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Ciprofibrate-loaded nanoparticles prepared by nanoprecipitation: Synthesis, characterization, and drug release

DOI: 10.3390/polym13183158 DOI Help

Authors: Raissa Lohanna Gomes Quintino Corrêa (Federal University of ABC (UFABC)) , Renan Dos Santos (Federal University of ABC (UFABC)) , Lindomar José Calumby Albuquerque (Federal University of ABC (UFABC); Brazilian Synchrotron Light Laboratory (LNLS)) , Gabriel Lima Barros De Araujo (University of Sao Paulo) , Charlotte Jennifer Edwards-Gayle (Diamond Light Source) , Fabio Furlan Ferreira (Federal University of ABC (UFABC)) , Fanny Nascimento Costa (Federal University of ABC (UFABC); Diamond Light Source)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Polymers , VOL 13

State: Published (Approved)
Published: September 2021
Diamond Proposal Number(s): 26698

Open Access Open Access

Abstract: Ciprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties lacking. In parallel, recent studies have led to the improvement of drug administration, including encapsulation in polymeric nanoparticles (NPs). Here, we present CIP’s crystal structure determined by PDRX data. We also propose an encapsulation method for CIP in micelles produced from Pluronic P123/F127 and PEO-b-PCL, aiming to improve its solubility, hydrophilicity, and delivery. We determined the NPs’ physicochemical properties by DLS, SLS, ELS, and SAXS and the loaded drug amount by UV-Vis spectroscopy. Micelles showed sizes around 10–20 nm for Pluronic and 35–45 nm for the PEO-b-PCL NPs with slightly negative surface charge and successful CIP loading, especially for the latter; a substantial reduction in ζ-potential may be evidenced. For Pluronic nanoparticles, we scanned different conditions for the CIP loading, and its encapsulation efficiency was reduced while the drug content increased in the nanoprecipitation protocol. We also performed in vitro release experiments; results demonstrate that probe release is driven by Fickian diffusion for the Pluronic NPs and a zero-order model for PEO-b-PCL NPs.

Journal Keywords: ciprofibrate; drug delivery; Rietveld method; crystallography; nanotechnology

Subject Areas: Biology and Bio-materials, Medicine


Instruments: B21-High Throughput SAXS

Added On: 23/09/2021 09:20

Discipline Tags:

Drug Delivery Health & Wellbeing Materials Science Nanoscience/Nanotechnology Polymer Science Life Sciences & Biotech

Technical Tags:

Scattering Small Angle X-ray Scattering (SAXS)