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


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.


CONCLUSIONS
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).


CONCLUSIONS
Most of the natural phytochemical or antioxidants show pretreatment effectiveness. We, however, developed and established S-FBs for sustained curative effect.
Department of Pharmaceutics, UGC Centre for Advance Study, University Institute of Pharmaceutical Sciences, Panjab University , Chandigarh , India.
T
T
Geetha
Parneet Kaur
PK
Deol
Indu Pal
IP
Kaur
D000818:Animals; D052117:Benzodioxoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D009374:Neoplasms, Experimental / Q000097:blood* / Q000139:chemically induced / Q000188:drug therapy*; D010636:Phenols / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013274:Stomach Neoplasms / Q000097:blood* / Q000139:chemically induced / Q000188:drug therapy*
D052117:Benzodioxoles; D004337:Drug Carriers; D010636:Phenols; C025583:sesamol
Antioxidant; FDDS; calcium alginate beads; pharmacokinetics