Abstract
Rutin is a flavone glycoside contained in many plants, and exhibits antioxidant, anti-inflammatory, anticancer, and wound-healing properties. The main disadvantage related to the use of this molecule for pharmaceutical application is its poor bioavailability, due to its low solubility in aqueous media. Poloxamer 407-hydrogels show interesting thermo-sensitive properties that make them attractive candidates as pharmaceutical formulations. The hydrophobic domains in the chemical structure of the copolymer, a polymer made up of two or more monomer species, are useful for retaining poorly water-soluble compounds. In this investigation various poloxamer 407-based hydrogels containing rutin were developed and characterized as a function of the drug concentration. In detail, the Turbiscan stability index, the micro- and dynamic rheological profiles and in vitro drug release were investigated and discussed. Rutin (either as a free powder or solubilized in ethanol) did not modify the stability or the rheological properties of these poloxamer 407-based hydrogels. The drug leakage was constant and prolonged for up to 72 h. The formulations described are expected to represent suitable systems for the in situ application of the bioactive as a consequence of their peculiar versatility.
Highlights
Hydrogels are a peculiar class of drug-delivery systems characterized by a natural or semi-synthetic three-dimensional polymeric network [1]
The microrheology of rutin-loaded poloxamer 407 (P407) hydrogels was measured using a Rheolaser® Master (Formulaction, Toulouse, France) the technology of which is based on multi-speckle diffusing wave spectroscopy (MS-DWS)
The samples were analyzed at λmax 362 nm of rutin by a PerkinElmer Lambda 35 ultraviolet–visible (UV–vis) spectrophotometer equipped with PerkinElmer acquisition software (Perkin-Elmer GmbH Uberlingen, Germany)
Summary
Hydrogels are a peculiar class of drug-delivery systems characterized by a natural or semi-synthetic three-dimensional polymeric network [1]. In order to overcome this shortcoming, various strategies were adopted such as the nanoencapsulation of drugs within biocompatible delivery systems, the physico-chemical modification of the polymer and the use of organic solvents [9,10,11] The integration of both organic and inorganic materials into the network of hydrogels is typically performed in order to improve their properties and functionalities, obtaining the so-called “hybrid materials” [12,13,14]. The solubilization of hydrophobic compounds in the micelle POP core is energetically favorable and does not require any energy input [11] The purpose of this investigation was to evaluate the influence of rutin on the stability and rheological features of P407-based hydrogels in order to obtain suiTable Systems for the in situ administration of the active compound. TThheeiinnfflluueenncceeooffvvaarriioouuss ccoonncceennttrraattiioonnss ooffrurutitnin(as(aaspaowpdoewr dorersoolurbsiloizluedbiilnizeetdhainnole)tohnanthoel)pohnysitchoe-chpehmysicicaol -acnhdemrhiecoallogaincdal rfheeaotulorgeiscaolffePa4t0u7r-ebsaosfedP4h0y7-dbraosgeedlshywdarsoginevlsewstiagsaitnevde.stIingadteedta. iIln, dtheetaTilu, rthbeisTcaunrbsitsacbanilisttyabinilditeyxin(TdSeIx), (tThSeI)m, itchreo-manicdrod-ynanamd idc yrhneaomloicgicrhalepolroogfiilceasl, apnrdoftihleesi,navnidtrothderuign rveilteraosedprruogfilreeslewaesree pevroafliuleastedwaenred edviaslcuuastseedda(nFdigduirsec1u)s.sed (Figure 1)
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