PMID- 28392387 OWN - NLM STAT- MEDLINE DCOM- 20180312 LR - 20180312 IS - 1879-0003 (Electronic) IS - 0141-8130 (Linking) VI - 102 DP - 2017 Sep TI - Functionally modified polyacrylamide-graft-gum karaya pH-sensitive spray dried microspheres for colon targeting of an anti-cancer drug. PG - 829-839 LID - S0141-8130(16)32774-X [pii] LID - 10.1016/j.ijbiomac.2017.04.023 [doi] AB - An effort was made to formulate and evaluate pH-sensitive spray dried microspheres using hydrolyzed polyacrylamide-graft-gum karaya (PAAm-g-GK) for colon specific delivery of an anti-cancer agent, capecitabine. The synthesis of pH-sensitive PAAm-g-GK copolymer was done by free radical polymerization followed by alkaline hydrolysis and characterized satisfactorily. The microspheres were spherical in shape; drug entrapment efficiency was found to be in the range of 77.30% to 88.74%. Pulsatile swelling study indicates that the PAAm-g-GK consists of considerable pH-sensitivity. The in-vitro drug release suggested that the microspheres prepared using native GK were incapable to retard the drug release within 5h in the environment of stomach and small intestine. While, those microspheres prepared using pH-sensitive PAAm-g-GK copolymer having crosslinked with glutaraldehyde (GA), released little amount of drug within 5h, but maximum amount of drug was targeted to colonic region in a controlled manner up to 24h. For example, GK10 Microspheres showed only 19.16% drug release at the end of 5th h, while about 80.14% of drug was targeted to colonic region. Cross-linking with GA reduced the early drug release in the upper part of gastrointestinal tract and guaranteed maximum drug release in the colonic region. A rapid enhancement in drug release was witnessed in rat caecal content medium due to the action of colonic bacteria on PAAm-g-GK copolymer. CI - Copyright (c) 2017 Elsevier B.V. All rights reserved. FAU - Alange, Vijaykumar V AU - Alange VV AD - Department of Pharmaceutics, BLDEA's SSM College of Pharmacy and Research Centre, BLDE University Campus, Vijayapur (Bijapur), 586103, Karnataka, India. FAU - Birajdar, Ravindra P AU - Birajdar RP AD - Department of Pharmaceutics, BLDEA's SSM College of Pharmacy and Research Centre, BLDE University Campus, Vijayapur (Bijapur), 586103, Karnataka, India. FAU - Kulkarni, Raghavendra V AU - Kulkarni RV AD - Department of Pharmaceutics, BLDEA's SSM College of Pharmacy and Research Centre, BLDE University Campus, Vijayapur (Bijapur), 586103, Karnataka, India. Electronic address: pharma_75raghu@yahoo.com. LA - eng PT - Journal Article DEP - 20170406 PL - Netherlands TA - Int J Biol Macromol JT - International journal of biological macromolecules JID - 7909578 RN - 0 (Acrylic Resins) RN - 0 (Antineoplastic Agents) RN - 0 (Drug Carriers) RN - 6804DJ8Z9U (Capecitabine) RN - 9000-36-6 (Karaya Gum) RN - 9003-05-8 (polyacrylamide) SB - IM MH - Acrylic Resins/*chemistry MH - Animals MH - Antineoplastic Agents/*chemistry/*metabolism MH - Capecitabine/chemistry/metabolism MH - Cecum/metabolism MH - Colon/*metabolism MH - Drug Carriers/*chemistry MH - Drug Liberation MH - Hydrogen-Ion Concentration MH - Karaya Gum/*chemistry MH - *Microspheres MH - Rats OTO - NOTNLM OT - Capecitabine OT - Colon targeting OT - Gum karaya OT - Spray drying OT - pH-sensitive graft copolymer EDAT- 2017/04/11 06:00 MHDA- 2018/03/13 06:00 CRDT- 2017/04/11 06:00 PHST- 2016/12/05 00:00 [received] PHST- 2017/03/26 00:00 [revised] PHST- 2017/04/05 00:00 [accepted] PHST- 2017/04/11 06:00 [pubmed] PHST- 2018/03/13 06:00 [medline] PHST- 2017/04/11 06:00 [entrez] AID - S0141-8130(16)32774-X [pii] AID - 10.1016/j.ijbiomac.2017.04.023 [doi] PST - ppublish SO - Int J Biol Macromol. 2017 Sep;102:829-839. doi: 10.1016/j.ijbiomac.2017.04.023. Epub 2017 Apr 6.