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Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon.
Drug Dev Ind Pharm. 2015; 41(12):2018-28.DD

Abstract

Enteric-coated epichlorohydrin crosslinked dextran microspheres containing 5-Fluorouracil (5-FU) for colon drug delivery was prepared by emulsification-crosslinking method. The formulation variables studied includes different molecular weights of dextran, volume of crosslinking agent, stirring speed, time and temperature. Dextran microspheres showed mean entrapment efficiencies ranging between 77 and 87% and mean particle size ranging between 10 and 25 µm. About 90% of drug was released from uncoated dextran microspheres within 8 h, suggesting the fast release and indicated the drug loaded in uncoated microspheres, released before they reached colon. Enteric coating (Eudragit-S-100 and Eudragit-L-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method. The release study of 5-FU from coated dextran microspheres was complete retardation in simulated gastric fluid (pH 1.2) and once the coating layer of enteric polymer was dissolved at higher pH (7.4 and 6.8), a controlled release of the drug from the microspheres was observed. Further, the release of drug was found to be higher in the presence of dextranase and rat caecal contents, indicating the susceptibility of dextran microspheres to colonic enzymes. Organ distribution and pharmacokinetic study in albino rats was performed to establish the targeting potential of optimized formulation in the colon.

Authors+Show Affiliations

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

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26006331

Citation

Rai, Gopal, et al. "Enteric-coated Epichlorohydrin Crosslinked Dextran Microspheres for Site-specific Delivery to Colon." Drug Development and Industrial Pharmacy, vol. 41, no. 12, 2015, pp. 2018-28.
Rai G, Yadav AK, Jain NK, et al. Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon. Drug Dev Ind Pharm. 2015;41(12):2018-28.
Rai, G., Yadav, A. K., Jain, N. K., & Agrawal, G. P. (2015). Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon. Drug Development and Industrial Pharmacy, 41(12), 2018-28. https://doi.org/10.3109/03639045.2015.1044901
Rai G, et al. Enteric-coated Epichlorohydrin Crosslinked Dextran Microspheres for Site-specific Delivery to Colon. Drug Dev Ind Pharm. 2015;41(12):2018-28. PubMed PMID: 26006331.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon. AU - Rai,Gopal, AU - Yadav,Awesh K, AU - Jain,Narendra K, AU - Agrawal,Govind P, Y1 - 2015/05/26/ PY - 2015/5/27/entrez PY - 2015/5/27/pubmed PY - 2016/8/19/medline KW - 5-FU KW - Colon cancer KW - enzymatic degradation KW - organ distribution KW - pharmacokinetic SP - 2018 EP - 28 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 41 IS - 12 N2 - Enteric-coated epichlorohydrin crosslinked dextran microspheres containing 5-Fluorouracil (5-FU) for colon drug delivery was prepared by emulsification-crosslinking method. The formulation variables studied includes different molecular weights of dextran, volume of crosslinking agent, stirring speed, time and temperature. Dextran microspheres showed mean entrapment efficiencies ranging between 77 and 87% and mean particle size ranging between 10 and 25 µm. About 90% of drug was released from uncoated dextran microspheres within 8 h, suggesting the fast release and indicated the drug loaded in uncoated microspheres, released before they reached colon. Enteric coating (Eudragit-S-100 and Eudragit-L-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method. The release study of 5-FU from coated dextran microspheres was complete retardation in simulated gastric fluid (pH 1.2) and once the coating layer of enteric polymer was dissolved at higher pH (7.4 and 6.8), a controlled release of the drug from the microspheres was observed. Further, the release of drug was found to be higher in the presence of dextranase and rat caecal contents, indicating the susceptibility of dextran microspheres to colonic enzymes. Organ distribution and pharmacokinetic study in albino rats was performed to establish the targeting potential of optimized formulation in the colon. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/26006331/Enteric_coated_epichlorohydrin_crosslinked_dextran_microspheres_for_site_specific_delivery_to_colon_ L2 - http://www.tandfonline.com/doi/full/10.3109/03639045.2015.1044901 DB - PRIME DP - Unbound Medicine ER -