Colon-specific tablets containing 5-fluorouracil microsponges for colon cancer targeting

Mahmoud H. Othman, Gamal M. Zayed, Usama F. Ali, Ahmed A.H. Abdellatif

Research output: Contribution to journalJournal articlepeer-review

2 Scopus citations


Most anticancer medications undergo major first-pass metabolism in the intestinal wall, the liver, or both. 5-fluorouracil (5-FU) is known to have erratic oral bioavailability due to first-pass metabolism. The present study aimed to develop 5-FU-loaded microsponges (MS) compressed in enteric-coated tablets as a new colon targeting to colorectal cancer. MS was prepared as a controlled release system for 5-FU and characterized for drug encapsulation efficiency, and surface morphology. Further, hydroxypropyl methylcellulose (HPMC) was mixed with pectin and characterized for their flow as a tablet coat enclosing the core tablets of 5-FU-MS. Moreover, in vitro drug release behavior was studied in different pH media, while the X-ray imaging was used to monitor the in vivo movement of prepared tablets containing 5-FU-MS throughout the GI system. The results showed that MS were spherical in shape and have several pores on their surfaces. The encapsulation efficiency was from 71.80 ± 1.62% − 101.3 ± 2.60%, while the particle size was from 53.11 ± 41.03 − 118.12 ± 48.21 nm. The formulated tablets were fulfilling all official and other specifications and exhibited sustained release of 5-FU only inside the colon. The in vivo human volunteer study of X-ray has shown that the tablets ultimately reached the colon without disturbing in the upper GI system. The obtained carrier formulation is considered as a novel system to deliver 5-FU to the colon tumor with 100% targeting without any drug release in the upper GIT or first-pass metabolism.

Original languageEnglish
Pages (from-to)2081-2088
Number of pages8
JournalDrug Development and Industrial Pharmacy
Issue number12
StatePublished - 2020


  • 5-fluorouracil (5-FU)
  • Colon targeting
  • HPMC
  • microsponges (MS)
  • pectin
  • X-ray imaging


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