Mucoadhesive properties of various pectins on gastrointestinal mucosa: An in vitro evaluation using texture analyzer

Thirawong, Nartaya; Nunthanid, Jurairat; Puttipipatkhachorn, Satit; Sriamornsak, Pornsak

doi:10.1016/j.ejpb.2007.01.010

Cited by 243 publications

(129 citation statements)

References 26 publications

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“…Fortunately, pectin shows maximum mucoadhesion on the large intestinal tissue compared to other regions of the GIT, which represents an added advantage for colon targeting (Thirawong et al, 2007). It is noteworthy that the pressure applied to adhere MPs to the hydrated mucin discs is not relevant to the in vivo conditions but this test is helpful in screening the most promising formulation in terms of mucoadheisve strength.…”

Section: In Vitro Mucoadhesion Studiesmentioning

confidence: 99%

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

et al. 2015

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The colon is a promising target for drug delivery owing to its long transit time of up to 78 h, which is likely to increase the time available for drug absorption. Progesterone has a short elimination half-life and undergoes extensive first-pass metabolism, which results in very low oral bioavailability ($25%). To overcome these shortcomings, we developed an oral multiparticulate system for the colonic delivery of progesterone. Zn-pectinate/chitosan microparticles were prepared by ionotropic gelation and characterized for their size, shape, weight, drug entrapment efficiency, mucoadhesion and swelling behavior. The effect of crosslinking pH, cross-linking time and chitosan concentration on progesterone release were also studied. Spherical microparticles having a diameter of 580-720 mm were obtained. Drug entrapment efficiency of $75-100% was obtained depending on the microparticle composition. Microparticle mucoadhesive properties were dependent on the pectin concentration, as well as the cross-linking pH. Progesterone release in simulated gastric fluids was minimal (3-9%), followed by burst release at pH 6.8 and a sustained phase at pH 7.4. The in vivo study revealed that the microparticles significantly increased progesterone residence time in the plasma and increased its relative bioavailability to $168%, compared to the drug alone. This study confirms the potential of Zn-pectinate/chitosan microparticles as a colon-specific drug delivery system able to enhance the oral bioavailability of progesterone or similar drugs.

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Section: In Vitro Mucoadhesion Studiesmentioning

confidence: 99%

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

et al. 2015

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“…The process of mucoadhesion 60 involves wetting and swelling of polymer, interpenetration between the polymer chains and the mucosal membrane and formation of chemical bonds between the entangled chains and mucin (Palacio et al, 2012). There are several approaches used to assess the mucoadhesive performance of polymeric dosage forms including texture analyser (Thirawong et al, 2007;Ayensu et al, 2012), rheometry (Tamburic and Craig, 1997) and chemometrics (Boateng et 65 al., 2015). The texture analyser technique (TA) assesses the stickiness, the total work of adhesion (TWA) and the cohesiveness of the dosage forms.…”

Section: Introductionmentioning

confidence: 99%

“…Stickiness is described as the maximum force (peak adhesive force -PAF)) required to separate the probe attached to the formulation from the mucosal substrate whereas, the total amount of work exerted in detaching the probe from the mucosal substrate is referred to as work of adhesion and is calculated from 70 the area under the force versus distance curve. Cohesiveness is defined as the intermolecular attraction between the mucosal substrate and formulation, and determined by the travel distance in mm on the force versus distance plot (Thirawong et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Functional physico-chemical, ex vivo permeation and cell viability characterization of omeprazole loaded buccal films for paediatric drug delivery

Khan

Trivedi

Boateng

2016

International Journal of Pharmaceutics

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25Buccal films were prepared from aqueous and ethanolic Metolose gels using the solvent casting approach (40°C). The hydration (PBS and simulated saliva), mucoadhesion, physical stability (20°C, 40°C), in vitro drug (omeprazole) dissolution (PBS and simulated saliva), ex vivo permeation (pig buccal mucosa) in presence of simulated saliva, ex vivo bioadhesion and cell viability using MTT of drug loaded (DL) films were investigated. Hydration and mucoadhesion 30 results showed that swelling capacity and adhesion was higher in the presence of PBS than simulated saliva (SS) due to differences in ionic strength. Omeprazole was more stable at 20°C than 40°C whilst omeprazole release reached a plateau within 1 hour and faster in PBS than in SS. Fitting release data to kinetic models showed that Korsmeyer-Peppas equation best fit the dissolution data. Drug release in PBS was best described by zero order via non-Fickian 35 diffusion but followed super case II transport in SS attributed to drug diffusion and polymer erosion. The amount of omeprazole permeating over 2 hours was 275ug/cm 2 whilst the formulations and starting materials showed cell viability values greater than 95%, confirming their safety for potential use in paediatric buccal delivery.

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“…It has been suggested that the interaction between a mucosal (moist) surface and mucoadhesive polymers is a result of physical entanglement and secondary interactive forces, mainly due to hydrogen bonding and van der Waals attraction forces which depend upon the chemical structure of the polymer 10 . Peppas and Buri proposed certain characteristics which are necessary for effective mucoadhesion.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of in vitro wound adhesion characteristics of composite film and wafer based dressings using texture analysis and FTIR spectroscopy: a chemometrics factor analysis approach

Boateng

Pawar

2015

RSC Adv.

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The adhesive properties of two dressing types, solvent cast films and freeze-dried wafers have been determined and compared using two analytical techniques, combined with chemometrics data analysis. Films and wafers were prepared from gels containing polyox (POL) combined with carrageenan (CAR) or sodium alginate (SA), glycerol (GLY) as plasticiser (films) with streptomycin and diclofenac as model drugs. The gels were dried in an oven at 40°C or freeze-dried to obtain films and wafers respectively. The adhesive performance of the films and wafers was assessed with 6.67% w/v gel using a texture analyser to measure the stickiness, work of adhesion and cohesiveness. The effect of viscosity of simulated wound fluid[(containing (2% w/w or 5% w/w bovine serum albumin)] and mucin solution (2% w/w) present on the gelatin surface on texture analyser profiles was investigated. Furthermore, the adhesive properties were estimated and evaluated using attenuated total reflectance Fourier transform infrared spectroscopy by monitoring the diffusion of mucin solution [2% w/w in phosphate buffered saline (PBS) pH 7.4] through the formulations. The diffusion data was analysed using target factor analysis (chemometrics approach) to establish proof of concept for predicting adhesion by measuring mucin interaction and its diffusion through films and wafers. There was a significant effect of simulated wound fluid, viscosity, plasticizer (for films) and drug loading on the adhesive performance of both films and wafers. POL-SA films showed higher mucoadhesive performance in the presence of viscous simulated wound fluid containing 5% bovine serum albumin. Wafers and plasticised films demonstrated high detachment force indicating strong interactions between the chains of the polymers (POL, SA and CAR) and the model wound surface (gelatin). ATR-FTIR spectroscopy showed that mucin diffused independently through the solvent and across the films and wafers. POL-CAR films generally showed slower diffusion of mucin when compared with POL-SA films whilst the opposite effect was observed for diffusion through POL-CAR wafers and POL-SA wafers. Generally, diffusion through wafers was faster than the corresponding films.

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Mucoadhesive properties of various pectins on gastrointestinal mucosa: An in vitro evaluation using texture analyzer

Cited by 243 publications

References 26 publications

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

Functional physico-chemical, ex vivo permeation and cell viability characterization of omeprazole loaded buccal films for paediatric drug delivery

Evaluation of in vitro wound adhesion characteristics of composite film and wafer based dressings using texture analysis and FTIR spectroscopy: a chemometrics factor analysis approach

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