Metabolism of pectin in the gastrointestinal tract

Dongowski, G.; Anger, H.

doi:10.1016/s0921-0423(96)80300-5

Cited by 13 publications

(11 citation statements)

References 5 publications

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“…Pectin is completely fermented in colon by microflora with low esterified pectin being fermented faster than high esterified pectin (61). It appears that only a partial degradation is possible at the pH 2 to 4 conditions of stomach via side chain hydrolysis and at pH 5 to 6 conditions of small intestine via β-elimination of main chain or de-esterification (61,62).…”

Section: Pectin As Colon-specific Oral Drug Delivery Vehiclementioning

confidence: 99%

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Pectin Matrix as Oral Drug Delivery Vehicle for Colon Cancer Treatment

2010

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Abstract. Colon cancer is the fourth most common cancer globally with 639,000 deaths reported annually. Typical chemotherapy is provided by injection route to reduce tumor growth and metastasis. Recent research investigates the oral delivery profiles of chemotherapeutic agents. In comparison to injection, oral administration of drugs in the form of a colon-specific delivery system is expected to increase drug bioavailability at target site, reduce drug dose and systemic adverse effects. Pectin is suitable for use as colon-specific drug delivery vehicle as it is selectively digested by colonic microflora to release drug with minimal degradation in upper gastrointestinal tract. The present review examines the physicochemical attributes of formulation needed to retard drug release of pectin matrix prior to its arrival at colon, and evaluate the therapeutic value of pectin matrix in association with colon cancer. The review suggests that multi-particulate calcium pectinate matrix is an ideal carrier to orally deliver drugs for site-specific treatment of colon cancer as (1) crosslinking of pectin by calcium ions in a matrix negates drug release in upper gastrointestinal tract, (2) multi-particulate carrier has a slower transit and a higher contact time for drug action in colon than single-unit dosage form, and (3) both pectin and calcium have an indication to reduce the severity of colon cancer from the implication of diet and molecular biology studies. Pectin matrix demonstrates dual advantages as drug carrier and therapeutic for use in treatment of colon cancer.

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Section: Pectin As Colon-specific Oral Drug Delivery Vehiclementioning

confidence: 99%

“…It appears that only a partial degradation is possible at the pH 2 to 4 conditions of stomach via side chain hydrolysis and at pH 5 to 6 conditions of small intestine via β-elimination of main chain or de-esterification (61,62). Nonetheless, pectin is an aqueous soluble polymer.…”

Section: Pectin As Colon-specific Oral Drug Delivery Vehiclementioning

confidence: 99%

Pectin Matrix as Oral Drug Delivery Vehicle for Colon Cancer Treatment

2010

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“…Minispheres coated with Surelease ® /Pectin were detected in the rat colon by X-ray imaging just before disintegrating, demonstrating the suitability of this formulation for colonic release of sCT. Even though rat colonic microflora is not able to digest pectin (unlike in man), pectin is still resistant to proteases active in the upper GI tract of both species [40]. In addition, pectin is retained in the coating layer absorbing surrounding water, and swells to form water channels and facilitates dissolution.…”

Section: Discussionmentioning

confidence: 99%

Coated minispheres of salmon calcitonin target rat intestinal regions to achieve systemic bioavailability: Comparison between intestinal instillation and oral gavage

Aguirre

Aversa

Rosa

et al. 2016

Journal of Controlled Release

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Achieving oral peptide delivery is an elusive challenge. Emulsion-based minispheres of salmon calcitonin (sCT) were synthesized using single multiple pill (SmPill ® ) technology incorporating the permeation enhancers (PEs): sodium taurodeoxycholate (NaTDC), sodium caprate (C 10 ), or coco-glucoside (CG), or the pH acidifier, citric acid (CA). Minispheres were coated with an outer layer of Eudragit ® L30 D-55 (designed for jejunal release) or Surelease ® /Pectin (designed for colonic release). The process was mild and in vitro biological activity of sCT was retained upon release from minispheres stored up to 4 months. In vitro release profiles suggested that sCT was released from minispheres by diffusion through coatings due to swelling of gelatin and the polymeric matrix upon contact with PBS at pH 6.8.X-ray analysis confirmed that coated minispheres dissolved at the intended intestinal region of rats following oral gavage. Uncoated minispheres at a dose of ~2000 I.U. sCT/kg were administered to rats by intra-jejunal (i.j.) or intra-colonic (i.c.) instillation and caused hypocalcaemia. Notable sCT absolute bioavailability (F) values were: 5.5% from minispheres containing NaTDC (i.j), 17.3% with CG (i.c.) and 18.2 % with C 10 (i.c.). Coated minispheres administered by oral gavage at threefold higher doses also induced hypocalcaemia. A highly competitive F value of 2.7% was obtained for orally-administered sCT-minispheres containing CG (45 μmol/kg) and coated with Eudragit ® . In conclusion, the SmPill ® technology is a potential dosage form for several peptides when formulated with PEs and coated for regional delivery. PK data from instillations over-estimates oral bioavailability and poorly predicts rank ordering of formulations .

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“…Pectic substances are generally regarded as nondigestible in the upper intestine. In rats, pectin is depolymerized and deesterified only to a small extent after passing through the small intestine and is excreted nearly unchanged in germ-free rats (39). Fermentation of pectic polysaccharides by gut microflora, however, may produce short intermediates that could be absorbed in the colon.…”

Section: Bioavailabilitymentioning

confidence: 99%