title: Design and evaluation of acrylate polymeric carriers for fabrication of pH-sensitive microparticles.
abstract: Colon-targeted microparticles loaded with a model anti-inflammatory drug were fabricated using especially designed acrylic acid-butyl methacrylate copolymers. Microparticles were prepared by oil-in-oil solvent evaporation method using Span 80 as emulsifier. Microparticles were found to be spherical in shape, hemocompatible and anionic with zeta potential of -27.4 and -29.0 mV. Entrapment of drug in the microparticles was confirmed by Fourier transform infrared (FTIR) spectroscopy. However, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) revealed amorphous nature of microparticles due to the dilution effect of amorphous polymer. The microparticles released less than 5% drug at pH 1.2, while more than 90% of the drug load was released at pH 7.4. This suggested the colon targeting nature of the formulations. In experimentally developed colitis in Wistar rats, the microparticle formulation showed significant reduction (p < .05) in the disease activity score (disease symptoms), the colon-to-body weight ratio (tissue edema) and the myeloperoxidase, tumor necrosis factor (TNF)-α and interleukin (IL)-1β activities.
authors.affiliation: a Delhi Institute of Pharmaceutical Sciences and Research, (formerly College of Pharmacy) , University of Delhi, Pushp Vihar, Sector III , New Delhi , India.
authors.forename: Amit
authors.initials: A
authors.lastname: Arya
authors.affiliation: a Delhi Institute of Pharmaceutical Sciences and Research, (formerly College of Pharmacy) , University of Delhi, Pushp Vihar, Sector III , New Delhi , India.|b School of Pharmaceutical Sciences , Apeejay Stya University , Sohna , Haryana , India.
authors.forename: Dipak K
authors.initials: DK
authors.lastname: Majumdar
authors.affiliation: a Delhi Institute of Pharmaceutical Sciences and Research, (formerly College of Pharmacy) , University of Delhi, Pushp Vihar, Sector III , New Delhi , India.
authors.forename: Dharam Pal
authors.initials: DP
authors.lastname: Pathak
authors.affiliation: a Delhi Institute of Pharmaceutical Sciences and Research, (formerly College of Pharmacy) , University of Delhi, Pushp Vihar, Sector III , New Delhi , India.
authors.forename: Anil K
authors.initials: AK
authors.lastname: Sharma
authors.affiliation: c Centre for Biomedical Engineering , Indian Institute of Technology , Hauz Khas , New Delhi , India.
authors.forename: Alok R
authors.initials: AR
authors.lastname: Ray
mesh_terms: D000179:Acrylates / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D003106:Colon / Q000187:drug effects* / Q000378:metabolism; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D006863:Hydrogen-Ion Concentration; D008689:Methacrylates / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D000179:Acrylates; D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D008689:Methacrylates; D011108:Polymers; C036658:acrylic acid
keywords: colitis; colonic drug delivery; microparticles; pH-sensitive copolymer; targeted polymers