title: Triblock polymeric micelles as carriers for anti-inflammatory drug delivery.
abstract: This study evaluated the properties of poly(ethylene oxide)-b-poly(n-butyl acrylate)-b-poly(acrylic acid) (PEO-PnBA-PAA) polymeric micelles as carriers for anti-inflammatory drugs (prednisolone and budesonide). The micelles comprising a hydrophobic PnBA core and a PEO/PAA corona showed average diameter less than 40 nm. The size of the drug-loaded micelles did not change during eight hours into media that mimic physiological fluids indicating high colloidal stability. The calculation of Flory-Huggins parameter showed greater compatibility between budesonide and micellar core suggesting its location in the micellar core, whereas prednisolone was located also into the interface layer. This observation correlated further with slower release of budesonide, especially in acid medium (pH = 1.2). The inclusion of budesonide into micelles showed significant protective effect against the cytotoxic damage induced by the co-cultivation of differentiated human EOL-1 and HT-29 cells. This study revealed the capacity of PEO-PnBA-PAA terpolymer as carrier of nanosized micelles suitable for oral delivery of anti-inflammatory drugs.
authors.affiliation: Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Medical University of Sofia , Sofia , Bulgaria .
authors.forename: Krassimira
authors.initials: K
authors.lastname: Yoncheva
authors.forename: Petar
authors.initials: P
authors.lastname: Petrov
authors.forename: Ivanka
authors.initials: I
authors.lastname: Pencheva
authors.forename: Spiro
authors.initials: S
authors.lastname: Konstantinov
mesh_terms: D000179:Acrylates / Q000737:chemistry*; D000180:Acrylic Resins / Q000737:chemistry*; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage*; D019819:Budesonide / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002460:Cell Line; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D006801:Humans; D008823:Micelles; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D011239:Prednisolone / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D000179:Acrylates; D000180:Acrylic Resins; D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; C498324:poly(n-butyl acrylate); D011092:Polyethylene Glycols; C006903:carbopol 940; D019819:Budesonide; D011239:Prednisolone
keywords: Cytoprotective effect; micellar stability; poly(acrylic acid); poly(ethylene oxide); poly(n-butyl acrylate); polymeric micelles