title: Calcium alginate-carboxymethyl cellulose beads for colon-targeted drug delivery.
abstract: The present study delineates preparation, characterization and application of calcium alginate (CA)-carboxymethyl cellulose (CMC) beads for colon-specific oral drug delivery. Here, we exploited pH responsive swelling, mucoadhesivity and colonic microflora-catered biodegradability of the formulations for colon-specific drug delivery. The CA-CMC beads were prepared by ionic gelation method and its physicochemical characterization was done by SEM, XRD, EDAX, DSC and texture analyzer. The swelling and mucoadhesivity of the beads was found higher at the simulated colonic environment. Variation was more prominent in compositions with lower CMC concentrations. CA-CMC formulations degraded slowly in simulated colonic fluid, however the degradation rate increased drastically in the presence of colonic microflora. In vitro release study of anticancer drug 5-fluorouracil (5-FU) showed a release (>90%) in the presence of colonic enzymes. A critical analysis of drug release profile along with FRAP (fluorescence recovery after photobleaching) study revealed that the presence of CMC in the formulation retarded the release rate of 5-FU. 5-FU-loaded formulations were tested against colon adenocarcinoma cells (HT-29). Cytotoxicity data, nuclear condensation-fragmentation and apoptosis analysis (by flow cytometry) together confirmed the therapeutic potential of the CA-CMC formulations. In conclusion, CA-CMC beads can be used for colon-specific drug delivery.
authors: Department of Biotechnology and Medical Engineering, National Institute of Technology, Rourkela Odisha 769008, India. Electronic address: tarun3agarwal5@gmail.com.
authors: Tarun
authors: T
authors: Agarwal
authors: Department of Biotechnology and Medical Engineering, National Institute of Technology, Rourkela Odisha 769008, India. Electronic address: gotam.jillu66@gmail.com.
authors: S N Gautham Hari
authors: SN
authors: Narayana
authors: Department of Biotechnology and Medical Engineering, National Institute of Technology, Rourkela Odisha 769008, India. Electronic address: pal.kunal@yahoo.com.
authors: Kunal
authors: K
authors: Pal
authors: Department of Biotechnology and Medical Engineering, National Institute of Technology, Rourkela Odisha 769008, India. Electronic address: kpr@nitrkl.ac.in.
authors: Krishna
authors: K
authors: Pramanik
authors: Department of Chemistry, National Institute of Technology, Rourkela Odisha, 769008, India. Electronic address: girisupr@gmail.com.
authors: Supratim
authors: S
authors: Giri
authors: Department of Biotechnology and Medical Engineering, National Institute of Technology, Rourkela Odisha 769008, India. Electronic address: indraniliit@gmail.com.
authors: Indranil
authors: I
authors: Banerjee
mesh_terms: D000268:Adhesiveness; D000464:Alginates / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D002266:Carboxymethylcellulose Sodium / Q000494:pharmacology*; D003106:Colon / Q000187:drug effects / Q000378:metabolism* / Q000382:microbiology; D019245:Compressive Strength / Q000187:drug effects; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000494:pharmacology; D020723:Glucuronic Acid / Q000494:pharmacology; D006041:Goats; D019073:HT29 Cells; D006603:Hexuronic Acids / Q000494:pharmacology; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D009093:Mucus / Q000378:metabolism; D014961:X-Ray Diffraction
chemical_list: D000464:Alginates; D000970:Antineoplastic Agents; D006603:Hexuronic Acids; D020723:Glucuronic Acid; D002266:Carboxymethylcellulose Sodium; D005472:Fluorouracil
keywords: Bead; Calcium alginate; Carboxymethyl cellulose; Colon-specific delivery; Mucoadhesivity; pH sensitivity