title: Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon-specific delivery.
abstract: The primary objective of the study was to develop a pH and transit time controlled sigmoidal release polymeric matrix for colon-specific delivery of indomethacin. Tablet matrices were prepared using a combination of hydrophilic polymers (polycarbophil or carbopol) having pH-sensitive swelling properties with hydrophobic polymer ethyl cellulose. The prepared matrices were characterized for physical properties and in vitro release kinetics. The presence of ethyl cellulose in a hydrophilic polymer matrix resulted in a sigmoidal in vitro drug release pattern with negligible-to-very low drug release in the initial phase (0-6 h) followed by controlled release for 14-16 h. The retardation in initial release can be attributed to the presence of ethyl cellulose that reduced swelling of hydrophilic polymer(s), while in the later portion, polymer relaxation at alkaline pH due to the ionization of acrylic acid units on carbopol and polycarbophil resulted in enhanced drug release. Thus, a sigmoidal release pattern was obtained that could be ideal for colonic delivery of indomethacin in the potential treatment of colon cancer.
authors.affiliation: Formulation Development & Pharmacokinetics Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani, India.
authors.forename: Laila Fatima
authors.initials: LF
authors.lastname: Ali Asghar
authors.forename: Md
authors.initials: M
authors.lastname: Azeemuddin
authors.forename: Varun
authors.initials: V
authors.lastname: Jain
authors.forename: Sajeev
authors.initials: S
authors.lastname: Chandran
mesh_terms: D002626:Chemistry, Pharmaceutical; D003106:Colon / Q000187:drug effects / Q000378:metabolism; D012809:Colon, Sigmoid / Q000187:drug effects / Q000378:metabolism; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005772:Gastrointestinal Transit / Q000187:drug effects / Q000502:physiology; D006863:Hydrogen-Ion Concentration; D007213:Indomethacin / Q000008:administration & dosage / Q000378:metabolism
chemical_list: D003692:Delayed-Action Preparations; D007213:Indomethacin