, kinetic release, and anti-cancer activity of these drugs were studied. The triblock copolymer PCL-PEG-PCL was synthesized by a ring opening polymerization of e-caprolactone in the presence of PEG as the initiator and Sn(oct)2 as the catalyst. The synthesized copolymers and nanoparticles were characterized by FTIR, HNMR, GPC, DLS, and AFM analyses. The drug loading and release of drugs were studied by UV-Vis. Additionally, MTT assays on HFF-2 cell lines were performed for determination of biocompatibility of micelles. Finally, the anticancer activity of micelles was studied on MCF-7 breast cancer cell lines. The results showed that the average diameter of nanoparticles was less than 45 nm. The loading capacity of atorvastatin and rosuvastatin was 20.0 ± 1.01% and 13.21 ± 1.18%, respectively, and encapsulation efficiency of atorvastatin and rosuvastatin was 88.19 ± 1.11% and 69.32 ± 0.23%, respectively. The results showed strong and dose-dependent inhibition of cell (MCF-7line) growth by the nanoparticles compared with statins. The result of cell viability assay on the MCF-7 cell line verified that the bare nanoparticles showed little inherent cytotoxicity whereas the statins-loaded nanoparticles were cytotoxic.
- Subjects :
- Cell Survival
Polymers
Atorvastatin
Chemistry, Pharmaceutical
Polyesters
Pharmaceutical Science
Antineoplastic Agents
Breast Neoplasms
macromolecular substances
02 engineering and technology
030226 pharmacology & pharmacy
Micelle
Polyethylene Glycols
03 medical and health sciences
0302 clinical medicine
PEG ratio
medicine
Humans
Rosuvastatin
Viability assay
Particle Size
Rosuvastatin Calcium
Cytotoxicity
Micelles
Drug Carriers
Chemistry
technology, industry, and agriculture
nutritional and metabolic diseases
General Medicine
021001 nanoscience & nanotechnology
Drug Liberation
MCF-7 Cells
Nanoparticles
Female
Hydroxymethylglutaryl-CoA Reductase Inhibitors
0210 nano-technology
Drug carrier
Nuclear chemistry
medicine.drug
Subjects
Details
- ISSN :
- 10979867
- Volume :
- 24
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- Pharmaceutical development and technology
- Accession number :
- edsair.doi.dedup.....d282ea82f0f23a07594d32625c268a44