Current Applications of Polysaccharides in Colon Targeting

Hovgaard, Lars; Brøndsted, H.V.

doi:10.1615/critrevtherdrugcarriersyst.v13.i3-4.10

Cited by 115 publications

(55 citation statements)

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“…films and wafers) and mucosal fluid such as mucin solution [43] [44] or simulated wound fluid [40]. [45]. They can easily be modified chemically and biochemically and are highly stable, safe, nontoxic, hydrophilic and gel forming and in addition biodegradable.…”

Section: Mucoadhesion Measurement Techniquesmentioning

confidence: 99%

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

Boateng

Okeke²,

Khan³

2015

CPD

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There has been increased interest in novel drug delivery systems to be administered via mucosal routes as an alternative to the currently used traditional routes such as parenteral (injections) and oral routes of administration. This is due to the several advantages they offer including avoiding first pass metabolism in the liver for oral administration and local activity which avoids the need for high systemic doses. To achieve the foregoing objectives, bioadhesive vehicles are required that ensure prolonged residence time to achieve systemic bioavailability via substantial drug absorption or significant drug concentration for local action.The drug delivery system is also required to be non-deleterious to the site of application and be well tolerated by vulnerable groups such as paediatric and geriatric patients. These essential characteristics are mainly satisfied by naturally occurring polymers, including polysaccharide based polymers which have the advantage of biocompatibility, biodegradability and therefore safety. This review discusses various bioadhesive polymers of polysaccharide origin formulated into a variety of dosage forms for drug delivery via the body's mucosal (moist) surfaces including ocular, oral (buccal and sublingual), nasal, gastrointestinal and vaginal mucosa, as well as moist wound sites. The anatomy and / or physiology of each site, coupled with the unique challenges each poses, the strategies employed for ensuring therapeutic efficacy, as well as the current state of the art will also be covered.

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Section: Mucoadhesion Measurement Techniquesmentioning

confidence: 99%

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

Boateng

Okeke²,

Khan³

2015

CPD

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“…[5][6][7] The main principle of action of microflora-activated systems is enzymatic degradation of polysaccharides (such as chitosan, inulin, guar gum, cellulose, xanthan gum, amylose, alginates, dextran, pectin, khaya, and albizia gum) present in the system by colonic bacteria. 8,9 In vitro evaluation of these systems remains a challenge in dissolution studies inhibiting the further discovery of treatment regimes. Moreover, the anaerobic microflora that are highly specific to the colonic region are challenging to assimilate into USP dissolution methods.…”

Section: Introductionmentioning

confidence: 99%

A novel dissolution media for testing drug release from a nanostructured polysaccharide-based colon specific drug delivery system: an approach to alternative colon media

Kotla¹,

Singh²,

Maddiboyina³

et al. 2016

IJN

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The aim of this study was to develop a novel microbially triggered and animal-sparing dissolution method for testing of nanorough polysaccharide-based micron granules for colonic drug delivery. In this method, probiotic cultures of bacteria present in the colonic region were prepared and added to the dissolution media and compared with the performance of conventional dissolution methodologies (such as media with rat cecal and human fecal media). In this study, the predominant species (such as Bacteroides, Bifidobacterium, Lactobacillus species, Eubacterium and Streptococcus ) were cultured in 12% w/v skimmed milk powder and 5% w/v grade “A” honey. Approximately 10 10 –10 11 colony forming units m/L of probiotic culture was added to the dissolution media to test the drug release of polysaccharide-based formulations. A USP dissolution apparatus I/II using a gradient pH dissolution method was used to evaluate drug release from formulations meant for colonic drug delivery. Drug release of guar gum/Eudragit FS30D coated 5-fluorouracil granules was assessed under gastric and small intestine conditions within a simulated colonic environment involving fermentation testing with the probiotic culture. The results with the probiotic system were comparable to those obtained from the rat cecal and human fecal-based fermentation model, thereby suggesting that a probiotic dissolution method can be successfully applied for drug release testing of any polysaccharide-based oral formulation meant for colonic delivery. As such, this study significantly adds to the nanostructured biomaterials’ community by elucidating an easier assay for colonic drug delivery.

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“…These include formation of prodrugs, 13,14 time-dependent delivery systems, 15,16 and coating with pH-sensitive polymers. [17][18][19][20] However, as a site for drug delivery, the colon offers a near-neutral pH, reduced digestive enzymatic activity, and a long transit time. The side effects of drugs are minimized by maximizing their local concentrations at the target site.…”

Section: Introductionmentioning

confidence: 99%

A nanomedicine-promising approach to provide an appropriate colon-targeted drug delivery system for 5-fluorouracil

Singh¹,

Kotla²,

Tomar³

et al. 2015

IJN

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Targeted drug delivery plays a significant role in disease treatment associated with the colon, affording therapeutic responses for a prolonged period of time with low side effects. Colorectal cancer is the third most common cancer in both men and women with an estimated 102,480 cases of colon cancer and 40,340 cases of rectal cancer in 2013 as reported by the American Cancer Society. In the present investigation, we developed an improved oral delivery system for existing anticancer drugs meant for colon cancer via prebiotic and probiotic approaches. The system comprises three components, namely, nanoparticles of drug coated with natural materials such as guar gum, xanthan gum (that serve as prebiotics), and probiotics. The natural gums play a dual role of protecting the drug in the gastric as well as intestinal conditions to allow its release only in the colon. In vitro results obtained from these experiments indicated the successful targeted delivery of 5-fluorouracil to the colon. Electron microscopy results demonstrated that the prepared nanoparticles were spherical in shape and 200 nm in size. The in vitro release data indicated that the maximum release occurs at pH 7.2 and 7.4 with 93% of the drug released in the presence of 4% (w/v) of rat cecal content. In vivo results conclude a practical mechanism to maintain the integrity and intactness of the intestinal/colonic microflora, in the face of a “chemical attack” by oral colon-targeted drug delivery for colon cancer treatment.

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Current Applications of Polysaccharides in Colon Targeting

Cited by 115 publications

References 0 publications

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

A novel dissolution media for testing drug release from a nanostructured polysaccharide-based colon specific drug delivery system: an approach to alternative colon media

A nanomedicine-promising approach to provide an appropriate colon-targeted drug delivery system for 5-fluorouracil

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