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Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon.
Drug Deliv. 2016; 23(1):328-37.DD

Abstract

Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes.

Authors+Show Affiliations

a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India.a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India.a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India.a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

24845476

Citation

Rai, Gopal, et al. "Eudragit-coated Dextran Microspheres of 5-fluorouracil for Site-specific Delivery to Colon." Drug Delivery, vol. 23, no. 1, 2016, pp. 328-37.
Rai G, Yadav AK, Jain NK, et al. Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon. Drug Deliv. 2016;23(1):328-37.
Rai, G., Yadav, A. K., Jain, N. K., & Agrawal, G. P. (2016). Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon. Drug Delivery, 23(1), 328-37. https://doi.org/10.3109/10717544.2014.913733
Rai G, et al. Eudragit-coated Dextran Microspheres of 5-fluorouracil for Site-specific Delivery to Colon. Drug Deliv. 2016;23(1):328-37. PubMed PMID: 24845476.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon. AU - Rai,Gopal, AU - Yadav,Awesh K, AU - Jain,Narendra K, AU - Agrawal,Govind P, Y1 - 2014/05/20/ PY - 2014/5/22/entrez PY - 2014/5/23/pubmed PY - 2016/10/25/medline KW - Colon cancer KW - dextran microspheres KW - dextranase KW - organ distribution KW - pH-sensitive polymers SP - 328 EP - 37 JF - Drug delivery JO - Drug Deliv VL - 23 IS - 1 N2 - Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/24845476/Eudragit_coated_dextran_microspheres_of_5_fluorouracil_for_site_specific_delivery_to_colon_ L2 - http://www.tandfonline.com/doi/full/10.3109/10717544.2014.913733 DB - PRIME DP - Unbound Medicine ER -