Simulated Gastrointestinal Media Research Articles

Nanocochleates as novel delivery vehicles for enhancement of water solubility, stability and controlled release of dihydromyricetin in gastrointestinal tract

Dihydromyricetin (DHM) possesses impressive antioxidant and anti-inflammatory properties; however, its effectiveness is limited by poor bioavailability. Liposomes improve the solubility and stability of insoluble bioactives but encounter challenges in gastrointestinal fluids after oral administration. Consequently, DHM-loaded nanocochleates were fabricated to enhance the solubility, stability, and release behavior of DHM. The nanoliposomes exhibited an entrapment efficiency (EE) ranging from 85.64 % to 88.79 %, a particle size between 136.20 and 150.70 nm, a polydispersity index (PDI) of 0.36 to 0.43, and a zeta potential of –6.82 to –11.13 mV. In contrast, the cylindrical-shaped nanocochleates demonstrated an EE ranging from 74.94 % to 84.64 %, a particle size between 239.07 and 571.43 nm, a PDI from 0.16 to 0.61, and a zeta potential ranging from –21.97 to –27.10 mV. The nanocochleates exhibited improved water solubility (64.75 %) and retained antioxidant activity (41.38 %) compared to free DHM. Additionally, they demonstrated enhanced stability of DHM compared to nanoliposomes during 30 days of storage. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed that DHM was encapsulated within nanocochleate structures via ionic and chemical interactions. X-ray diffraction revealed a distinct organization of the nanocochleates in comparison to the nanoliposomes. The release of DHM from nanocochleates demonstrated a prolonged and controlled release in simulated gastrointestinal medium, unlike the burst release observed with nanoliposomes. This study hightlighted the potential of nanocochleates as novel delivery vehicles for enhancing the stability and bioavailability of DHM. It also offered a unique perspective on developing functional food formulations that utilize nanocochleates as promising nanocarriers for bioactives.

Green Synthesis, Characterization, Encapsulation, and Measurement of the Release Potential of Novel Alkali Lignin Micro-/Submicron Particles.

The applicability of biopolymer micro-/nano- technology in human, veterinary medicine, pharmaceutical, and food technology is rapidly growing due to the great potential of biopolymer-based particles as effective carrier systems. The use of lignin as a basic heteropolymer biomatrix for the design of innovative micro-/submicron formulations allows the achievement of increased biocompatibility and offers various active functional groups presenting opportunities for customization of the physicochemical properties and bioactivities of the formulations for diverse applications. The aim of the present study was to develop a simple and ecofriendly methodology for the synthesis of lignin particles with micro- and submicron size; to evaluate their physicochemical, spectral, and structural characteristics; and to examine their capacity for encapsulation of biologically active molecules and potential for in vitro release of bioflavonoids in simulated gastrointestinal media. The presented methodologies apply cheap and green solvents; easy, straightforward, quick, and sensitive processes requiring little equipment, non-toxic substances, and simple methods for their characterization, the determination of encapsulation capacity towards the poorly water-soluble bioactive compounds morin and quercetin, and the in vitro release potential of the lignin matrices.

Chitosan/Albumin Coating Factorial Optimization of Alginate/Dextran Sulfate Cores for Oral Delivery of Insulin.

The design of nanoparticle formulations composed of biopolymers, that govern the physicochemical properties of orally delivered insulin, relies on improving insulin stability and absorption through the intestinal mucosa while protecting it from harsh conditions in the gastrointestinal (GI) tract. Chitosan/polyethylene glycol (PEG) and albumin coating of alginate/dextran sulfate hydrogel cores are presented as a multilayer complex protecting insulin within the nanoparticle. This study aims to optimize a nanoparticle formulation by assessing the relationship between design parameters and experimental data using response surface methodology through a 3-factor 3-level optimization Box-Behnken design. While the selected independent variables were the concentrations of PEG, chitosan and albumin, the dependent variables were particle size, polydispersity index (PDI), zeta potential, and insulin release. Experimental results showed a nanoparticle size ranging from 313 to 585 nm, with PDI from 0.17 to 0.39 and zeta potential ranging from -29 to -44 mV. Insulin bioactivity was maintained in simulated GI media with over 45% cumulative release after 180 min in a simulated intestinal medium. Based on the experimental responses and according to the criteria of desirability on the experimental region's constraints, solutions of 0.03% PEG, 0.047% chitosan and 1.20% albumin provide an optimum nanoparticle formulation for insulin oral delivery.

Chitosan Sponges with Instantaneous Shape Recovery and Multistrain Antibacterial Activity for Controlled Release of Plant-Derived Polyphenols.

Biomass-derived materials with multiple features are seldom reported so far. Herein, new chitosan (CS) sponges with complementary functions for point-of-use healthcare applications were prepared by glutaraldehyde (GA) cross-linking and tested for antibacterial activity, antioxidant properties, and controlled delivery of plant-derived polyphenols. Their structural, morphological, and mechanical properties were thoroughly assessed by Fourier-transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and uniaxial compression measurements, respectively. The main features of sponges were modulated by varying the CS concentration, cross-linking ratio, and gelation conditions (either cryogelation or room-temperature gelation). They exhibited complete water-triggered shape recovery after compression, remarkable antibacterial properties against Gram-positive (Staphylococcus aureus (S. aureus), Listeria monocytogenes (L. monocytogenes)) and Gram-negative (Escherichia coli (E. coli), Salmonella typhimurium (S. typhimurium)) strains, as well as good radical scavenging activity. The release profile of a plant-derived polyphenol, namely curcumin (CCM), was investigated at 37 °C in simulated gastrointestinal media. It was found that CCM release was dependent on the composition and the preparation strategy of sponges. By linearly fitting the CCM kinetic release data from the CS sponges with the Korsmeyer-Peppas kinetic models, a pseudo-Fickian diffusion release mechanism was predicted.

A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo

The aim of this study was to develop, characterize and evaluate the in vivo oral efficacy of self-emulsifying drug delivery systems (SEDDS) containing fexinidazole (FEX) in the experimental treatment of visceral leishmaniasis (VL). The developed FEX-SEDDS formulation presented as a clear, yellowish liquid, with absence of precipitate. The droplet size, polydispersion index and zeta potential after dilution in water (1:200) was of 91 ± 3 nm, 0.242 ± 0.005 and −16.7 ± 0.2, respectively. In the simulated gastric and intestinal media, the FEX-SEDDS had a size of 97 ± 1 and 106 ± 9 nm, respectively. The FEX retention in droplet after SEDDS dilution in simulated gastrointestinal media was almost 100 %. Antileishmanial efficacy studies showed that FEX-SEDDS was the only treatment able to significantly (p < 0.05) reduce the parasite burden in the liver and spleen of animals experimentally infected with Leishmania infantum. Our intestinal permeability data suggest that FEX-SEDDS showed no evidence of injury to the intestinal mucosa. These findings suggest that FEX-SEDDS can be a promising oral alternative for the treatment of VL caused by L. infantum.

Assembly of electrospun tri-layered nanofibrous structure of zein/basil seed gum/zein for increasing the bioaccessibility of lycopene

In this work, tri-layered nanofibers including zein (30% w/v) in top/bottom layers and the optimal volume ratio of polyvinyl alcohol (PVA, 10% w/v)/basil seed gum (BSG, 1% w/v) with lycopene in the middle layer was used to enhance the bioaccessibility of lycopene. Viscosity, electrical conductivity, and surface tension of BSG/PVA solutions in different volume ratios were measured. According to SEM images, it was found that the solution with BSG to PVA ratio of 70:30 ratio was the best nanofiber for trapping lycopene. The encapsulation efficiency of lycopene in tri-layered nanofibers was in the range of 81.7–92.26%. According to the DSC diagram, lycopene was successfully encapsulated in tri-layered nanofibers. DSC diagrams confirmed the improvement of lycopene thermal resistance in tri-layered nanofibers. The FTIR analysis showed no chemical interaction between the tri-layered nanofiber components. The bioaccessibility of lycopene in the small intestine using tri-layered nanofiber was 16.18%. The release behavior of lycopene was studied by Kopcha, Higuchi, Korsmeyer-Peppas, and Peppas-Sahlin models, which showed that the diffusion and erosion mechanisms were involved in the release of lycopene from tri-layered nanofibers in simulated gastrointestinal media.

Quercetin LipoMicel—A Novel Delivery System to Enhance Bioavailability of Quercetin

Background: Quercetin, a flavonoid found in plant-based foods, has a range of biological activities that may be beneficial for human health. The pharmacokinetic profile of quercetin remains, however, a limiting factor for its use as a nutritional supplement. Quercetin LipoMicel®—a novel delivery system encapsulating quercetin into a liquid micelle matrix—has been designed to address the low bioavailability issue associated with non-conjugated forms by improving the absorption of quercetin. Objective: The purpose of this study was to evaluate the solubility and gastrointestinal absorption of quercetin in a novel Quercetin LipoMicel delivery system in healthy adult volunteers by comparing it with free quercetin and another commercial quercetin product. Several pharmacokinetic parameters were compared between these three formulations. Methods: Twelve healthy adult male and female volunteers aged between 21 and 65, with BMIs under 30, participated in a non-blinded, crossover bioavailability study conducted with three quercetin products. Each treatment contained a total dose of 500 mg quercetin. Capillary whole blood samples from participants were collected serially at intervals from 0–24 hours. Quercetin concentrations were detected and measured by ultra-performance liquid chromatography (UHPLC) coupled to a Thermo QExactive Orbitrap Mass Spectrometer. Solubility of quercetin in water and simulated gastrointestinal media was determined by UHPLC. Results: Oral absorption of quercetin was significantly enhanced with the LipoMicel delivery system compared to free quercetin. Improvements in in vitro gastric stability and intestinal solubility were observed with LipoMicel, leading to significantly higher blood concentration and enhanced duration of a stable concentration of quercetin in the body. Compared to free quercetin, 8- and 9-fold increases in AUC and Cmax were attained with the LipoMicel delivery system, and 10-fold higher quercetin plasma concentrations detected at 12 hours after administration. Conclusions: Quercetin LipoMicel represents an efficient delivery system for augmenting the bioavailability of quercetin in vivo. Significantly higher blood concentrations and a sustained release of quercetin over the study period was achieved following the administration of quercetin via the LipoMicel technology. Optimization in the in vivo bioavailability of quercetin may promote its salutary effects.

Gelatin-Graphene Oxide Nanocomposite Hydrogels for Kluyveromyces lactis Encapsulation: Potential Applications in Probiotics and Bioreactor Packings

Nutraceutical formulations based on probiotic microorganisms have gained significant attention over the past decade due to their beneficial properties on human health. Yeasts offer some advantages over other probiotic organisms, such as immunomodulatory properties, anticancer effects and effective suppression of pathogens. However, one of the main challenges for their oral administration is ensuring that cell viability remains high enough for a sustained therapeutic effect while avoiding possible substrate inhibition issues as they transit through the gastrointestinal (GI) tract. Here, we propose addressing these issues using a probiotic yeast encapsulation strategy, Kluyveromyces lactis, based on gelatin hydrogels doubly cross-linked with graphene oxide (GO) and glutaraldehyde to form highly resistant nanocomposite encapsulates. GO was selected here as a reinforcement agent due to its unique properties, including superior solubility and dispersibility in water and other solvents, high biocompatibility, antimicrobial activity, and response to electrical fields in its reduced form. Finally, GO has been reported to enhance the mechanical properties of several materials, including natural and synthetic polymers and ceramics. The synthesized GO-gelatin nanocomposite hydrogels were characterized in morphological, swelling, mechanical, thermal, and rheological properties and their ability to maintain probiotic cell viability. The obtained nanocomposites exhibited larger pore sizes for successful cell entrapment and proliferation, tunable degradation rates, pH-dependent swelling ratio, and higher mechanical stability and integrity in simulated GI media and during bioreactor operation. These results encourage us to consider the application of the obtained nanocomposites to not only formulate high-performance nutraceuticals but to extend it to tissue engineering, bioadhesives, smart coatings, controlled release systems, and bioproduction of highly added value metabolites.

Encapsulation of Anthocyanins from Cornelian Cherry Fruits Using Heated or Non-Heated Soy Proteins.

In the current study, the effect of temperature on the potential of soy proteins to ensure the encapsulation and gastric stability of bioactives, such as anthocyanins from cornelian cherry fruits, was investigated. The powders obtained after freeze-drying were analyzed in relation to flow properties, encapsulation retention and efficiency, stability in simulated gastrointestinal medium, color, and morphology. Preheating the soy proteins generated a powder with low density. Powders obtained with native soy proteins allowed the highest encapsulation efficiency and the lowest was obtained when using preheated soy proteins. The heat treatment of the mixture of soy proteins and cornelian cherry fruits prior to encapsulation generated powders with the highest lightness and the lowest intensity of red shades among all samples. The in vitro experiments revealed that the highest protection in simulated gastric environment was provided when protein was heat treated either alone or in combination with bioactives to be encapsulated. The morphological analysis highlighted that powders consisted of large and rigid structures.

Solid Lipid Nanoparticles as Formulative Strategy to Increase Oral Permeation of a Molecule Active in Multidrug-Resistant Tuberculosis Management.

The role of mycobacterial efflux pumps in drug-resistant tuberculosis has been widely reported. Recently, a new compound, named SS13, has been synthesized, and its activity as a potential efflux inhibitor has been demonstrated. In this work, the chemical–physical properties of the SS13 were investigated; furthermore, a formulative study aimed to develop a formulation suitable for oral administration was performed. SS13 shows nonintrinsic antitubercular activity, but it increases the antitubercular activity of all the tested drugs on several strains. SS13 is insoluble in different simulated gastrointestinal media; thus, its oral absorption could be limited. Solid lipid nanoparticles (SLNs) were, therefore, developed by using two different lipids, Witepsol and/or Gelucire. Nanoparticles, having a particle size (range of 200–450 nm with regards to the formulation composition) suitable for intestinal absorption, are able to load SS13 and to improve its permeation through the intestinal mucosa compared to the pure compound. The cytotoxicity is influenced by the concentration of nanoparticles administered. These promising results support the potential application of these nanocarriers for increasing the oral permeation of SS13 in multidrug-resistant tuberculosis management.

Xylan microparticles for controlled release of mesalamine: Production and physicochemical characterization

Xylan extracted from corn cobs was used to produce mesalamine-loaded xylan microparticles (XMP5-ASA) by cross-linking polymerization using a non-hazardous cross-linking agent. The microparticles were characterized by thermal analysis (DSC/TG), X-ray diffraction (XRD), Infrared spectroscopy (FTIR-ATR) and scanning electron microscopy (SEM). A comparative study of the in vitro drug release from XMP5-ASA and from gastro-resistant capsules filled with XMP5-ASA (XMPCAP5-ASA) or 5-ASA was also performed. NMR, FTIR-ATR, XRD and DSC/TG studies indicated molecularly dispersed drug in the microparticles with increment on drug stability. The release studies showed that XMPCAP5-ASA allowed more efficient drug retention in the simulated gastric fluid and a prolonged drug release lasting up to 24 h. XMPCAP5-ASA retained approximately 48 % of its drug content after 6 h on the drug release assay. Thus, the encapsulation of 5-ASA into xylan microparticles together with gastro-resistant capsules allowed a better release control of the drug during different simulated gastrointestinal medium.

Designation and characterization of cold-set whey protein-gellan gum hydrogel for iron entrapment

This study is aimed at designing of a composite cold-set hydrogel using whey protein isolate (WPI) and gellan gum as iron carrier. The effect of total polymer concentration (TPC) (0.5 and 1.5%), WPI/gellan ratio (1:1, 1:2, and 1:3), and iron concentration (10, 40, and 70 mM) on physicochemical and rheological characteristics of hydrogel were analyzed. By increasing TPC, the release mechanism became complex regarding less erosion of structure in simulated gastrointestinal medium. Moreover, the CO peak area of FTIR spectra was enhanced. As WPI/gellan ratio decreased, the faster release occurred due to a more porous structure. The cumulative release of iron in acidic and neutral pH increased up to 71.74 and 9.14%; however, iron was released up to 88.55 and 28.72% in simulated gastric and intestinal medium, respectively. The iron release followed a chemically-controlled mechanism in all samples. The area and number of gel pores and water-holding capacity decreased as Fe concentration was enhanced, but denaturation temperature increased. These results suggest that the strong texture with a solid elastic behavior along with a high cumulative release of iron made our hydrogel suitable for iron delivery to reduce iron deficiency-related disorders.

Gum tragacanth-polyvinyl alcohol aerogel for oral delivery of silymarin

This study reports for the first time the fabrication of highly porous aerogels of mixed gum tragacanth-polyvinyl alcohol (GT-PVA) for loading and oral delivery of silymarin (SM). Various analytical techniques were used to investigate changes in the physical, textural, mechanical and microstructural properties of aerogels as affected by blending ratio and vacuum impregnation (VI) of SM. Results showed that the mixing ratio of 1:1 led to aerogels of larger surface area (1029.20 m2·g−1) and superior physicochemical properties. However, at mixing ratio of 3:1 (GT:PVA) higher loading capacity (45.57% ± 2.3%) was obtained. SM loading, on the other hand, had an adverse effect on the porosity, microstructure and physical attributes of aerogels transforming them from meso-porous to macro-porous structures. The release rate of SM in simulated gastrointestinal media was found to follow Korsmeyere-Peppas model.

Dexketoprofen trometamol-loaded poly-lactic-co-glycolic acid (PLGA) nanoparticles: Preparation, &lt;i&gt;in vitro&lt;/i&gt; characterization and cyctotoxity

Purpose: To design, formulate and characterize sustained-release formulations of dexketoprofen trometamol (DT) nanoparticles (NPs)Methods: Dexketoprofen trometamol (DT)-loaded poly(lactic-co-glycolic acid) (PLGA) NPs were produced by double emulsion-solvent evaporation method. The NPs were variously characterized for drug loading and release, particle profile, as well as by thermal analysis, x-ray difraction (XRD), Fourier transform infrared spectroscopy (FTIR) and nuclear magnetic resonance analysis (1H-NMR). Furthermore, the NPs were evaluated for cytotoxicity against NIH-3T3 cells by 3-(4,5-dimethylthiazol-2- Yl)-2,5-diphenyltetrazolium bromide (MTT) assay.Results: The DT-loaded NPs demonstrated nanostructural characteristics and extended drug release. Particle size was in the range of 243 and 295 nm which remained unchanged in drug stability testing in simulated gastrointestinal media. Encapsulation efficiency ranged from 49 – 64 % for all the formulations. Higuchi and Korsmeyer-Peppas were the best-fit release kinetic models for the NPs containing 5 and 10 % DT, respectively. The NPs with 10 % DT presented no significant cytotoxicty at the doses and periods studied.Conclusion: Stable and non-toxic DT NPs with potential for sustained and controlled release of the drug have been successfully developed.Keywords: Dexketoprofen trometamol, Poly-lactic-co-glycolic acid (PLGA), Nanoparticles, Release kinetics, Stability

Overcoming the Common Ion Effect for Weakly Basic Drugs: Inhibiting the Crystallization of Clofazimine Hydrochloride in Simulated Gastrointestinal Media

Bile salts, phospholipids, and digestive proteins are amphipathic compounds found naturally in the human gastrointestinal system. Therefore, it is important to consider their effects on the crystal...

Production of the Neurotoxin Salsolinol by a Gut-Associated Bacterium and Its Modulation by Alcohol.

Utilizing a simulated gastrointestinal medium which approximates physiological conditions within the mammalian GI tract, experiments aimed at isolating and identifying unique microbial metabolites were conducted. These efforts led to the finding that Escherichia coli, a common member of the gut microbiota, is capable of producing significant quantities of salsolinol. Salsolinol is a neuroactive compound which has been investigated as a potential contributor to the development of neurodegenerative diseases such as Parkinson’s disease (PD). However the origin of salsolinol within the body has remained highly contested. We herein report the first demonstration that salsolinol can be made in vitro in response to microbial activity. We detail the isolation and identification of salsolinol produced by E. coli, which is capable of producing salsolinol in the presence of dopamine with production enhanced in the presence of alcohol. That this discovery was found in a medium that approximates gut conditions suggests that microbial salsolinol production could exist in the gut. This discovery lays the ground work for follow up in vivo investigations to explore whether salsolinol production is a mechanism by which the microbiota may influence the host. As salsolinol has been implicated in the pathogenesis of PD, this work may be relevant, for example, to investigators who have suggested that the development of PD may have a gut origin. This report suggests, but does not establish, an alternative microbiota-based mechanism to explain how the gut may play a critical role in the development of PD as well other conditions involving altered neuronal function due to salsolinol-induced neurotoxicity.

Novel protein-lipid composite nanoparticles with an inner aqueous compartment as delivery systems of hydrophilic nutraceutical compounds.

Food protein and lipid based nanoparticles have attracted recent interest as a means of delivering nutraceuticals. Nanoparticle encapsulation of nutraceuticals faces challenges to overcome for it to be readily applied in the food industry, such as low encapsulation efficiency for hydrophilic compounds and poor stability once in the gastrointestinal tract. This research introduces a new protein-lipid composite nanoparticle with a three-layered structure (a barley protein layer, α-tocopherol layer and phospholipid layer) and an inner aqueous compartment to load hydrophilic nutraceuticals. This delivery system showed efficient encapsulation of vitamin B12 (69%) and controlled release behavior in simulated gastrointestinal media. An in vitro cell evaluation demonstrated that nanoparticles could internalize into Caco-2 cells via energy-dependent endocytosis and significantly increase the uptake and transport efficiency of vitamin B12 in this model. In vivo, the developed vitamin B12 loaded nanoparticle showed increased serum vitamin B12 levels upon oral administration and reduced the methylmalonic acid level more efficiently than the free form in rats. A 14-day in vivo toxicity study showed no evidence of toxicity in rats implying the safety of the developed nanoparticles in long term use. Overall, the results of this study show the great potential of the developed nanoparticles in increasing the absorption of vitamin B12 upon oral administration.

In vivo fate of lipid-silybin conjugate nanoparticles: Implications on enhanced oral bioavailability

Lipid-drug conjugates (LDCs) of a poorly soluble and poorly permeable drug silybin (SB) and lipids with different chain lengths (6C, 12C, 18C) are synthesized and formulated into solid lipid nanoparticles (SLNs). The in vivo fate of LDCs as well as SLNs is investigated by tracking either SB or LDCs or SLNs. LDCs are prone to be hydrolyzed by lipases either in simulated gastrointestinal media or in Caco-2 cell lines in a lipid chain length-dependent mode. The oral bioavailability of SB is enhanced by 5–7-fold in comparison with a fast-release formulation. No integral LDCs are detected in plasma confirms the readily degradable nature of LDCs. The absorption of LDCs by enteric epithelia and subsequent transportation into circulation might play a leading role in absorption enhancement, whereas the contribution of then M-cell pathway is not as remarkable. A shorter lipid chain favors earlier lipolysis and faster absorption along the intestine-to-circulation path.

Dissolution kinetics of polyphenol bearing calcium pectate hydrogels in simulated gastric or intestinal media and their anti-carcinogenic capacities

Cherry laurel is an underutilized agricultural resource with a significant content of polyphenolic compounds that potentially may demonstrate antioxidant and anti-carcinogenic activities. In this study, the preparation of calcium pectate gels bearing cherry laurel polyphenols was aimed and their dissolution behaviors in simulated gastric and intestinal media were tested. In addition, the released fractions were collected and tested in cell culture media in order to determine the anti-proliferative characteristics. Cherry laurel polyphenol extracts were mixed with pectin dispersions (1:1) and calcium pectate gels were prepared by the extrusion dripping method. The freeze dried gel samples were analyzed for morphological characteristics (SEM) and dissolution kinetics in simulated gastrointestinal media. The rate of release in gastric medium was substantial (≥94.9%) in all cases and dissolved fractions demonstrated significant anti-proliferative activity (approx. 85% inhibition for 55K06 and 61K04 extracts) against MCT 116 colon carcinoma cells even after 20× dilution. The findings were discussed with emphasis on their relevance to pectin-polyphenol interactions in dissolution behavior of the gels in simulated gastrointestinal media, and also to the preparation of functional lyophilizates that can be utilized in functional foods and pharmaceuticals.

Aminopropyl groups of the functionalized Mobil Crystalline Material 41 as a carrier for controlled diclofenac sodium and piroxicam delivery.

Objective:Synthetic Mobil Crystalline Material 41 (MCM-41) as a mesoporous material and functionalized MCM-41 using aminopropyl groups were studied in order to investigate their ability to encapsulate and to control the release of diclofenac sodium and piroxicam.Materials and Methods:MCM-41 was synthesized through sol–gel procedure and functionalized with aminopropyl groups. The physicochemical properties of MCM-41 were studied through particle size analysis, infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, and carbon–hydrogen–nitrogen analysis. Diclofenac sodium and piroxicam were loaded into the MCM-41 matrix using the filtration and solvent evaporation methods. The drug-loading capacity was determined by ultraviolet, Fourier transform infrared, X-ray diffraction, and Brunauer–Emmett–Teller analysis.Results:According to the results for pure drug release, >57% was released in the 1st h, but when these drugs were loaded into pure Mobil Crystalline Material 41 (MCM-41) and functionalized MCM-41, the release into the simulated gastrointestinal medium was less, continuous, and slower. The release of piroxicam from functionalized MCM-41 was slower than that from MCM-41 in the simulated intestinal medium because of the formation of electrostatic bonds between piroxicam and the aminopropyl groups of the functionalized MCM-41. However, in the case of diclofenac sodium, there was no significant difference between pure MCM-41 and functionalized MCM-41. The difference between piroxicam and diclofenac sodium was due to the high solubility of diclofenac sodium in the intestinal medium (pH 6.8), which caused more rapid release from the matrixes than for piroxicam.Conclusion:Our findings indicate that, after functionalization of MCM-41, it could offer a good means of delivering controlled diclofenac sodium and piroxicam.