Simulated Colonic Conditions Research Articles

Structural, physicochemical, and in vitro digestion properties of microgel-reinforced synbiotic hydrogel beads filled with pectic oligosaccharides as a delivery system for Limosilactobacillus reuteri

Pea protein microgel (MG)-reinforced synbiotic low methoxyl pectin (LMP) hydrogel beads filled with different concentrations (0 %, 0.2 %, and 0.4 %) of pectic oligosaccharides (POS) were developed as delivery system for Limosilactobacillus reuteri (L. reuteri). SEM results revealed that incorporating POS into the hydrogel beads made the gel matrix smoother and more compact, reducing probiotic leakage and higher encapsulation efficiency. FT-IR analysis observed new ionic crosslinking between LMP and calcium ions. In vitro digestion results suggested that MG-reinforced synbiotic hydrogel beads showed higher survival rates throughout upper gastrointestinal tract than MG, and the highest values were observed in the hydrogel beads with 0.4 % of POS. Most L. reuteri was released from the developed system after exposure to simulated colonic conditions for 48 h. MG-reinforced synbiotic hydrogel beads showed higher thermal and storage stability than MG alone, indicating that adding hydrogel bead layer to MG can efficiently protect L. reuteri from environmental stresses.

Screening, characterization and growth of γ-aminobutyric acid-producing probiotic candidates from food origin under simulated colonic conditions.

This study aims to isolate probiotic bacteria candidates from various starter cultures and fermented foods and characterize their ability to produce γ-aminobutyric acid (GABA). GABA is a major inhibitory neuromediator of the central and enteric nervous systems with a role in several health disorders. Fourteen strains of lactic acid bacteria were isolated from food environment and screened for the presence of the glutamate decarboxylase (gadB) gene using PCR and GAD enzymatic assay. The identified potent GABA-producers included Strep. thermophilus, Lactiplantibacillus plantarum and Lact. delbrueckii subsp. bulgaricus. GC-FID analyses confirmed the high GABA production capacity of Strep. thermophilus ST16 (1641.5 ± 154.15 μmol l-1 ), Strep. thermophilus ST8 (1724.5 ± 48.08 μmol/L). To a lesser extent, Bif. animalis ST20, Lact. acidophilus LP16-2 and Ent. faecium ST3 produced 947.5 ± 70.71, 918.0 ± 121.42, and 907.83 ± 55.15 μmol/L of GABA, respectively. These potent strains were able to grow and produce GABA in MRS broth and pre-fermented Macfarlane broth, the latter medium mimicking the nutrient and metabolome composition encountered in the colon. The identified bioactive strains exhibited strong biological safety and probiotic potential profiles as indicated by sensitivity to antibiotics, absence of virulence factors and survival in gastrointestinal conditions. Several GABA producing probiotic candidates, including Bif. animals ST20, Strep. thermophilus ST8, Lact. acidophilus LP16-2, L. plantarum LP6 & LP9, and Ent. faecium ST3, have shown potential to grow under simulated colonic conditions. Findings from this study provide evidence of the suitability of the isolated GABA-producing probiotic candidates for the development of health-oriented functional food products.

PH-Responsive Alginate-Based Microparticles for Colon-Targeted Delivery of Pure Cyclosporine A Crystals to Treat Ulcerative Colitis.

Cyclosporine A (CsA) is a potent immunosuppressant for treating ulcerative colitis (UC). However, owing to severe systemic side effects, CsA application in UC therapy remains limited. Herein, a colon-targeted drug delivery system consisting of CsA crystals (CsAc)-loaded, Eudragit S 100 (ES)-coated alginate microparticles (CsAc-EAMPs) was established to minimize systemic side effects and enhance the therapeutic efficacy of CsA. Homogeneously-sized CsAs (3.1 ± 0.9 μm) were prepared by anti-solvent precipitation, followed by the fabrication of 47.1 ± 6.5 μm-sized CsAc-EAMPs via ionic gelation and ES coating. CsAc-EAMPs exhibited a high drug loading capacity (48 ± 5%) and a CsA encapsulation efficacy of 77 ± 9%. The in vitro drug release study revealed that CsA release from CsAc-EAMPs was suppressed under conditions simulating the stomach and small intestine, resulting in minimized systemic absorption and side effects. Following exposure to the simulated colon conditions, along with ES dissolution and disintegration of alginate microparticles, CsA was released from CsAc-EAMPs, exhibiting a sustained-release profile for up to 24 h after administration. Given the effective colonic delivery of CsA molecules, CsAc-EAMPs conferred enhanced anti-inflammatory activity in mouse model of dextran sulfate sodium (DSS)-induced colitis. These findings suggest that CsAc-EAMPs is a promising drug delivery system for treating UC.

Encapsulation of bifidobacterium in alginate microgels improves viability and targeted gut release

Biopolymer microgels were designed to encapsulate and protect probiotics during storage and passage through the upper human gastrointestinal tract (GIT), but then release them in the colon. An anaerobic probiotic strain (Bifidobacterium pseudocatenulatum G7; BPG7) was encapsulated within calcium alginate microgels. In some cases, either colloidal antacid (CaCO3) or colloidal antacid and nanoemulsion (nE) lipid droplets were co-encapsulated with the probiotics. These additives were used to control the porosity and/or internal pH of the microgels. Initially, the viability of free and encapsulated probiotics was evaluated when they were stored at 4 °C for 28 days. The free probiotics rapidly degraded during storage.Encapsulation greatly improved the stability of the probiotics, with the effectiveness depending on the formulation: antacid-microgels > control microgels > antacid-nE-microgels. These effects were mainly attributed to the ability of the colloidal CaCO3 particles to inhibit molecular diffusion processes. The ability of the microgels to protect the probiotics under simulated gastrointestinal tract (GIT) conditions was then assessed. The free probiotics were completely inactivated when exposed to gastric and small intestine conditions. In contrast, the antacid- and antacid-nE-microgels were highly effective at improving the viability of the probiotics during passage through the upper GIT. Moreover, these microgels were fermented under simulated colonic conditions, thereby releasing the probiotics. These results suggest that antacid-loaded calcium alginate microgels can be used for the encapsulation, protection, and colonic delivery of probiotics. Nevertheless, further studies are required using in vivo models.

In vitro gastrointestinal digestion and simulated colonic fermentation of pistachio nuts determine the bioaccessibility and biosynthesis of chronobiotics.

Chronodisruption leads to obesity and other metabolic disorders that can be alleviated by food-derived potential chronobiotics, such as phytomelatonin (PMT), phenolic compounds (PCs) and dietary fiber rich pistachios. Pistachios with (PN + SC) or without (PN) the seed coat were investigated for their in vitro chronobiotic potential since they are one of the main reported PMT sources. Consequently we evaluated the bioaccessibility, permeability, and biosynthesis of pistachio chronobiotics, particularly PMT, during gastrointestinal and colonic fermentation. The maximum in vitro bioaccessibility and apparent permeability (efflux-prone) of PCs, flavonoids and PMT were sample-specific [∼1.3% (both), 27 and 3.4% (PN + SC)], but additional amounts (flavonoids > PCs > PMT) were released under simulated colonic conditions. Short-chain fatty acids (SCFAs; 38 mM; >50% butyrate, PN + SC > PN) and some metabolites (e.g., indole, benzaldehyde, phenolic acids, and aliphatic/aromatic hydrocarbons) were detected depending on the sample. The predominant pistachio butyrate production during in vitro colonic fermentation can improve chronodisruption and benefit obese individuals. Pistachio's digestion increases the bioaccessibility and intestinal permeability of potential chronobiotics (PMT and PCs) and the biosynthesis of colonic metabolites (SCFAs, among others) also with chronobiotic potential.

Hydrophobic agave fructans for sustained drug delivery to the human colon

Given their glycosidic β 2−1 and β 2−6 linkages, fructans from Agave tequilana Weber var. azul (AtF) may be employed for the design of drug carriers targeting the human colon. However, the high water solubility of AtF prevents their use for such a purpose. In this work, AtF were esterified with acetyl, lauroyl and palmitoyl groups with the aim to encapsulate ibuprofen as a model drug and characterize its enzymatic release in simulated colon conditions. It was found that efficiency of encapsulation increased from 0.8% (unmodified fructan) to 17 or 21.5% when AtF was esterified with acetyl groups at high degree of substitution (2.75 DS) or with a long acyl chain such as palmitoyl at low DS (0.18) respectively. Hydrophilic fructan based microspheres (AtF, and lauroyl fructan, 46 and 61.3° contact angle respectively) had poor encapsulation efficiency (0.8–1.5%) and lost most of their cargo (85%) at gastric conditions. In contrast, hydrophobic fructan based microspheres (acetyl and palmytoyl, 91–98° contact angle) showed high stability at gastric pH and were able to release the drug for long periods. These characteristics make hydrophobic fructans appropriate vehicles that show great potential for the delivery of drugs to the colon, allowing long drug bioavailability during its delivery and release.

Bile-induced promoters for gene expression in Lactobacillus strains.

Bioengineering of probiotics allows the improvement of their beneficial characteristics. In this work, we develop a molecular tool that would allow the activation of desirable traits in probiotics once they reach the intestine. The activity of upstream regions of bile-inducible genes of Lactobacillus casei BL23 and Lactobacillus plantarum WCFS1 was analyzed using plasmids encoding an anaerobic fluorescent protein as reporter. The promoter P16090 from Lb. casei BL23 was selected and its bile induction confirmed in Lb. casei BL23, Lb. plantarum WCFS1, and in Lactobacillus rhamnosus and Lactobacillus reuteri strains. However, the induction did not occur in Lactococcus lactis MG1363 or Bifidobacterium strains. Studies with different bile compounds revealed the importance of cholic acid in the bile induction process. Induction of fluorescence was also confirmed for transformed Lb. casei BL23 under simulated colonic conditions and in the presence of intestinal microbiota. The developed vector, pNZ:16090-aFP, constitutes a promising tool suitable for the expression of genes of interest under intestinal conditions in probiotic strains of the species Lb. casei, Lb. plantarum, Lb. rhamnosus, and Lb. reuteri.

Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release.

In the present work, we demonstrate the preparation of chitosan-based composites as vehicles of the natural occurring multi-drug resveratrol (RES). Such systems are endowed with potential therapeutic effects on inflammatory bowel diseases (IBD), such as Crohn’s disease (CD) and ulcerative colitis, through the sustained colonic release of RES from long-lasting mucoadhesive drug depots. The loading of RES into nanoparticles (NPs) was optimized regarding two independent variables: RES/polymer ratio, and temperature. Twenty experiments were carried out and a Box–Behnken experimental design was used to evaluate the significance of these independent variables related to encapsulation efficiency (EE). The enhanced RES EE values were achieved in 24 h at 39 °C and at RES/polymer ratio of 0.75:1 w/w. Sizes and polydispersities of the optimized NPs were studied by dynamic light scattering (DLS). Chitosan (CTS) dispersions containing the RES-loaded NPs were ionically gelled with tricarballylic acid to yield CTS-NPs composites. Macro- and microscopic features (morphology and porosity studied by SEM and spreadability), thermal stability (studied by TGA), and release kinetics of the RES-loaded CTS-NPs were investigated. Release patterns in simulated colon conditions for 48 h displayed significant differences between the NPs (final cumulative drug release: 79–81%), and the CTS-NPs composites (29–34%).

In vitro drug release from acetylated high amylose starch-zein films for oral colon-specific drug delivery

This study describes the preparation of free films of zein with and without acetylated high amylose maize starch (HAS) and their corresponding coated tablets as a novel approach to colonic drug delivery. We hypothesise that the embedding of a digestible starch component within the inert zein would allow the film to remain intact until the large intestine is reached. Free films of zein alone and starch/zein were prepared and characterized. SEM and AFM images of film surface showed that films were morphologically inhomogeneous, particularly at lower HAS/Zein ratios; however, nanothermal analysis data suggested that these differences in appearance within the same film are not compositional differences. Moreover, FT-IR could detect no molecular interaction between the two polymers. Paracetamol tablets were coated with HAS/Zein aqueous based coatings of different compositions to a TWG of 20%. Drug release from zein alone and 1:5 HAS/Zein coated tablets under upper gastrointestinal conditions (pH 1.2, pH 6.8 with pepsin and pancreatin included) was very similar (for example approximately 12% and 14% of the drug was released, respectively, after 6 h in a sequential in vitro test), suggesting that release in this region is limited and is not influenced by the presence of HAS in the ratio to zein under study. Studies using an in vitro colon model showed that under simulated colonic conditions, the drug release was significantly (p < 0.05) more rapid from 1:5 HAS/Zein, compared to the zein alone coating formulation. These data therefore support the potential use of zein-starch mixed films for colonic targeting purposes.

Colonic fermentation of polyphenols from Chilean currants (Ribes spp.) and its effect on antioxidant capacity and metabolic syndrome-associated enzymes

The Chilean wild currants Ribes magellanicum and R. punctatum are a good source of polyphenols. Polyphenolic-enriched extracts (PEEs) from both species were submitted to in vitro colonic fermentation to assess the changes in phenolic composition, antioxidant capacity and inhibition of metabolic syndrome-associated enzymes. The phenolic profiles of the fermented samples showed significant changes after 24 h incubation. Nine metabolites, derived from the microbial fermentation, were tentatively identified, including dihydrocaffeic acid, dihydrocaffeoyl-, dihydroferuloylquinic acid, 1-(3,4-dihydroxyphenyl)-3-(2,4,6-trihydroxyphenyl)propan-2-ol (3,4-diHPP-2-ol), among others. The content of anthocyanins and hydroxycinnamic acids was most affected by simulated colonic conditions, with a loss of 71–92% and 90–100% after 24 h incubation, respectively. The highest antioxidant capacity values (ORAC) were reached after 8 h incubation. The inhibitory activity against the enzyme α-glucosidase was maintained after the fermentation process. Our results show that simulated colonic fermentation exerts significant changes on the polyphenolic composition of these berries, modifying their health-promoting properties.

Optimizing Prednisolone Loading into Distiller's Dried Grain Kafirin Microparticles, and In vitro Release for Oral Delivery.

Kafirin microparticles have potential as colon-targeted delivery systems because of their ability to protect encapsulated material from digestive processes of the upper gastrointestinal tract (GIT). The aim was to optimize prednisolone loading into kafirin microparticles, and investigate their potential as an oral delivery system. Response surface methodology (RSM) was used to predict the optimal formulation of prednisolone loaded microparticles. Prednisolone release from the microparticles was measured in simulated conditions of the GIT. The RSM models were inadequate for predicting the relationship between starting quantities of kafirin and prednisolone, and prednisolone loading into microparticles. Compared to prednisolone released in the simulated gastric and small intestinal conditions, no additional drug release was observed in simulated colonic conditions. Hence, more insight into factors affecting drug loading into kafirin microparticles is required to improve the robustness of the RSM model. This present method of formulating prednisolone-loaded kafirin microparticles is unlikely to offer clinical benefits over commercially available dosage forms. Nevertheless, the overall amount of prednisolone released from the kafirin microparticles in conditions simulating the human GIT demonstrates their ability to prevent the release of entrapped core material. Further work developing the formulation methods may result in a delivery system that targets the lower GIT.

Analysis of microsamples of human faeces: a non-invasive approach to study the bioavailability of fat-soluble bioactive compounds.

Bioavailability is a critical feature in the assessment of the role of micronutrients in human health. Poorly bioavailable micronutrients like carotenoids may reach significant concentrations in the gastrointestinal tract where they may exert biological actions. We evaluated a simple collection protocol to determine vitamin A, E and carotenoids in microsamples of human faeces as a non-invasive approach for nutritional studies. Microsamples of human faeces were collected using a commercially available device, extracted and analysed on two LC systems. Suitability of the protocol was assessed by evaluating several factors including the effect of simulated colonic conditions and two nutritional scenarios with different dietary components, chemical forms, nutritional goals and target groups. The protocol was reproducible and representative of a faeces sample. The major dietary and serum carotenoids, and several "unidentified" compounds (possibly metabolites) could be detected, and cis-/trans-β-carotene profile reflected dietary intervention. In faeces of neonates, free retinol, retinyl and α-tocopheryl acetate (from infant formula), long-chain fatty acid retinyl esters (from human milk), free γ-tocopherol and α-tocopherol could be detected. Our results show that the analysis of vitamin A, E and carotenoids in microsamples of human faeces is a suitable, non-invasive approach that may provide relevant information regarding responsiveness, nutrient stability and metabolism and may help assess adequacy of chemical forms and delivery systems reaching the colon.

Using Nanoparticle Tracking Analysis (NTA) to Decipher Mucoadhesion Propensity of Curcumin-Containing Chitosan Nanoparticles and Curcumin Release

Real-time nanoparticle tracking analysis (NTA) was used to evaluate the propensity of curcumin-containing chitosan nanoparticles (CUR-CS-NP) to muco adhere and release curcumin under simulated colon conditions. This novel procedure is relatively simple and fast and does not require use of animals, but more importantly, it permits the correlation of physical changes to the CUR-CS-NP with the observed behavior under simulated conditions in realtime. The CUR-CS-NP formed spontaneous aggregates in response to exposure to mucin. This observation correlated with curcumin release from CUR-CS-NP was observed in phosphate buffer (pH 7.4) where, 81% of curcumin was released within 6 hours. Atomic force microscopy imaging CUR-CS-NP exposed to mucin solution revealed a decorated surface of the CUR-CS-NP by mucin, consistent with expected electrostatic interactions between the two. The use of NTA, thus, provided us with a means of ascertaining the performance of the CUR-CS-NP under simulated colonic conditions and we propose that this prototype delivery system could be the basis for an effective colon mucoadhesive drug delivery system.

Growth, acid production and bacteriocin production by probiotic candidates under simulated colonic conditions

The aim of this study is to evaluate the capacity of three bacteriocin producers, namely Lactococcus lactis subsp. lactis biovar diacetylactis UL719 (nisin Z producer), L. lactis ATCC 11454 (nisin A producer) and Pediococcus acidilactici UL5 (pediocin PA-1 producer), and to grow and produce their active bacteriocins in Macfarlane broth, which mimics the nutrient composition encountered in the human large intestine. The three bacteriocin-producing strains were grown in Macfarlane broth and in De Man-Rogosa-Sharpe (MRS) broth. For each strain, the bacterial count, pH drop and production of organic acids and bacteriocins were measured for different period of time. The ability of the probiotic candidates to inhibit Listeria ivanovii HPB 28 in co-culture in Macfarlane broth was also examined. Lactococcus lactis subsp. lactis biovar diacetylactis UL719, L. lactis ATCC 11454 and Ped. acidilactici UL5 were able to grow and produce their bacteriocins in MRS broth and in Macfarlane broth. Each of the three candidates inhibited L. ivanovii HPB 28, and this inhibition activity was correlated with bacteriocin production. The role of bacteriocin production in the inhibition of L. ivanovii in Macfarlane broth was confirmed for Ped. acidilactici UL5 using a pediocin nonproducer mutant. The data provide some evidence that these bacteria can produce bacteriocins in a complex medium with carbon source similar to those found in the colon. This study demonstrates the capacity of lactic acid bacteria to produce their bacteriocins in a medium simulating the nutrient composition of the large intestine.

A novel and green biomaterial based silver nanocomposite hydrogel: Synthesis, characterization and antibacterial effect

In the present study, we report a facile and eco-friendly method for the preparation of a novel silver nanocomposite hydrogel (SNH) based on poly(acrylic acid) (PAA) grafted onto salep as a water soluble polysaccharide backbone. The presence of inorganic silver nanoparticles (nano-Ag) in the hydrogel was confirmed by thermo-gravimetric (TG) analysis. The TEM images illustrated the presence of embedded nano-Ag throughout the hydrogel matrix. In addition, the transmission electron microscopy (TEM) images showed that the formed nano-Ag had an average particle size of 5–10nm. The potential of obtained SNH was examined for Tetracycline hydrochloride (TH) release in simulated colon conditions. Lastly, the in vitro antibacterial properties of the obtained optimum sample were successfully evaluated against gram-negative and gram-positive bacteria.

Characterizing permeability and stability of microcapsules for controlled drug delivery by dynamic NMR microscopy

Microscopic capsules made from polysaccharides are used as carriers for drugs and food additives. Here, we use NMR microscopy to assess the permeability of capsule membranes and their stability under different environmental conditions. The results allow us to determine the suitability of different capsules for controlled drug delivery. As a measure of the membrane permeability, we monitor the diffusion of paramagnetic molecules into the microcapsules by dynamic NMR microimaging. We obtained the diffusion coefficients of the probe molecules in the membranes and in the capsule core by comparing the measured time dependent concentration maps with numerical solutions of the diffusion equation. The results reveal that external coatings strongly decrease the permeability of the capsules. In addition, we also visualized that the capsules are stable under gastric conditions but dissolve under simulated colonic conditions, as required for targeted drug delivery. Depending on the capsule, the timescales for these processes range from 1 to 28h.

In vitro and in vivo release properties of colon-specific prodrug of indomethacin

Objective To explore in vitro and in vivo release properties of indomethacin-block-amyloses (IDM-Am-I-6) microbially triggered. Methods In vitro dissolution of IDM-Am-1-6 was employed under simulated gastric (pH 1.2, 4 h), small intestinal (pH 6.8, 1% porcine pancreatin, 6 h), and colonic conditions (pH 7.2, faecal bacteria, 36 h), and accumulative release was determined by ultraviolet spectrophotometer. Sprague-Dawley rats were orally administered with IDM (3 mg/kg) and IDM-Am-3 respectively. IDM concentrations in peripheral blood and portal vein were determined by HPLC, and then pharmacokinetic parameters were calculated with compartment model. Results IDM-Am-3 was degraded 1.3%, 9.3% and 95.3% respectively in simulated gastric fluid for 4 h, small intestine for 6 h, and colon for 36 h, respectively. In vivo experiment of IDM-Am-3 showed that absorption was delayed obviously (P < 0.01), peak time (11.35±2.45) h, ehmination half-life (16.74±4.04) h and mean residence time (22.27 ± 0. 52) h were significantly prolonged (P < 0.01 ), as well as peak serum concentrations (9.69 ± 2.40) mg/L and AUC_(0-t) (236.7 ± 13.1 ) mg/L × h were decreased markedly (P < 0.01 ) as com-pared with those of IDM regarding to portal vein. Also, AUC_(0-t) of IDM-Am-3 in peripheral blood was re-markably lower than that in portal vein (P <0. 01 ). Conclusion IDM-Am-3 could target IDM specifically to colon and simultaneously possessed advantage of sustained release in portal vein. Key words: Indomethacin; Drug delivery systems; Pharmacokinetics

Pectin-based microspheres for colon-specific delivery of vancomycin

Abstract Objectives The aim of this study was to describe a colon-specific delivery system based on pectin hydrogels formed by complexation with chitosan. Methods Hydrogels were prepared at different weight ratios (4: 1, 7: 1, 10: 1; pectin/chitosan), loaded with vancomycin hydrochloride (2: 1, 4: 1; polymer/drug weight ratio) and collected by spray-drying. The microspheres obtained were characterized in terms of morphology, swelling behaviour, mucoadhesive properties and drug loading efficiency. The influence of different pectin/chitosan hydrogels on the release behaviour of microspheres at pH 2.0, 5.5 and 7.4 were evaluated in vitro with and without pectinolytic enzyme. Key findings The results showed that water uptake was increased by raising the environmental pH (from 2.0 to 7.4) and the pectin/chitosan weight ratio, while drug availability was increased by raising the environmental pH (from 2.0 to 7.4) and decreased by raising the pectin/chitosan weight ratio. In the presence of pectinase, the glycoside bonds of pectin were degraded and a considerable amount of drug was released in a short time. Conclusions This study suggested that pectin/chitosan microspheres were able to limit the release of vancomycin under acidic conditions and release it under simulated colonic conditions, confirming their potential for a colon-specific drug delivery system.

Pectin-based microspheres for colon-specific delivery of vancomycin

The aim of this study was to describe a colon-specific delivery system based on pectin hydrogels formed by complexation with chitosan. Hydrogels were prepared at different weight ratios (4:1, 7:1, 10:1; pectin/chitosan), loaded with vancomycin hydrochloride (2:1, 4:1; polymer/drug weight ratio) and collected by spray-drying. The microspheres obtained were characterized in terms of morphology, swelling behaviour, mucoadhesive properties and drug loading efficiency. The influence of different pectin/chitosan hydrogels on the release behaviour of microspheres at pH 2.0, 5.5 and 7.4 were evaluated in vitro with and without pectinolytic enzyme. The results showed that water uptake was increased by raising the environmental pH (from 2.0 to 7.4) and the pectin/chitosan weight ratio, while drug availability was increased by raising the environmental pH (from 2.0 to 7.4) and decreased by raising the pectin/chitosan weight ratio. In the presence of pectinase, the glycoside bonds of pectin were degraded and a considerable amount of drug was released in a short time. This study suggested that pectin/chitosan microspheres were able to limit the release of vancomycin under acidic conditions and release it under simulated colonic conditions, confirming their potential for a colon-specific drug delivery system.

Design and development of mixed film of pectin: ethyl cellulose for colon specific drug delivery of sennosides and triphala.

The present study was aimed at developing colon specific drug delivery system for sennosides and Triphala. These drugs are reputed Ayurvedic medicines for constipation in India. The proposed device explored the application of pectin and ethyl cellulose as a mixed film for colon specific delivery. This mixed film was prepared using non-aqueous solvents like acetone and isopropyl alcohol. A 32 factorial design was adopted to optimize the formulation variables like, ratio of ethyl cellulose to pectin (X1) and coat weight (X2). The rate and extent of drug release were found to be related to the thickness and the ratio of pectin to ethyl cellulose within the film. Statistical treatments to the drug release data revealed that the X1 variable was more important than X2. Under simulated colonic conditions, drug release was more pronounced from coating formulations containing higher proportions of pectin. The surface of the device was coated with Eudragit S100 to ensure that the device was more pH dependent and trigger the drug release only at higher pH. The final product is expected to have the advantage of being biodegradable and pH dependant. This type of a film effectively releases the drug while maintaining its integrity.