Release Of 5-aminosalicylic Acid Research Articles

Sustained release of 5-aminosalicylic acid from azoreductase-responsive polymeric prodrugs for prolonged colon-targeted colitis therapy

Ulcerative colitis (UC) is a challenging inflammatory gastrointestinal disorder, whose therapies encounter limitations in overcoming insufficient colonic retention and rapid systemic clearance. In this study, we report an innovative polymeric prodrug nanoformulation for targeted UC treatment through sustained 5-aminosalicylic acid (5-ASA) delivery. Amphiphilic polymer-based 13.5 nm micelles were engineered to incorporate azo-linked 5-ASA prodrug motifs, enabling cleavage via colonic azoreductases. In vitro, micelles exhibited excellent stability under gastric/intestinal conditions while demonstrating controlled 5-ASA release over 24 h in colonic fluids. Orally administered micelles revealed prolonged 24-h retention and a high accumulation within inflamed murine colonic tissue. At an approximately 60% dose reduction from those most advanced recent studies, the platform halted DSS colitis progression and outperformed standard 5-ASA therapy through a 77–97% suppression of inflammatory markers. Histological analysis confirmed intact colon morphology and restored barrier protein expression. This integrated prodrug nanoformulation addresses limitations in colon-targeted UC therapy through localized bioactivation and tailored pharmacokinetics, suggesting the potential of nanotechnology-guided precision delivery to transform disease management.

Mechanistic Investigation of Enzyme Triggered Release from a Xyloglucan Matrix Tablet for Controlled Colonic Drug Delivery

The objective of this study was to investigate the mechanisms underlying drug release from a controlled colonic release (CCR) tablet formulation based on a xyloglucan polysaccharide matrix and identify the factors that control the rate of release for the purpose of fundamentally substantiating the concept and demonstrating its robustness for colonic drug delivery. Previous work demonstrated in vitro limited release of 5-aminosalicylic acid (5-ASA) and caffeine from these tablets in small intestinal environment and significant acceleration of release by xyloglucanase, an enzyme of the colonic microbiome. Targeted colonic drug delivery was verified in an animal study in vivo. In the present work, interaction of the xyloglucan matrix tablets with aqueous dissolution media containing xyloglucanase was found to lead to the spontaneous formation of a hydrated highly viscous gummy layer at the surface of the matrix which had a reduced drug content compared to the underlying regions and persisted with a nearly constant thickness that was inversely correlated to the enzyme concentration throughout the duration of the release process. Enzymatic hydrolysis of xyloglucan was determined to take place at the surface of the matrix leading to matrix erosion and a relation for the rate of enzymatic reaction as a function of bulk enzyme concentration and the concentration of dissolved xyloglucan in the gummy layer was derived. A mathematical model was developed encompassing aqueous medium ingress, matrix metamorphosis due to xyloglucan dissolution and matrix swelling, enzymatic hydrolysis of the polysaccharide and concomitant drug release due to matrix erosion and simultaneous drug diffusion. The model was fitted to data of reducing sugar equivalents in the medium reflecting matrix erosion and released drug amount. Enzymatic reaction parameters and reasonable values of medium ingress velocity, xyloglucan dissolution rate constant and drug diffusion coefficient were deduced that provided an adequate approximation of the data. Erosion was shown to be the overwhelmingly dominant drug release mechanism while the role of diffusion marginally increased at low enzyme concentration and high drug solubility. Changing enzyme concentration had a rather weak effect on matrix erosion and drug release rate as demonstrated by model simulations supported by experimental data, while xyloglucan dissolution was slow and had a stronger effect on the rate of the process. Therefore, reproducible colonic drug delivery not critically influenced by inter- and intra-individual variation of microbial enzyme activity may be projected.

Statement of Retraction: Synthesis of Chemically Cross-Linked Hydroxypropyl Methyl Cellulose Hydrogels and their Application in Controlled Release of 5-Amino Salicylic Acid

Statement of Retraction: Synthesis of Chemically Cross-Linked Hydroxypropyl Methyl Cellulose Hydrogels and their Application in Controlled Release of 5-Amino Salicylic Acid

Preparation and in-vitro characterization of 5-aminosalicylic acid loaded hydrogels for colon specific delivery

The aim of the current investigation was to prepare and characterize the novel pH-sensitive hydrogels of pluronic F127 and sodium polystyrene sulfonate for the controlled delivery of 5-aminosalicylic acid to colon. Pluronic F127 and sodium polystyrene sulfonate were crosslinked with acrylic acid by N,N′-Methylene bisacrylamide. Various studies including porosity, drug loading, swelling, and drug release were performed for the fabricated hydrogels. Greater swelling and drug release were observed at high pH 7.4 as compared to pH 4.6 and 1.2, thus depicted pH-sensitive nature of developed hydrogel. Characterizations such as Fourier transform infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), X-ray diffraction (XRD) analysis, and scanning electron microscopy (SEM), were performed in order to evaluate the crosslinking, thermal stability, crystallinity, and surface morphology of the fabricated hydrogel, respectively. The toxicity of the developed drug carrier system was investigated by the HET-CAM test and revealed no toxic effects on the chorioallantoic membrane of the chicken egg. Conclusively, the fabricated hydrogel could be applied as a potential alternate to conventional dosage forms for controlled release of 5-aminosalicylic acid for prolonged period of time.

Manufacturing of self-standing multi-layered 3D-bioprinted alginate-hyaluronate constructs by controlling the cross-linking mechanisms for tissue engineering applications

Three-dimensional (3D) bioprinting of self-supporting stable tissue and organ structure is critically important in extrusion-based bioprinting system, especially for tissue engineering and regenerative medicine applications. However, the development of self-standing bioinks with desired crosslinking density, biocompatibility, tunable mechanical strength and other properties like self-healing, in situ gelation, drug or protein incorporation is still a challenge. In this study, we report a hydrogel bioink prepared from alginate (Alg) and hyaluronic acid (HA) crosslinked through multiple crosslinking mechanisms, i.e. acyl-hydrazone, hydrazide interactions and calcium ions. These Alg-HA gels were highly dynamic and shear-thinning with exceptional biocompatibility and tunable mechanical properties. The increased dynamic nature of the gels is mainly chemically attributed to the presence of acyl-hydrazone bonds formed between the amine groups of the acyl-hydrazide of alginate and the monoaldehyde of the HA. Among the different combinations of Alg-HA gel compositions prepared, the A5H5 (Alginate-acyl-hydrazide:HA-monoaldehyde, ratio 50:50) gel showed a gelation time of ∼60 s, viscosity of ∼400 Pa s (at zero shear rate), high stability in various pH solutions and increased degradation time (>50 days) than the other samples. The A5H5 gels showed high printability with increased post-printing stability as observed from the 3D printed structures (e.g. hollow tube (∼100 layers), porous cube (∼50 layers), star, heart-in, meniscus and lattice). The scanning electron microscopy analysis of the 3D constructs and hydrogels showed the interconnected pores (∼181 µm) and crosslinked networks. Further, the gels showed sustained release of 5-amino salicylic acid and bovine serum albumin. Also, the mechanical properties were tuned by secondary crosslinking via different calcium concentrations. In vitro assays confirmed the cytocompatibility of these gels, where the 3D bioprinted lattice and tubular (∼70 layers) constructs demonstrated high cell viability under fluorescence analysis. In in vivo studies, Alg-HA gel showed high biocompatibility (>90%) and increased angiogenesis (threefolds) and reduced macrophage infiltration (twofold decrease), demonstrating the promising potential of these hydrogels in 3D bioprinting applications for tissue engineering and regenerative medicine with tunable properties.

Hemoglobin bio-adhesive nanoparticles as a colon-specific delivery system for sustained release of 5-aminosalicylic acid in the effective treatment of inflammatory bowel disease

A colonic drug delivery system was developed to specifically deliver 5-aminosalicylic acid (5-ASA) to the inflamed site by conjugating with hemoglobin nanoparticles (HbNPs). The 5-ASA-HbNPs (eight 5-ASA molecules per Hb molecule) with the size of 220 nm and zeta potential of −14.6 mV is a tailored nanoparticle able to pass through the mucus layer. The 5-ASA-HbNPs do not undergo chemical and enzymatic hydrolysis in the simulated gastrointestinal fluids over 6 h. Significantly higher cellular uptakes and prolonged release was seen for the 5-ASA-HbNPs in Caco-2 cells, compared to free 5-ASA over 72 h. In addition, 5-ASA-HbNPs revealed similar therapeutic effectiveness with free 5-ASA against tumor necrosis factor and showed less inhibitory concentration (IC50) for myeloperoxidase enzyme activity. In vivo imaging of mouse demonstrated the localization of drug in the descending colon after oral administration and about 15% of the administered dose was recovered as 5-ASA from urine in 6 h. The use of these nanoparticles with the mucus adhesion properties and permeability to intestinal epithelial cells can be a good candidate with potential application in the colonic drug delivery field.

Застосування препаратів 5-аміносаліцилової кислоти в лікуванні запальних захворювань кишечника

Стаття присвячена порівняльній характеристиці різних похідних 5-аміносаліцилової кислоти. Дослідження останніх десятиліть змінили уявлення про можливості застосування аміносаліцилатів у терапії різних запальних захворювань кишечника. У зв’язку з невідомою етіологією хвороби Крона та неспецифічного виразкового коліту етіотропної терапії цих захворювань немає. Сутність лікування зводиться до гальмування активності запалення при загостреннях і проведенні курсів протирецидивної терапії. Численні дослідження, проведені протягом останніх 20 років, показали, що основу базисної терапії хронічних неспецифічних запальних захворювань кишечника становлять препарати 5-аміносаліцилової кислоти, або саліцилати. При виборі лікарської форми слід ураховувати відмінності між препаратами месалазину залежно від типу оболонки. Показано, що з точки зору фармакокінетики найбільш ефективними лікарськими формами месалазину для лікування неспецифічного виразкового коліту та хвороби Крона з ураженням товстої кишки є таблетки з кишковорозчинним покриттям, що забезпечує рН-залежне поступове вивільнення 5-аміносаліцилової кислоти на протязі усієї товстої кишки. Наявні на сьогодні на фармацевтичному ринку препарати 5-аміносаліцилової кислоти здатні контролювати перебіг виразкового коліту та хвороби Крона з ураженням товстої кишки в переважної більшості пацієнтів. Застосування препаратів 5-аміносаліцилової кислоти не обмежується терапією неспецифічного виразкового коліту та хвороби Крона. Препарат широко застосовується при інших захворюваннях кишечника, таких як дивертикулярна хвороба товстої кишки, банальні коліти, променеві ураження ободової кишки, а також для лікування такої поширеної хвороби, як синдром подразненого кишечника. Результати дослідження, що було проведено у відділенні захворювань кишечника ДУ «Інститут гастроентерології НАМН України» упродовж 2 років, показали позитивний ефект 20-денного лікування Месаколом неускладненої дивертикулярної хвороби. Месакол у дозі 1600 мг на добу призвів до повного купірування абдомінальної симптоматики у 68,7 % хворих.

Application of inulin/Eudragit RS in 5-ASA pellet coating with tuned, sustained-release feature in an animal model of ulcerative colitis

A tunable release of 5-aminosalicylic acid (5-ASA) could bring therapeutic benefits in the treatment of inflammatory bowel disease (IBD).A 32 factorial design was used to achieve a tuned delivery of 5-ASA pellets in the small and large intestine using a coating composed of inulin/Eudragit RS (RS). The ratio of inulin/RS and coating level were independent variables while the dependent variables were the percent of drug release at pH 1.2 in 2 h and total release of drug in 10 h at pH 6.8. 5-ASA release from pellets was examined at different pH levels and the therapeutic efficacy of the optimum pellets was compared to 5-ASA pellets of Pentasa in rats with ulcerative colitis.The inulin/RS of 18/82 at a coating level of 16% was found to be the optimum for delivery of the drug to the small and large intestine. The coated pellets offered a superior therapeutic outcome compared to uncoated pellets and Pentasa in terms of colitis activity index (CAI), and the colon's tissue enzymes of GSH and MDA.The optimum coating composed of inulin and RS could offer a tuned sustained release of 5-ASA throughout the small and large intestine with the sensitivity of drug release to microbial degradation.

Effects of fiber intake on intestinal pH, transit, and predicted oral mesalamine delivery in patients with ulcerative colitis.

Limited data are available on the effects of fermentable fiber in altering intestinal pH and transit to predict efficacy-based delivery profiles of pH-dependent mesalamine coatings in ulcerative colitis (UC). This study aimed to examine regional pH and transit after acute changes in fermentable fiber intake in quiescent UC patients and their effects on drug release systems. In a randomized, double-blind study, 18 patients with quiescent UC and 10 healthy controls were supplied meals high (13g) or low (≤2g) in fermentable fiber and subsequently ingested a wireless pH-motility capsule. After a ≥3-day washout, they crossed over to the other diet. Measurements of intestinal pH and transit were used to predict drug release for the various pH-dependent coatings. Increasing fermentable fiber intake lowered overall (median 6.2 [6.1-6.7] vs low: 6.9 [range or interquartile range: 6.4-7.4]; P=0.01) and distal pH (7.8 [7.3-8.1] vs 8.2 [8.0-8.5]; P=0.04) in controls. In UC patients, only cecal pH was decreased (high: 5.1 [4.8-5.5] vs low: 5.5 [5.3-5.7]; P<0.01). Colonic transit in the UC cohort varied widely after a low-fiber intake but tended to normalize after the high fermentable fiber intake. Hypothetical coating dissolution profiles were heterogeneous in UC patients, with a multi-matrix delayed release system having the highest likelihood of patients (20-40%) with incomplete dissolution, and predominant small intestinal dissolution predicted for Eudragit L (94% patients) and S (44-69%). Patients with quiescent UC have abnormalities in intestinal pH and transit in response to acute changes in fermentable fiber intake. These have potentially detrimental effects on predicted luminal release patterns of pH-dependent 5-aminosalicylic acid release systems.

Functionalization of ginger derived nanoparticles with chitosan to design drug delivery system for controlled release of 5-amino salicylic acid (5-ASA) in treatment of inflammatory bowel diseases: An in vitro study

The present study aimed at synthesising chitosan bound ginger nanocarriers for slow and controlled release of the drug 5-amino salicylic acid (5-ASA) against inflammatory bowel diseases (IBD). The chitosan, extracted from naturally occurring biopolymer chitin, was reacted to ginger extract (Zingiber officinale) to prepare chitosan-bounded ginger derived nanocarriers (C-GDNC) and further loaded with 5-ASA drug. The as-obtained drug loaded chitosan coated ginger derived nanocarriers (D-C-GNDC) were studied for controlled release of 5-ASA. In vitro experimental data implied slow and controlled release of 5-ASA and were kinetically justified by applying different kinetic models. The obtained percent drug loading capacity and entrapment efficiency were more than 50%. Various experimental factors affecting swelling controlled drug release of 5-ASA, such as change in pH of release medium, chemical composition of nanocarriers, percent drug loading, and simulated biofluids as release media, were investigated. The prepared nanomaterials were well characterized and examined for chemical stability and in vitro cytotoxicity to check their biocompatible nature. The overall studies concluded that the controlled release of 5-ASA was favourable at the gastrointestinal pH which is desirably beneficial against inflammation of bowl.

Synthesis of ginger derived nanocarriers (GDNC) and study of in vitro release of 5-amino salicylic acid (5-ASA) as an anti inflammatory drug

In the present study ginger derived nanocarriers were prepared, characterized and used for the controlled release of an anti-inflammatory drug 5-ASA (5-amino salicylic acid). The mechanism of drug targeting was based on the release of 5-ASA drug molecules from the ginger derived nanocarriers having 62.24% drug loading capacity and 80.55% drug entrapment efficiency, and undergoing swelling in aqueous release medium. The present study considered the ginger not only for preparing nanocarriers but also as a medicine with anti-inflammatory, anti-oxidative and anti-bacterial actions. The nanocarriers obtained as a fine powder were characterized by different techniques such as Fourier-Transform Infrared Spectroscopy (FTIR), X-ray diffraction (XRD) analysis, Differential Scanning Calorimetry (DSC), Thermal Gravimetric Analysis (TGA), Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), and Dynamic Light Scattering (DLS) based measurements of size and zeta potential, respectively. The particle size was found to be within 50 nm–100 nm range whereas the zeta potential was −29.2 mV at pH 6.9. The effect of various factors like drug loading and entrapment efficiency, pH, and nature of the release medium was observed on the release profiles of 5-amino salicylic acid. The in vitro experiments were also conducted to check the stability of carriers in different pH environments and simulated biofluids.

Controlled drug release behavior of 5-aminosalicylic acid using polyacrylamide grafted oatmeal (OAT-g-PAM): a pH-sensitive drug carrier

In the present investigation, we have evaluated the in vitro drug release of 5-aminosalicylic acid (5-ASA) using polyacrylamide grafted oatmeal (OAT-g-PAM). The graft co-polymer was synthesized by following free radical co-polymerization pathway using acrylamide as a monomer and ceric ammonium nitrate as a free radical initiator in the presence of microwave. The matrix tablet was prepared using the different grades of developed graft co-polymers following standard protocol. In vitro release phenomena of 5-ASA from the prepared matrix tablet up to 12 h in different buffer solution, i.e., pH 2.0, 7.0 and 7.4, an ideal condition for colon specific drug delivery was studied. The release rate of 5-ASA can be controlled efficiently by tuning the pH value. The drug release kinetic of 5-ASA from different matrix tablet was evaluated on the basis of in vitro controlled drug release results. The result indicates that the novel pH-sensitive matrices under study showing Fickian diffusion mechanism and potentially constructive for colonic drug delivery system.

Starch film-coated microparticles for oral colon-specific drug delivery

The aim of this study was to prepare and characterize a novel type of starch-coated microparticles (MPs) allowing site-specific delivery of bioactives to the colon. An oral colon-specific controlled-release system was developed in the form of MPs coated with a resistant starch (RS2/RS3) film (RS@MPs) through an aqueous suspension coating process. The RS2 was chosen from a high-amylose cornstarch with 88.5% digestion resistibility. The RS3 was prepared by a high-temperature/pressure (HTP) treatment, with the following of enzymatic debranching, and retrogradation, resulting in a dramatic increase in enzymatic resistance (RS3 content: 76.6%). RS@MPs showed 40.7% of 5-aminosalicylic acid release within 8 h. The in vivo study of fluorescein-loaded RS@MPs indicated the high acidic and enzymatic resistibility of RS@MPs and a restrained release in the upper GIT. Therefore, RS@MPs has revealed to be a high potential system for accurately targeting bioactive compound delivery to the colon.

Synthesis of Aloevera/Acrylonitrile based Nanoparticles for targeted drug delivery of 5-Aminosalicylic acid

Aloevera (AV) polysaccharide/acrylonitrile (AN) nanoparticles (AVANp4 of ∼50nm size) have been crafted via free radical polymerization method using persulfate/ascorbic acid (KPS/AA) and methylenebisacrylamide (MBA) as the redox initiator and crosslinker respectively. AVANp4 was extensively characterized using FTIR, SEM, TEM, XRD, and Thermal analysis (TGA & DTG). Inclusion of AN in AV polysaccharide has been evidenced by nitrile stretching peak at 2244cm−1 in FTIR spectrum of AVANp4. Colon specific targeted in-vitro release of 5-Aminosalicylic acid from AVANp4 has been studied in pH 1.2 and pH 7.4 buffer solutions at 37°C. The controlled release was witnessed up to 48h for AVANp4 in contrast to AV for which the release exhausted within 7–8h in both the buffers. The delayed release of the drug from AVANp4 is attractive since it can allow the drug to reach colon rather than being released in the upper part of the gastrointestinal tract.

P638 Release of 5-aminosalicylic acid from mesalazine formulations: a novel dynamic dissolution model simulating gastrointestinal pH changes

P638 Release of 5-aminosalicylic acid from mesalazine formulations: a novel dynamic dissolution model simulating gastrointestinal pH changes

Synthesis and characterization of new shellac–hydroxypropylmethylcellulose composite for pharmaceutical applications

A new pH-responsive carrier matrix was designed from combination of shellac (Sh), hydroxpropylmethylcellulose (HPMC) and acrylic acid (AA). Characterization of materials was done using various advanced instrumentation techniques. The kinetics of thermal decomposition of materials were studied and compared using Coats–Redfern (CR) and Kissinger–Akahira–Sunose (KAS) mathematical models. The Arrhenius equations for thermal decomposition of shellac and chemically modified shellac (Sh–HPMC–AA) were computed to be k = (3.4 × 1021) e−159.9/RT and k = (141.8) e−19.6/RT s−1, respectively. The pH-responsive characteristics of Sh–HPMC–AA shows 288% swelling ratio. Further, the controlled release of 5-amino salicylic acid (5-ASA) was studied in buffer medium and Fick’s diffusion equation was applied for calculation of transport phenomenon. The enzymatic degradation study of Sh–HPMC–AA is also reported.

Obtaining the palygorskite:chitosan composite for modified release of 5-aminosalicylic acid

This study's aim was to obtain composites from palygorskite (PLG) and chitosan (CS) in order to modify 5-aminosalicylic (5-ASA) release. Initially, the PLG:CS composite was obtained using glutaraldehyde (GLA) as a reticular agent. Then, PLG, CS and PLG:CS were characterized by means of analytical techniques such as CHN elemental analysis, surface area analysis, XRD, FTIR, DSC and TG, SEM, adsorption tests and release profiles. Based on analytical data, the formation of the PLG:CS composite which showed the presence about 19% of CS, decrease in specific surface area, morphological analysis modified, visible change of crystallinity, of FTIR and thermal analysis. In relation to the drug-composite interaction, PLG:CS exhibited a significant increase in adsorption with 5-ASA at 58.24% in relation to PLG and CS which were at 16.29% and 23.96% respectively. The release profiles show that the PLG:CS composite changed the 5-ASA release speed in analyzed simulated fluids (intestinal and stomach) unlike other systems. Thus, the PLG:CS composite with proven synergy of the PLG and CS inherent properties showing 5-ASA effective modified release. Hence, this composite has potential benefits for the vectorization of drugs.

PH Responsive Shellac for Pharmaceutical Applications: Preparation, Thermal Stability and Controlled Release of 5-Amino salicylic Acid

pH Responsive Shellac for Pharmaceutical Applications: Preparation, Thermal Stability and Controlled Release of 5-Amino salicylic Acid

Release of 5-Aminosalicylic Acid (5-ASA) from Mesalamine Formulations at Various pH Levels.

IntroductionOral formulations of 5-aminosalicylic acid (5-ASA) for treatment of ulcerative colitis have been developed to minimize absorption prior to the drug reaching the colon. In this study, we investigate the release of 5-ASA from available oral mesalamine formulations in physiologically relevant pH conditions.MethodsRelease of 5-ASA from 6 mesalamine formulations (APRISO®, Salix Pharmaceuticals, Inc., USA; ASACOL® MR, Procter & Gamble Pharmaceuticals UK Ltd.; ASACOL® HD, Procter & Gamble Pharmaceuticals, USA; MEZAVANT XL®, Shire US Inc.; PENTASA®, Ferring Pharmaceuticals, Ltd., UK; SALOFALK®, Dr. Falk Pharma UK Ltd.) was evaluated using United States Pharmacopeia apparatus I and II at pH values of 1.0 (2 h), 6.0 (1 h), and 6.8 (8 h). Dissolution profiles were determined for each formulation, respectively.ResultsOf the tested formulations, only the PENTASA formulation demonstrated release of 5-ASA at pH 1.0 (48%), with 56% cumulative release after exposure to pH 6.0 and 92% 5-ASA release after 6–8 h at pH 6.8. No other mesalamine formulation showed >1% drug release at pH 1.0. The APRISO formulation revealed 36% 5-ASA release at pH 6.0, with 100% release after 3 h at pH 6.8. The SALOFALK formulation revealed 11% 5-ASA release at pH 6.0, with 100% release after 1 h at pH 6.8. No 5-ASA was released by the ASACOL MR, ASACOL HD, and MEZAVANT XL formulations at pH 6.0. At pH 6.8, the ASACOL MR and ASACOL HD formulations exhibited complete release of 5-ASA after 4 and 2 h, respectively, and the MEZAVANT XL formulation demonstrated complete 5-ASA release over 6–7 h.Conclusion5-Aminosalicylic acid release profiles were variable among various commercially available formulations.FundingShire Development LLC.Electronic supplementary materialThe online version of this article (doi:10.1007/s12325-015-0206-4) contains supplementary material, which is available to authorized users.

Modified hydroxypropyl methyl cellulose: Efficient matrix for controlled release of 5-amino salicylic acid

Hydroxypropyl methyl cellulose has been modified by grafting synthetic polyacrylamide chains [g-HPMC (M)] in presence of microwave irradiation, which has used as carrier for controlled release of 5-amino salicylic acid (5-ASA). The FTIR and UV–vis–NIR studies reveal the excellent compatibility between g-HPMC (M) and 5-ASA. Field emission scanning electron microscopy (FESEM) and UV–vis–NIR analyses suggest that physical interaction predominates between the drug and matrix. % equilibrium swelling ratio (% ESR) of g-HPMC (M) decreased with addition of salt solutions and follow the order: Na+>K+>Mg2+>Ca2+>Al3+. The in vitro 5-ASA release studies indicate that g-HPMC (M) delivers the drug preferentially in colonic region in more sustained way than that of HPMC. The 5-ASA release follows first order kinetics and non-Fickian diffusion mechanism. These favorable features make the graft copolymer a potential matrix for colon specific delivery of 5-ASA.