Role of sesamol-loaded floating beads in gastric cancers: a pharmacokinetic and biochemical evidence.

Abstract

CONTEXT:

Sesamol, a potential antioxidant with marked anticancer potential suffers from issues of extensive tissue distribution and local gastric irritation on oral administration.

OBJECTIVE:

To develop multiunit gastro-retentive floating beads (S-FBs) for localised and prolonged release of sesamol to treat gastric cancers.

MATERIALS AND METHODS:

S-FBs prepared using calcium carbonate, sodium alginate and hydroxypropylmethyl cellulose (HPMC) in different proportions, were characterised and evaluated in vivo in N-methyl-N-nitro-N-nitroguanidine-induced gastric cancer in rats. Single oral dose plasma pharmacokinetic study was also performed for free sesamol and S-FBs.

RESULTS AND DISCUSSION:

Restraining sesamol in floating beads, significantly lowered the release (diffusion controlled) rate, increased t50% (31 times) and reduced its in vivo clearance (>1.5 times). Preclinical evaluation showed S-FBs (10 mg/kg) to be significantly better than free sesamol and better/equivalent to methotrexate (2 mg/kg).

CONCLUSION:

Most of the natural phytochemical or antioxidants show pretreatment effectiveness. We, however, developed and established S-FBs for sustained curative effect.

• Authors: T Geetha, Parneet Kaur Deol, Indu Pal Kaur
• Journal: Journal of microencapsulation (J Microencapsul) Vol. 32 Issue 5 Pg. 478-87 ( 2015) ISSN: 1464-5246 [Electronic] England
• PMID: 26268954 (Publication Type: Journal Article)

Chemical References

• Benzodioxoles
• Drug Carriers
• Phenols
• sesamol

Topics

• Animals
• Benzodioxoles (chemistry, pharmacokinetics, pharmacology)
• Drug Carriers (chemistry, pharmacokinetics, pharmacology)
• Male
• Neoplasms, Experimental (blood, chemically induced, drug therapy)
• Phenols (chemistry, pharmacokinetics, pharmacology)
• Rats
• Rats, Wistar
• Stomach Neoplasms (blood, chemically induced, drug therapy)