Colonic delivery of compression coated nisin tablets using pectin/HPMC polymer mixture

Uğurlu, Timuçin; Türkoğlu, Murat; Gürer, Ümran Soyoğul; Akarsu, Burçak

doi:10.1016/j.ejpb.2007.01.016

Cited by 95 publications

(37 citation statements)

References 25 publications

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“…Development of colon cancer by chromosomal and microsatellite instability pathways specifically to the colon is ideal for the exploitation of new biotechnology drugs, such as peptides or protein drugs, due to minimized acidic and enzymatic drug degradation otherwise predominant in the upper gastrointestinal tract. The degree of drug absorption can be enhanced by exploiting the greater colon susceptibility to absorption enhancer effects and prolonged dosage form transit time in comparison to upper gastrointestinal tract (28). However, to succeed in colon targeting, it is imperative to deliver drugs at adequate local concentration and without premature drug release/loss in the upper gastrointestinal tract.…”

Section: Colon-specific Oral Drug Delivery Systemmentioning

confidence: 99%

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: Colon-specific Oral Drug Delivery Systemmentioning

confidence: 99%

Pectin Matrix as Oral Drug Delivery Vehicle for Colon Cancer Treatment

2010

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“…However, poor compressibility and difficulties with quality control, particularly with respect to the amount of calcium in the formulation, has impeded the use of calcium pectinate. Stronger polymers, such as hydroxypropyl methylcellulose, have been employed to strengthen pectin gels (Ugurlu et al, 2007;Hodges et al, 2009); however, the presence of these polymers often compromises the sensitivity of the compression coat to colonic microflora.…”

Section: Introductionmentioning

confidence: 99%

Anin situcrosslinked compression coat comprised of pectin and calcium chloride for colon-specific delivery of indomethacin

Wei

Lü

et al. 2014

Drug Delivery

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(2015) An insitu crosslinked compression coat comprised of pectin and calcium chloride for colon-specific delivery of indomethacin, Drug Delivery, 22:3, 298-305, DOI: 10.3109/10717544.2013 AbstractThe use of pectin for colon-specific drug delivery has been extensively investigated; however, when used alone, pectin is often compromised due to its high solubility. This study explored the feasibility of using an in situ compression-coated crosslinking system, composed of pectin and calcium chloride, for colon-specific drug delivery. A pectin/calcium chloride (P/Ca) coating was compressed onto a core tablet. The colon specificity of the compression-coated tablet was verified by dissolution, pharmacokinetics and scintigraphy with 99m Tc labeling. The in situ pectin and calcium chloride gel slowed the release of indomethacin. The lag time varied between 3 h and 7 h depending on the amount of calcium chloride and the coating weight. Pectinase triggered the release of indomethacin from the compression-coated tablet, which was then accelerated by the calcium chloride in the coating layer. The compression-coated tablet had a prolonged t max and apparent t 1/2 , as well as a decreased C max and AUC 0-t , compared with the core tablet counterpart. Evaluation with g-scintigraphy verified colonspecific delivery of the compression-coated tablet. In conclusion, the P/Ca in situ crosslinking system worked well for colon-specific drug delivery.

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“…Although oral administration is not suitable for systemic applications, it is suitable for local applications. Using specialized tablets Ugurlu et al were able to deliver nisin to specific parts of the gut [16]. Other local administration routes as intravaginal, dermic or inhaled forms can be used to achieve local effect as only very low absorption is detected [17][18][19][20].…”

Section: Lantibiotics Versus Antibioticsmentioning

confidence: 99%