Tags

Type your tag names separated by a space and hit enter

Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting.
AAPS PharmSciTech. 2007 Feb 16; 8(1):12.AP

Abstract

An objective of the present investigation was to prepare and evaluate Eudragit-coated pectin microspheres for colon targeting of 5-fluorouracil (FU). Pectin microspheres were prepared by emulsion dehydration method using different ratios of FU and pectin (1:3 to 1:6), stirring speeds (500-2000 rpm) and emulsifier concentrations (0.75%-1.5% wt/vol). The yield of preparation and the encapsulation efficiencies were high for all pectin microspheres. Microspheres prepared by using drug:polymer ratio 1:4, stirring speed 1000 rpm, and 1.25% wt/vol concentration of emulsifying agent were selected as an optimized formulation. Eudragit-coating of pectin microspheres was performed by oil-in-oil solvent evaporation method using coat:core ratio (5:1). Pectin microspheres and Eudragit-coated pectin microspheres were evaluated for surface morphology, particle size and size distribution, swellability, percentage drug entrapment, and in vitro drug release in simulated gastrointestinal fluids (SGF). The in vitro drug release study of optimized formulation was also performed in simulated colonic fluid in the presence of 2% rat cecal content. Organ distribution study in albino rats was performed to establish the targeting potential of optimized formulation in the colon. The release profile of FU from Eudragit-coated pectin microspheres was pH dependent. In acidic medium, the release rate was much slower; however, the drug was released quickly at pH 7.4. It is concluded from the present investigation that Eudragit-coated pectin microspheres are promising controlled release carriers for colon-targeted delivery of FU.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar, India.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Evaluation Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17408212

Citation

Paharia, Amol, et al. "Eudragit-coated Pectin Microspheres of 5-fluorouracil for Colon Targeting." AAPS PharmSciTech, vol. 8, no. 1, 2007, p. 12.
Paharia A, Yadav AK, Rai G, et al. Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting. AAPS PharmSciTech. 2007;8(1):12.
Paharia, A., Yadav, A. K., Rai, G., Jain, S. K., Pancholi, S. S., & Agrawal, G. P. (2007). Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting. AAPS PharmSciTech, 8(1), 12.
Paharia A, et al. Eudragit-coated Pectin Microspheres of 5-fluorouracil for Colon Targeting. AAPS PharmSciTech. 2007 Feb 16;8(1):12. PubMed PMID: 17408212.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting. AU - Paharia,Amol, AU - Yadav,Awesh K, AU - Rai,Gopal, AU - Jain,Sunil K, AU - Pancholi,Shyam S, AU - Agrawal,Govind P, Y1 - 2007/02/16/ PY - 2007/4/6/pubmed PY - 2007/5/2/medline PY - 2007/4/6/entrez SP - 12 EP - 12 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 8 IS - 1 N2 - An objective of the present investigation was to prepare and evaluate Eudragit-coated pectin microspheres for colon targeting of 5-fluorouracil (FU). Pectin microspheres were prepared by emulsion dehydration method using different ratios of FU and pectin (1:3 to 1:6), stirring speeds (500-2000 rpm) and emulsifier concentrations (0.75%-1.5% wt/vol). The yield of preparation and the encapsulation efficiencies were high for all pectin microspheres. Microspheres prepared by using drug:polymer ratio 1:4, stirring speed 1000 rpm, and 1.25% wt/vol concentration of emulsifying agent were selected as an optimized formulation. Eudragit-coating of pectin microspheres was performed by oil-in-oil solvent evaporation method using coat:core ratio (5:1). Pectin microspheres and Eudragit-coated pectin microspheres were evaluated for surface morphology, particle size and size distribution, swellability, percentage drug entrapment, and in vitro drug release in simulated gastrointestinal fluids (SGF). The in vitro drug release study of optimized formulation was also performed in simulated colonic fluid in the presence of 2% rat cecal content. Organ distribution study in albino rats was performed to establish the targeting potential of optimized formulation in the colon. The release profile of FU from Eudragit-coated pectin microspheres was pH dependent. In acidic medium, the release rate was much slower; however, the drug was released quickly at pH 7.4. It is concluded from the present investigation that Eudragit-coated pectin microspheres are promising controlled release carriers for colon-targeted delivery of FU. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/17408212/Eudragit_coated_pectin_microspheres_of_5_fluorouracil_for_colon_targeting_ L2 - https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/17408212/ DB - PRIME DP - Unbound Medicine ER -