title: Effects of lipid formulations on clove extract spray dried powders: comparison of physicochemical properties, storage stability and in vitro intestinal permeation.
abstract: Clove is an aromatic plant spice with potent antioxidant and anti-inflammatory activity. Eugenol is the main compound which contributes to such medicinal and nutritional benefits. To date, the formulation of unstable, volatile and poorly water-soluble compounds remains a challenging task. Lipid formulations can be used to improve physicochemical and biopharmaceutical properties of poorly soluble compounds. The aim of this study is to investigate the effects of lipids, such as Gelucire and Compritol on physicochemical properties; stability and in vitro intestinal permeation of spray dried powdered formulations loaded with clove's bioactive compounds. Results showed that eugenol retention in spray-dried powders could be correlated with antioxidant activity and with mass recovery after spray drying. Adding Gelucire but not Compritol to clove extract formulations, improved solubility of spray dried powders. Stability test in high humidity environment (63.5% RH) suggested that formulations including both Gelucire and Compritol were significantly more stable compared to the formulation without any lipid at the two tested temperatures (25 °C and 40 °C). This suggests that lipid additions to clove (Syzygium aromaticum) extract formulations provide protective effects for the spray dried powders in high-humidity environments. In addition, results from in vitro intestinal permeation studies suggested that eugenol uptake, was not being hindered by transporters nor was the absorption being affected by lipid formulations.
authors.affiliation: a Faculdade de Ciências Farmacêuticas de Ribeirão Preto , Universidade de São Paulo , Ribeirão Preto , Brazil.
authors.forename: Diego F
authors.identifier: http://orcid.org/0000-0002-5618-6284
authors.initials: DF
authors.lastname: Cortes-Rojas
authors.affiliation: a Faculdade de Ciências Farmacêuticas de Ribeirão Preto , Universidade de São Paulo , Ribeirão Preto , Brazil.
authors.forename: Claudia R F
authors.identifier: http://orcid.org/0000-0002-4152-8640
authors.initials: CRF
authors.lastname: Souza
authors.affiliation: b Department of Pharmaceutics , College of Pharmacy, University of Florida , Gainesville , FL , USA.
authors.forename: Mong-Jen
authors.identifier: http://orcid.org/0000-0002-7900-9395
authors.initials: MJ
authors.lastname: Chen
authors.affiliation: b Department of Pharmaceutics , College of Pharmacy, University of Florida , Gainesville , FL , USA.
authors.forename: Guenther
authors.identifier: http://orcid.org/0000-0002-7406-5558
authors.initials: G
authors.lastname: Hochhaus
authors.affiliation: a Faculdade de Ciências Farmacêuticas de Ribeirão Preto , Universidade de São Paulo , Ribeirão Preto , Brazil.
authors.forename: Wanderley P
authors.identifier: http://orcid.org/0000-0003-4356-2508
authors.initials: WP
authors.lastname: Oliveira
mesh_terms: D018938:Caco-2 Cells; D055598:Chemical Phenomena / Q000187:drug effects; D004339:Drug Compounding / Q000379:methods; D004355:Drug Stability; D004356:Drug Storage / Q000592:standards; D005079:Excipients / Q000737:chemistry / Q000493:pharmacokinetics; D005223:Fats / Q000737:chemistry* / Q000493:pharmacokinetics*; D065569:Gastrointestinal Absorption / Q000187:drug effects*; D006801:Humans; D009821:Oils / Q000737:chemistry* / Q000493:pharmacokinetics*; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000737:chemistry* / Q000302:isolation & purification / Q000493:pharmacokinetics*; D011208:Powders; D027842:Syzygium
chemical_list: D005079:Excipients; D005223:Fats; D009821:Oils; D010936:Plant Extracts; D011208:Powders; C071184:Gelucire 50-13
keywords: Eugenia caryophyllata; in vitro intestinal permeation; lipid systems; product stability; spray drying