title: Propolis as lipid bioactive nano-carrier for topical nasal drug delivery.
abstract: Propolis shows therapeutic properties ascribed to the presence of some flavonoids, phenolic acids, and their esters; it is a natural multifunctional material, solid at room temperature, and composed mainly of resin and waxes. We therefore used propolis as a lipid material to prepare solid lipid nanoparticles (SLNs); SLNs are proposed bioactive medications for topical intranasal therapy. Suitable formulation parameters were studied and the SLNs obtained by the high shear homogenization method were characterized; a selected formulation was viscosized to increase the residence time. Dimensional, morphological, and solid-state characterizations of the formulated SLNs were performed. In vitro and ex vivo permeation tests of diclofenac sodium, the model drug, and polyphenols were carried out. The propolis amount and surfactant concentration represent the key parameters that affect nanoparticle properties in terms of size, drug and polyphenol content, and physical stability. Size dispersions of about 600 nm and 0.4 PI were obtained, which do not change by increasing the viscosity. Drug is encapsulated in SLNs, as demonstrated by FTIR and DSC analyses. In vitro and ex vivo studies prove that drug and polyphenols do not cross the membranes; therefore, propolis-based SLNs could be used as delivery systems of diclofenac and flavonoids for the local treatment of nasal cavity diseases. Due to propolis composition, the proposed formulation could be used as a bioactive medication in which the carrier can exert a complementary effect with the loaded drug.
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy. Electronic address: grassu@uniss.it.
authors.forename: Giovanna
authors.initials: G
authors.lastname: Rassu
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy. Electronic address: m.cossu@uniss.it.
authors.forename: Massimo
authors.initials: M
authors.lastname: Cossu
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy. Electronic address: rita.langasco@hotmail.it.
authors.forename: Rita
authors.initials: R
authors.lastname: Langasco
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy. Electronic address: acarta@uniss.it.
authors.forename: Antonio
authors.initials: A
authors.lastname: Carta
authors.affiliation: Department of Science and Technology of Pharmaceutics, University of Torino, 10125 Torino, Italy. Electronic address: roberta.cavalli@unito.it.
authors.forename: Roberta
authors.initials: R
authors.lastname: Cavalli
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy. Electronic address: pgiunc@uniss.it.
authors.forename: Paolo
authors.initials: P
authors.lastname: Giunchedi
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy. Electronic address: eligav@uniss.it.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Gavini
mesh_terms: D000281:Administration, Intranasal; D016503:Drug Delivery Systems; D008055:Lipids / Q000737:chemistry*; D036103:Nanotechnology; D011429:Propolis; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D008055:Lipids; D011429:Propolis
keywords: Bioactive medication; Intranasal delivery; Local therapy; Propolis; Solid lipid nanoparticles