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PubMed2002

Drug release properties of pectinate microspheres prepared by emulsification method.

This study explored the potential of pectin for use in making microspheres for sustained-release of drugs. The pectin microspheres were prepared by external gelation using an emulsification technique with calcium chloride as the crosslinking agent. The influences of drug core (sulphanilamide, sulphaguanidine and sulphathiazole) and dissolution media (distilled water, USP HCl and phosphate buffers) on the drug release properties of the pectinate microspheres were examined. The morphology and drug content of the microspheres, and the solubility and solution pH of the drugs were also determined. Pectinate microspheres were successfully prepared by the emulsification technique. The rate of drug released from microspheres was highest in USP HCl buffer, followed by USP phosphate buffer and distilled water. Interestingly, the lowest percentage of drug released was produced by microspheres which were smallest in size and therefore largest in specific surface area, and consisting of sulphanilamide, the most water soluble drug. Further investigation showed that the microspheres consisted of both bound and unbound drugs. The percentage of drug released was predominantly determined by the relative contents of bound and unbound drugs embedded in the pectinate matrix.

Anti-Infective Agents↗
PubMed2000

Development of pectin matrix tablets for colonic delivery of model drug ropivacaine.

The objective of this work was to develop pectin-based matrix tablets for colonic delivery of the model drug ropivacaine, with the future perspective of radiolabelling the system by neutron activation technique for a gamma-scintigraphic study. The aim was to investigate some formulation factors that could reduce the release of the drug in the simulated gastric and intestinal fluids, increase the release in the simulated cecal fluid (with pectinolytic enzymes) and improve the poor compactibility of pectins. For dissolution studies, the flow-through apparatus with sequential dissolution liquids simulating the mouth-to-colon conditions was used. The effect of two pectin types, the incorporation of ethylcellulose as a dry matrix-additive and water or ethanol as granulation liquids were investigated in a study designed as a D-optimal mixture. Amidated pectin (Am.P) produced harder tablets than the calcium salt of pectin (Ca.P) and was more susceptible to enzymatic degradation. Addition of ethylcellulose increased the tablet strength and the dissolution rate. Furthermore, directly compressed Am.P tablets were produced by addition of coarse or micronised qualities of ethylcellulose. The latter improved the crushing strength markedly imposing a marginal release-reducing effect. Coating this formulation with Eudragit((R)) L 100 reduced the release in the simulated upper GI conditions without interference with the subsequent enzymatic activity.

Amides↗
PubMed2002

Pectinic acid, a novel excipient for production of pellets by extrusion/spheronisation: preliminary studies.

A very low soluble pectin-derivative (pectinic acid, degree of methoxylation 4%) was found to be well suited as an excipient for pelletisation by extrusion/spheronisation. Formulations containing pectinic acid and lactose in the following ratios were evaluated: 99/1, 80/20, 50/50 and 20/80. The capacity as an extrusion aid was found to be high; even formulations containing only 20% pectinic acid resulted in nearly spherical pellets. All pectinic acid pellets were mechanically stable, had an aspect ratio of approximately 1.15-1.20 and released 30-60% of a low solubility model drug within 15 min both in simulated gastric acid (0.1M HCl) and intestinal fluid (phosphate buffer pH 6.8).

Chemistry, Pharmaceutical↗
PubMed2004

Intestinal steroids in rats are influenced by the structural parameters of pectin.

We investigated the effects of pectin with different degrees of methylation (34.5, 70.8, and 92.6%, respectively) on the composition and concentration of intestinal and fecal bile acids and neutral sterols in conventional and germfree rats. Diets containing 6.5% pectin (galacturonan) were given for 3 weeks. High concentrations of free and secondary bile acids appeared in cecum and colon of conventional rats. With increasing degree of methylation, more bile acids were transported into lower parts of intestinal tract and excreted whereas the proportion of secondary bile acids decreased. In contrast, the composition of bile acids in intestinal contents and feces was relatively unchanged in germfree rats. Exclusively cholesterol was found as a neutral sterol in germfree rats. Coprostanol appeared in cecum of conventional rats and additionally coprostanone in colon. Amounts of neutral sterols increased with increasing degree of methylation of pectin. Additionally, concentrations of bile acids in plasma decreased if the pectin-containing diets were given. Besides the degree of methylation, the molecular weight of pectin used in the diets influenced concentration and composition of intestinal and fecal steroids in rats.

Animals↗
PubMedDate not supplied

Thermoreversible gelation of aqueous mixtures of pectin and chitosan. Rheology.

The synergistic interaction between pectin and chitosan in aqueous acid solution and in the gel phase has been studied by oscillatory shear measurements. Mixtures of pectin and chitosan form thermoreversible gels over a broad composition range by lowering the temperature. The value of the gelation temperature depends on the composition of the mixture, with low values for mixtures with low pectin contents. For incipient gels, a power law can describe the frequency dependence of the complex viscosity, with power law exponents close to -1. The gel evolution of pectin-chitosan mixtures upon a temperature quench below the gel point has been studied. Evidence is provided for a relation between gelation and phase separation in the process of temperature-induced gelation of pectin-chitosan mixtures. A simple model is proposed to rationalize the gelation process in these systems.

Carbohydrate Sequence↗
PubMedDate not supplied

Aggregation during coniferyl alcohol polymerization in pectin solution: a biomimetic approach of the first steps of lignification.

Coniferyl alcohol was polymerized in pectin solution in order to mimic the lignification that is the final step of biosynthesis of plant cell wall. Dehydrogenated polymers (DHP = coniferyl alcohol polymers = synthetic lignin) interact with pectin to form hydrophobic clusters as monitored by pyrene fluorescence spectroscopy. The structure of these clusters was studied during the polymerization of synthetic lignin by static and quasielastic light scattering and small angle neutron scattering experiments. We show that synthetic lignin and pectin contribute to the same clusters, but the inner structure of these clusters is very heterogeneous and displays three phases. One observes a segregation between well separated pectin and lignin rich phases at length scales below approximately 30 nm. As a corollary of this segregation, clusters embody a large amount of solvent. On average, the density of the polymer rich phase (lignin plus pectin) inside clusters increases while its specific surface area decreases throughout the polymerization process. These results are discussed with respect to in vivo lignification of the plant cell wall.

Biomimetic Materials↗
PubMed2003

Separation and characterization of a salt-dependent pectin methylesterase from Citrus sinensis var. Valencia fruit tissue.

A pectin methylesterase (PME) from sweet orange fruit rag tissue, which does not destabilize citrus juice cloud, has been characterized. It is a salt-dependent PME (type II) and exhibits optimal activity between 0.1 and 0.2 M NaCl at pH 7.5. The pH optimum shifted to a more alkaline range as the salt molarity decreased (pH 8.5-9.5 at 50 mM NaCl). It has an apparent molecular mass of 32.4 kDa as determined by gel filtration chromatography, an apparent molecular mass of 33.5 kDa as determined by denaturing electrophoresis, and a pI of 10.1 and exhibits a single activity band after isoelectric focusing (IEF). It has a K(m) of 0.0487 mg/mL and a V(max) of 4.2378 nkat/mg of protein on 59% DE citrus pectin. Deblocking the N-terminus revealed a partial peptide composed of SVTPNV. De-esterification of non-calcium-sensitive pectin by 6.5% increased the calcium-sensitive pectin ratio (CSPR) from 0.045 +/- 0.011 to 0.829 +/- 0.033 but had little, if any, effect on pectin molecular weight. These properties indicate this enzyme will be useful for studying the PME mode of action as it relates to juice cloud destabilization.

Carboxylic Ester Hydrolases↗
PubMed2004

Pectin hydroxamic acids exhibit antioxidant activities in vitro.

Commercial pectins with different degrees of esterification (DE) were reacted with equal volumes of 2 M alkaline hydroxylamine (pH 12.0) at room temperature for 4 h to prepare pectin hydroxamic acids (PHAs; DE94T4, DE65T4, and DE25T4) according to a previously reported method (Hou et al., J. Agric. Food Chem. 2003, 51, 6362-6366) and were used to test the antioxidant and antiradical activities in comparison with those of DE94, DE65, and DE25 pectins. The half-inhibition concentrations, IC(50), of scavenging activity against DPPH were 1.51, 5.43, and 5.63 mg/mL for DE94T4, DE65T4, and DE25T4, respectively, and were much lower than those of corresponding DE pectins under the same concentrations. The scavenging activities of PHAs for DPPH radicals were positively correlated with original DE values of pectin. The optimal pH of DE94T4 for scavenging DPPH radicals was 7.9 or 8.0. Using electron spin resonance (ESR) for scavenging hydroxyl radicals, under the same concentrations of 125 microg/mL, DE94T4, DE65T4, and DE25T4, respectively, exhibited 73.53, 69.01, and 55.17% antiradical activities. PHAs also exhibited protection against hydroxyl radical-mediated DNA damage and anti-human low-density lipoprotein peroxidation tests.

Animals↗
PubMed2006

Effects of heat treatment and pectin addition on beta-lactoglobulin allergenicity.

The specific effects of heat treatment and/or addition of low/high-methylated pectin (LMP/HMP) on the allergenicity of beta-lactoglobulin (beta-Lg) and its hydrolysis products were investigated through a two-step in vitro digestion approach. beta-Lg was first hydrolyzed by pepsin and then by a trypsin/chymotrypsin (T/C) mixture done in a dialysis bag with a molecular weight cutoff of 1000. The protein digestion was followed by SDS-PAGE electrophoresis performed on each digestion product, and their in vitro allergenicity was analyzed by immunoblotting. Such procedure was applied on beta-Lg samples mixed with the two kinds of pectin before or after heating (80 degrees C, 25 min) to determine the respective impact of heat treatment and pectin addition. Heat denaturation improved significantly the susceptibility of beta-Lg against the pepsin and the T/C. This effect, which was coupled to a reduction in immunoreactivity of the digested beta-Lg, appeared to be distinctively modulated by LMP and HMP. Through nonspecific interaction with the beta-Lg, pectin could reduce the accessibility of cleavage sites and/or epitope sequences. This mechanism of action is discussed in relation to the intra- and intermolecular interactions between beta-Lg and pectin initiated under the experimental conditions.

Allergens↗
PubMed2006

Use of a Plackett-Burman experimental design to examine the impact of extraction parameters on yields and compositions of pectins extracted from chicory roots (Chicorium intybus L.).

Chicory root pectin was isolated by acid extraction followed by alcohol precipitation. Because the extraction conditions have important effects on the features of pectins, an experimental design was used to study the influence of 17 different extraction parameters on yield and composition of pectin: pH, temperature, time of extraction, solid/liquid ratio, and different pretreatments of the pulps before extraction. Twenty extractions were conducted and examined for their significance on yield and sugar content using the Plackett-Burman factorial design. The acid extraction of chicory roots resulted in an average yield of 11% containing 86% of sugars. It was found that extraction temperature, time, protease pretreatment, water purity, and water washing of pulps significantly affected yield and pectin composition with an increase of yield and purity of pectin in harsher extraction conditions.

Chemical Precipitation↗
PubMed1998

An investigation into the suitability of amidated pectin hydrogel beads as a delivery matrix for chloroquine.

The aim of the present study was to delay the release of chloroquine to distal parts of the gastrointestinal tract by using a multiparticulate hydrogel formulation. Amidated pectin chloroquine beads (PC) with varying pectin-to-chloroquine ratios (PC) w/w loadings of 4:1, 2:1, and 1:1 in the dried beads were prepared by the gelation of drug-loaded pectin solutions in the presence of calcium. In vitro release studies of chloroquine from pectin-chloroquine hydrogel beads and chloroquine diphosphate powder were carried out in simulated gastric and intestinal fluids. The total release of the entrapped chloroquine from the hydrogel beads was achieved between 4 and 7 h in simulated intestinal fluid, but total release was not achieved in simulated gastric fluid. However, total release from chloroquine diphosphate powder was achieved by 1.5 and 2 h in gastric and intestinal fluids, respectively. The plasma pharmacokinetics of chloroquine from pectin hydrogel beads and chloroquine diphosphate solution following single or repeated dosing were compared in male Sprague-Dawley rats over a period of 60 h. Oral administration of the hyrogel beads to rats produced maximum plasma concentrations by 7 h, but highest plasma concentrations following chloroquine solution administration were observed by 2 h. The dissolution data and appearance of significant plasma concentrations of chloroquine 2 to 4 h after oral administration suggests release in duodenum, jejunum, or ileum.

Animals↗
PubMed2004

Green banana and pectin improve small intestinal permeability and reduce fluid loss in Bangladeshi children with persistent diarrhea.

To evaluate the effects of green banana and pectin (nondigestible, dietary sources of colonic shortchain fatty acids [SCFA]) on intestinal permeability, 57 boys (5-12 months) with persistent diarrhea (> or = 14 days) were given a week's treatment with a rice-based diet containing either cooked green banana (n = 19), pectin (n = 17), or rice diet alone (n = 21). Intestinal permeability was assessed before and after treatment by giving a lactulose-mannitol (LM) drink and measuring urinary recovery after 5 hr. Treatment with banana significantly (P < 0.05) reduced lactulose recovery, increased mannitol recovery, and decreased the LM ratio, indicating improvement of permeability. Pectin produced similar results. Permeability changes were associated with a 50% reduction in stool weights which correlated strongly (green banana, r2 = 0.84, pectin, r2 = 0.86) with the LM ratio. Green banana-derived and SCFA-mediated stimulation of colonic as well as small bowel absorption is responsible for their antidiarrheal effects. The antidiarrheal effects of green banana and pectin are mediated by improvement of small intestinal permeability in addition to their known colonotrophic effects.

Antidiarrheals↗
PubMed2003

Dietary pectin and calcium inhibit colonic proliferation in vivo by differing mechanisms.

Diet plays an important role in promoting and/or preventing colon cancer; however, the effects of specific nutrients remain uncertain because of the difficulties in correlating epidemiological and basic observations. Transmissible murine colonic hyperplasia (TMCH) induced by Citrobacter rodentium, causes significant hyperproliferation and hyperplasia in the mouse distal colon and increases the risk of subsequent neoplasia. We have recently shown that TMCH is associated with an increased abundance of cellular beta-catenin and its nuclear translocation coupled with up-regulation of its downstream targets, c-myc and cyclin D1. In this study, we examined the effects of two putatively protective nutrients, calcium and soluble fibre pectin, on molecular events linked to proliferation in the colonic epithelium during TMCH. Dietary intervention incorporating changes in calcium [high (1.0%) and low (0.1%)] and alterations in fibre content (6% pectin and fibre-free) were compared with the standard AIN-93 diet (0.5% calcium, 5% cellulose), followed by histomorphometry and immunochemical assessment of potential oncogenes. Dietary interventions did not alter the time course of Citrobacter infection. Both 1.0% calcium and 6% pectin diet inhibited increases in proliferation and crypt length typically seen in TMCH. Neither the low calcium nor fibre-free diets had significant effect. Pectin diet blocked increases in cellular beta-catenin, cyclin D1 and c-myc levels associated with TMCH by 70%, whereas neither high nor low calcium diet had significant effect on these molecules. Diets supplemented with either calcium or pectin therefore, exert anti-proliferative effects in mouse distal colon involving different molecular pathways. TMCH is thus a diet-sensitive model for examining the effect of specific nutrients on molecular characteristics of the pre-neoplastic colonic epithelium.

Adhesins, Bacterial↗
PubMed1982

Dietary fiber and cholesterol and bile acid metabolisms in axenic (germfree) and holoxenic (conventional) rats. II. Effect of pectin.

Axenic and holoxenic rats were fed with a semi-synthetic diet containing 5 p. 100 pectin as the only fiber. Although the microbial flora of the digestive tract converted most of the bile acids in holoxenic rats, it hardly changed the other characteristics of cholesterol and bile acid metabolisms, except intestinal bile salt pools which were much larger in the axenic rats. When the pectin-containing and pectin-free diets were compared, it appeared that the former diet increased cecal weight, especially in axenic rats, but slightly modified cholesterol and bile acid metabolisms. However, the values of some characteristics of those metabolisms varied individually in the holoxenic rat fed with the pectin-containing diet, while they were very homogeneous in the other groups. This heterogeneity might result from pectin-digestive tract microbial flora interactions which would vary among individuals.

Aging↗
PubMed1985

Dietary fiber and cholesterol and bile acid metabolism in axenic (germfree) and holoxenic (conventional) rats. III. Effect of non-sterilized pectin.

Axenic (germfree) and holoxenic (conventional) rats were given a pectin-containing diet (5%) or a pectin-free diet. The diet was not sterilized and the axenic state was maintained by the addition of antibiotics. Pectin modified little or not at all the quantity of bile acids in the small intestine, fecal bile acid excretion and fecal elimination of the sum of cholesterol and bile acids. It similarly decreased the concentration of liver cholesterol and the amount of bile acids in the cecum and large intestine of both germfree and conventional rats. Pectin decreased the absorption coefficient of dietary cholesterol and its plasma concentration and increased fecal cholesterol elimination in conventional rats but not in germfree animals. The data imply that some of the actions of pectin depend on the presence of the intestinal flora but the exact nature of this relationship is unclear.

Absorption↗
PubMed2001

Clinical studies in persistent diarrhea: dietary management with green banana or pectin in Bangladeshi children.

BACKGROUND & AIMS: Because of the beneficial intestinal effects of dietary fibers, we have evaluated the therapeutic effects of green banana or pectin in children with persistent diarrhea. METHODS: In a double-blind trial, 62 boys, age 5-12 months, were randomly given a rice-based diet containing either 250 g/L of cooked green banana (n = 22) or 4 g/kg pectin (n = 19) or the rice-diet alone (control, n = 21), providing 54 kcal/dL daily for 7 days. Stool weight and consistency, frequency of vomiting and purging, and duration of illness were measured. RESULTS: Most children (60%) had no pathogens isolated from stools, 17% had rotavirus, 5% Vibrio cholerae, 4% Salmonella group B, and 11% had enterotoxigenic Escherichia coli infections. By day 3 posttreatment, significantly (P < 0.001) more children recovered from diarrhea receiving pectin or banana than controls (59%, 55%, and 15%, respectively). By day 4, these proportions correspondingly increased to 82%, 78%, and 23%, respectively, the study diet groups being significantly (P < 0.001) different than controls. Green banana and pectin significantly (P < 0.05) reduced amounts of stool, oral rehydration solution, intravenous fluid, and numbers of vomiting, and diarrheal duration. CONCLUSIONS: Green banana and pectin are useful in the dietary management of persistent diarrhea in hospitalized children and may also be useful to treat children at home.

Antidiarrheals↗
PubMed1979

The effect of pectin on the structure and function of the rat small intestine.

1. The effect of pectin on the structure and function of the rat small intestine was compared with that of a standard pellet diet and of a fibre-free basal diet. 2. The length and wet weight of the small bowel was significantly greater inpect in-fed rats than in either pellet- or basal-diet-fed rats. 3. Histological measurements of longitudinal sections from the small bowel showed a significantly greater crypt depth and muscle layer thickness in the mid-jejunum and ileum of the pectin fed rats. Villous height showed less variation. 4. The specific activity of alkaline phosphatase (EC 3.1.3.1) and leucyl-beta-naphthylamidase (EC 3.4.11.1) in mucosal scrapings was significantly lower in the upper jejunum of pectin-fed rats compared with either of the other dietary groups. The differences were not so marked in mid-jejunum or ileum. 5. Glucose absorption measured in vivo from jejunal and ileal loops was similar in all three dietary groups. 6. With two minor exceptions there were no significant differences in any of these measurements between the pellet- and basal-diet-fed rats. 7. These findings could be explained by increased epithelial cell turnover caused by pectin. The possible mechanisms of this are discussed. 8. The effect of pectin on the human small bowel requires study before it can be widely prescribed in man.

Alkaline Phosphatase↗
PubMed1982

Comparison of the effects of high- and low-methoxyl pectins on blood and faecal lipids in man.

The effects on blood and faecal lipids of the addition of 15 g of either high- or low-methoxyl pectin to the habitual diets of ten healthy young adults have been studied. 2. Serum total cholesterol levels were reduced by a mean of 16% during consumption of low-methoxyl pectin and 18% during consumption of high-methoxyl pectin. High density lipoprotein cholesterol levels and triglyceride levels were unchanged. 3. There was no difference in faecal fat and steroid excretion between the two pectins. 4. The results suggest that it is the gel-forming properties of the pectins which are important in the cholesterol-lowering effect rather than differences in bile acid binding due to different methoxyl contents.

Adult↗