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 is 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 PXRD 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, 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.
Highlights
Ciprofibrate (CIP), chemical formula C13H14Cl2O3, is classified as a synthetic active pharmaceutical ingredient (API), which belongs to the fibrate class of drugs, generally used against dyslipidemia, a condition characterized by abnormal lipid levels in the blood system [1]
It was possible to characterize CIP’s crystal structure through this study, which has never been reported in the specific literature before
It crystallizes in a monoclinic crystal system in its solid-state, a pattern maintained due to strong H bonds between the –OH terminations of the molecules
Summary
Ciprofibrate (CIP), chemical formula C13H14Cl2O3, is classified as a synthetic active pharmaceutical ingredient (API), which belongs to the fibrate class of drugs, generally used against dyslipidemia, a condition characterized by abnormal lipid levels in the blood system [1]. Dyslipidemia is a risk factor for developing cardiac diseases such as atherosclerosis, an inflammation characterized by the formation of fat, calcium, and other elements’ plates in the walls of the heart’s arteries and vascular system in general. Designated by the Biopharmaceutics Classification System (BCS) as a class II drug, CIP presents low solubility and high permeability [6]. The high permeability allows a complete absorption of the drug by the small intestine; otherwise, its poor solubility limits its application to treatments. One possible way to overcome this problem is the use of micro- or nanostructures for improved drug delivery
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