Controlled Release Of Ibuprofen Research Articles

6-Carboxycellulose Acetate Butyrate: Effectiveness as an Amorphous Solid Dispersion Polymer.

Amorphous solid dispersion (ASD) in a polymer matrix is a powerful method for enhancing the solubility and bioavailability of otherwise crystalline, poorly water-soluble drugs. 6-Carboxycellulose acetate butyrate (CCAB) is a relatively new commercial cellulose derivative that was introduced for use in waterborne coating applications. As CCAB is an amphiphilic, carboxyl-containing, high glass transition temperature (Tg) polymer, characteristics essential to excellent ASD polymer performance, we chose to explore its ASD potential. Structurally diverse drugs quercetin, ibuprofen, ritonavir, loratadine, and clarithromycin were dispersed in CCAB matrices. We evaluated the ability of CCAB to create ASDs with these drugs and its ability to provide solubility enhancement and effective drug release. CCAB/drug dispersions prepared by spray drying were amorphous up to 25 wt % drug, with loratadine remaining amorphous up to 50% drug. CCAB formulations with 10% drug proved effective at providing in vitro solubility enhancement for the crystalline flavonoid drug quercetin as well as ritonavir, but not for the more soluble APIs ibuprofen and clarithromycin and the more hydrophobic loratadine. CCAB did provide slow and controlled release of ibuprofen, offering a simple and promising Long-duration ibuprofen formulation. Formulation with clarithromycin showed the ability of the polymer to protect against degradation of the drug at stomach pH. Furthermore, CCAB ASDs with both loratadine and ibuprofen could be improved by the addition of the water-soluble polymer poly(vinylpyrrolidone) (PVP), with which CCAB shows good miscibility. CCAB provided solubility enhancement in some cases, and the slower drug release exhibited by CCAB, especially in the stomach, could be especially beneficial, for example, in formulations containing known stomach irritants like ibuprofen.

Investigation of controlled drug release of ibuprofen with prepared and characterized innovative bigel materials

AbstractNew systems called bigels have been discovered recently, alongside other consolidations of hydrogels and organogels. The purpose of this research is to develop bigels using span 40, alginate, centaury oil, black cumin oil and sorbitan monopalmitate for controlled ibuprofen release. Characterization of prepared materials was performed using various analysis by fourier transform infrared spectroscopy and differential scanning calorimetry. The pH 7.2 level was used for the swelling test of bigels. Cytocompatibility of bigels was determined by using human immortalized human keratinocyte cells. Bigels have been tested for their effectiveness as controlled medication delivery formulations by in vitro studies. The prepared bigels did not show any toxic effects on human cells. This indicates that the prepared materials were biocompatible. For controlled drug release kinetics, zeroth‐order, first‐order, Higuchi, and Korsmeyer‐Peppas kinetic models were used. According to results, the kinetic modeling of bigels by Korsmeyer‐Peppas is also highly compatible. Consequently, controlled drug release was successfully carried out by the novel bigel materials formed by adding an active ingredient. Our results clearly indicate that bigels have been an alternative potential material for controlled drug delivery systems by the properties of biocompatibility, slower release of the drug and the diffusion release mechanism.

Controlled ibuprofen release from Pickering emulsions stabilized by pH-responsive cellulose-based nanofibrils

Pickering emulsions represent a promising avenue in the field of controlled drug delivery systems. Recently, cellulose nanofibers (CNFs) and chitosan nanofibers (ChNFs) have gained interest as eco-friendly stabilizers for Pickering emulsions, yet their application in pH-responsive drug delivery systems remains unexplored. However, the potential of these biopolymer complexes in formulating stable, pH-responsive emulsions for controlled drug release is of significant interest. Here, we show the development of a highly stable, pH-responsive fish oil-in-water Pickering emulsion stabilized by ChNF/CNF complexes, with optimal stability achieved at a 0.2 wt% ChNF concentration and an average emulsion particle size of approximately 4 μm. Our results demonstrate long-term stability (16 days of storage) for ChNF/CNF-stabilized emulsions, with the interfacial membrane's pH modulation facilitating controlled, sustained ibuprofen (IBU) release. Furthermore, we observed a remarkable release of approximately 95 % of the embedded IBU within the pH range of 5–9, while the drug loading and encapsulation efficiency of the drug-loaded microspheres reached their peak at a 1 % IBU dosage, with values of 1 % and 87 %, respectively. This study highlights the potential of using ChNF/CNF complexes in designing versatile, stable, and entirely renewable Pickering systems for controlled drug delivery, with potential applications in food and eco-friendly products.

Improvement of mesoporous silica nanoparticles: A new approach in the administration of NSAIDS

Nonsteroidal anti-inflammatory drugs (NSAIDs) constitute a heterogeneous group of compounds that exhibit analgesic, anti-inflammatory and antipyretic activity. However, the GI damage produced by NSAIDs has been widely studied. Thus, the aim of the present study was the development of mesoporous silica nanoparticles in order to increase the capacity of drug transport, emphasizing those with low solubility such as NSAIDs. The morphology and structure characteristics of the synthesized nanoparticles were studied by transmission electron microscopy (TEM), besides, its particle size, surface charge, specific area and cell viability will be determined. The analytical application of mesoporous silica nanoparticles as ibuprofen carrier was also evaluated by measuring their drug loading characteristics and release behavior. The results showed that the synthesized NPs had efficient physicochemical characteristics, high EE%, low toxicity, and controlled ibuprofen release.

Localized delivery of ibuprofen via a bilayer delivery system (BiLDS) for supraspinatus tendon healing in a rat model

The high prevalence of tendon retear following rotator cuff repair motivates the development of new therapeutics to promote improved tendon healing. Controlled delivery of non-steroidal anti-inflammatory drugs to the repair site via an implanted scaffold is a promising option for modulating inflammation in the healing environment. Furthermore, biodegradable nanofibrous delivery systems offer an optimized architecture and surface area for cellular attachment, proliferation, and infiltration while releasing soluble factors to promote tendon regeneration. To this end, we developed a bilayer delivery system (BiLDS) for localized and controlled release of ibuprofen (IBP) to temporally mitigate inflammation and enhance tendon remodeling following surgical repair by promoting organized tissue formation. In vitro evaluation confirmed the delayed and sustained release of IBP from Labrafil-modified poly(lactic-co-glycolic) acid microspheres within sintered poly(ε-caprolactone) electrospun scaffolds. Biocompatibility of the BiLDS was demonstrated with primary Achilles tendon cells in vitro. Implantation of the IBP-releasing BiLDS at the repair site in a rat rotator cuff injury and repair model led to decreased expression of proinflammatory cytokine, tumor necrotic factor-α, and increased anti-inflammatory cytokine, transforming growth factor-β1. The BiLDS remained intact for mechanical reinforcement and recovered the tendon structural properties by 8 weeks. These results suggest the therapeutic potential of a novel biocompatible nanofibrous BiLDS for localized and tailored delivery of IBP to mitigate tendon inflammation and improve repair outcomes. Future studies are required to define the mechanical implications of an optimized BiLDS in a rat model beyond 8 weeks or in a larger animal model.

FORMULATION AND EVALUATION OF IBUPROFEN CONTROLLED RELEASE MATRIX TABLETS USING ITS SOLID DISPERSION

Objective: The aim of the present work was to prepare solid dispersion of ibuprofen with PEG 6000 to increase the aqueous solubility of the drug and to develop the solid dispersed ibuprofen into tablet formulation with the combination of a hydrophilic and hydrophobic polymer to attain controlled release of ibuprofen.
 Methods: Solid dispersion of ibuprofen was prepared by melting-solvent method by varying the ratio of drug and PEG 6000. The solid dispersed ibuprofen was subjected to tablet formulation by using a hydrophilic swellable polymer-carbopol and hydrophobic non-swellable polymer-ethyl cellulose. The release of the drug from the polymer matrix was studied as the polymer ratio changes.
 Results: Compatibility between drug and polymers was established from FT-IR study. The saturated solubility was found to increase in the solid dispersed formulation. The swelling index was found within the range of 90±5.43 to 137±6.41. SEM image of swollen tablet confirmed the presence of irregular and porous surface. The cumulative drug release was found to vary within the range of 68.76±3.04 to 95.33±2.34 % after 8 h of dissolution.
 Conclusion: The combination of solid dispersion and application of hydrophilic and hydrophobic polymers in matrix formation can facilitate better dissolution and absorption profile with greater patient compliance.

Electrospun PLGA Nanofiber Scaffolds Release Ibuprofen Faster and Degrade Slower After In Vivo Implantation.

While delayed delivery of non-steroidal anti-inflammatory drugs (NSAIDs) has been associated with improved tendon healing, early delivery has been associated with impaired healing. Therefore, NSAID use is appropriate only if the dose, timing, and mode of delivery relieves pain but does not impede tissue repair. Because delivery parameters can be controlled using drug-eluting nanofibrous scaffolds, our objective was to develop a scaffold for local controlled release of ibuprofen (IBP), and characterize the release profile and degradation both in vitro and in vivo. We found that when incubated in vitro in saline, scaffolds containing IBP had a linear release profile. However, when implanted subcutaneously in vivo or when incubated in vitro in serum, scaffolds showed a rapid burst release. These data demonstrate that scaffold properties are dependent on the environment in which they are placed and the importance of using serum, rather than saline, for initial in vitro evaluation of biofactor release from biodegradable scaffolds.

Bi-directional controlled release of ibuprofen and Mg2 + from magnesium alloys coated by multifunctional composite

Two major problems for magnesium alloy implant are the high degradation rate and easy infection associated with implantation. Herein, a surface drug delivery system (Mg/Epoxy resin-ZnO/PCL-Ibuprofen) which can realize bi-directional controlled release of ibuprofen and Mg2+ was designed via a dip coating process followed by spraying. The in vitro test demonstrated that the ibuprofen in drug-eluting compound material showed sustained release profiles for 22days, which can effectively solve the local cellular rejection and inflammation during the early stage of implantation. Besides, the drug carrier also exhibited improved corrosion resistance duel to the high combining strength between Epoxy resin-ZnO coating and magnesium alloy, so Mg2+ can release slowly at first and then speeded up later. This approach may be suitable for coating other implant materials such as stainless steel, titanium alloy etc.

PH-responsive ordered mesoporous carbons for controlled ibuprofen release

Nitrogen-doped ordered mesoporous carbons (N-OMCs) were synthesized by nanocasting using SBA-15 silica as template and two polyaramide precursors: m-aminobenzoic acid (MABA) and p-aminobenzoic acid (PABA). The structure of the resulting materials was greatly influenced by the precursor used, since MABA yielded a CMK-3 type OMC, while PABA gave a CMK-5 one. Both carbons displayed differences in texture, structure and surface chemistry. These were reflected in a different pH dependence of ibuprofen adsorption and release. Although the two carbons exhibited a good behavior as drug adsorbents, the PABA-derived one was more efficient, in terms of drug delivery, than the carbon prepared from MABA, which was associated to the surface chemical nature and tube-like structure of the former. The desorption kinetics of both carbons presented an initial fast stage, reach the maximum ibuprofen delivery in 300min and the maximum drug concentration level remained constant up to 24h. Moreover, the carbons also exhibited a specific response toward the pH, which was associated to their different surface chemical and textural properties. This pH-responsive property was more evident for the PABA derived carbon, which allowed a sustained drug level of 10wt.% at pH=2 and of almost 40wt.% at pH=7.4.

Synthesis of Straight Rod-Shaped Mesoporous Silica Templated with Polyvinylpyrrolidone and P123 for Controlled Ibuprofen Release

Straight rod-shaped mesoporous silica materials (SRMS) were successfully prepared using polyvinylpyrrolidone and triblock copolymer as dual template, which would be further functionalized with (3-aminopropyl) triethoxysilane. SRMS and functionalized SRMS (NH-SRMS) were characterized by means of small-angle X-ray powder diffraction, field emission scanning electron microscopy, transmission electron microscopy, N2adsorptiondesorption. The results indicated that SRMS was straight rod-shaped mesoporous silica with a hexagonal symmetry structure (p6mm) and the structure did not change after functionalization. A comparative study of the loading and release of ibuprofen on the carriers of SRMS and NH-SRMS were carried out in phosphate buffered saline. NH-SRMS exhibited a lower release rate than SRMS, suggesting that NH-SRMS was a promising carrier for achieving prolonged drug release.

Controlled-release of ibuprofen on multilayer mesoporous vesicle

A concentric multilayer vesicle with mesoporous channels in each layer was synthesized and used as a drug carrier. The average size of the vesicles was about 100–300nm, with the cavities of an average distance of about 7nm between every two layers, and the mesoporous channels of an average diameter of 3.4nm in each layer. Ibuprofen was selected as the drug model to investigate the vesicle's loading and releasing performance. The vesicle showed a fast loading with the ibuprofen capacity (weight ratio of ibuprofen to material) of 30% within 2h, and a slow controllable release during about 15h. The Weibull model can be successfully used to describe the release performance. The analysis results demonstrated that fast loading and slow release of the vesicle were mainly attributed to its mesoporous multilayer structure.

Biofunctional mesoporous silica nanoparticles for magnetically oriented target and pH-responsive controlled release of ibuprofen

A dual-stimuli-responsive drug delivery system, with magnetic oriented target and pH-sensitive characters, has been prepared. The materials show highly ordered mesostructure, high pore volume, regular nanoparticle morphology (500nm), and superior magnetic property. The materials were characterized by XRD, TEM, BET, FTIR and vibrating sample magnetometer technique (VSM). The pH-sensitive magnetic mesoporous silica nanoparticles (MMSNs) was served as a drug carrier, with ibuprofen (IBU) being the model drug. The release kinetics in simulated gastric fluid (SGF, pH 1.2) and in simulated proximal intestine fluid (SIF, pH 7.4) were studied respectively. It is found that the drug release increased rapidly when the release medium was changed from SGF to SIF. These dual-functional drug delivery systems with magnetically oriented target and pH-responsive performances may predictably have application in biomedical field.

New solid lipid microparticles for controlled ibuprofen release: Formulation and characterization study

A hot melt dispersion method was used to prepare new sustained release ibuprofen composite microparticles of a solid lipid at ambient temperature, cetyl alcohol. The dispersion of colloidal silicon dioxide nanoparticles (hydrophilic Aerosil ® 200 or hydrophobic Aerosil ® R974) either in the oily phase or in the aqueous phase led to the preparation of large (about 400 μm diameter) surfactant free free-flowing particles. Mapping-scanning electronic microscopy using silicon probe revealed that silicon was in the oily core in all cases. The nature of silica nanoparticles and the way used for their dispersion influenced the internal structure of the composite microparticles and the aggregation of nanoparticles in the core of the microparticles. Hydrophobic Aerosil ® R974 allowed the formation of homogeneous microparticles. Although silica nanoparticles had no influence on thermic profile, crystalline state of ibuprofen and lipid, they had an influence on the kinetics drug release related to the increase of the size of the composite solid lipid microparticles prepared.

The effect of isopropanol addition on enhancement of transdermal controlled release of ibuprofen from ethylene vinyl acetate copolymer membranes

AbstractThis work reports the study of the addition of isopropanol on controlled release of ibuprofen from ethylene vinyl acetate (EVAc) copolymer membranes. An EVAc solution in cyclohexane (4% w/v) containing triethyl citrate (7% w/v) as plasticizer was mixed with ibuprofen at three different concentrations of 4, 6, and 8%. Isopropanol was mixed with each of the previous mixtures to form solutions of 1, 3, and 5% isopropanol concentrations. Samples were solvent cast on glass petri‐dishes to form membranes. Home‐made diffusion cells were used for in vitro study. These cells were composed of two compartments, donor (exposed to ambient conditions), and receptor (including buffer solution maintained at 37°C). Each cell was equipped with a sampling port and water in and out system. An ultraviolet spectrometer at 222 nm was used to measure release rates of obtained membranes. The diffusion mechanism for drug release was examined by zero‐order, first‐order, Higuchi and Korsmeyer‐Peppas theories to confirm the obtained membranes follow the matrix‐type system. By increasing the drug concentration from 4 to 8%, drug release (cumulative amount) was improved from 20 (47.5%) to 30 (36%) μg/cm2 after 24 h. Addition of 5% isopropanol to the above samples (4 and 8% loading) further increased drug release to 24 and 43 μg/cm2. Results were in good agreement with the Korsmeyer‐Peppas theory for samples with 4 (% w/w) of ibuprofen. The highest percentage of drug release after 24 h was 59% for the sample with 4% drug loading compared to 50% for the sample with 8% drug loading, both with 5% isopropanol. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011

Etomidate, Transfusion, and Vasospasm

Object. Leukocyte-endothelial cell interactions may play a role in the development of cerebral vasospasm after aneurysmal subarachnoid hemorrhage (SAH) because the extravasation of circulating leukocytes into the periadventitial space within 24 hours after the hemorrhage appears to be a critical event in this process. Ibuprofen is an antiinflammatory agent that inhibits the expression of specific cell adhesion molecules and, consequently, disrupts leukocyte-endothelial cell interactions. The authors investigated the efficacy of ibuprofen delivered locally from controlled-release polymers in the rabbit basilar artery (BA) model of cerebral vasospasm. Methods. Ibuprofen was incorporated into controlled-release ethylene-vinyl acetate copolymer (EVAc) constituting 45% of the resulting polymer by weight. Fifty-four New Zealand White rabbits were randomized to 10 groups: sham operation (seven animals); SAH only (seven animals); and SAH plus either empty EVAc or ibuprofen-EVAc polymer at 30 minutes or 6, 12, or 24 hours (five animals per group; 40 total). The rabbits were killed 72 hours after induction of SAH, at the time of maximal vasospasm. The efficacy of ibuprofen in preventing vasospasm was assessed by measuring lumen patency of the rabbit's BAs. The intracranial controlled release of ibuprofen resulted in a significant inhibition of vasospasm when treatment was initiated at 30 minutes (patency 92.3 ′ 5.1% compared with 52.1 ′ 5.1% in animals given empty EVAc; p < 0.001) and 6 hours (patency 69.5 ′ 3.5% compared with 47.2 ′ 1.5% in animals given empty EVAc; p < 0.03) after blood deposition compared with treatment with empty EVAc. No effect was observed when treatment was begun at either 12 or 24 hours. Conclusions. Local intracranial delivery of ibuprofen accomplished using controlled-release polymers prevents vasospasm in the rabbit BA model of vasospasm when administered within 6 hours after blood exposure.

Inhibition of cerebral vasospasm by intracranial delivery of ibuprofen from a controlled-release polymer in a rabbit model of subarachnoid hemorrhage.

Leukocyte-endothelial cell interactions may play a role in the development of cerebral vasospasm after aneurysmal subarachnoid hemorrhage (SAH) because the extravasation of circulating leukocytes into the periadventitial space within 24 hours after the hemorrhage appears to be a critical event in this process. Ibuprofen is an antiinflammatory agent that inhibits the expression of specific cell adhesion molecules and, consequently, disrupts leukocyte-endothelial cell interactions. The authors investigated the efficacy of ibuprofen delivered locally from controlled-release polymers in the rabbit basilar artery (BA) model of cerebral vasospasm. Ibuprofen was incorporated into controlled-release ethylene-vinyl acetate copolymer (EVAc) constituting 45% of the resulting polymer by weight. Fifty-four New Zealand White rabbits were randomized to 10 groups: sham operation (seven animals); SAH only (seven animals); and SAH plus either empty EVAc or ibuprofen-EVAc polymer at 30 minutes or 6, 12, or 24 hours (five animals per group; 40 total). The rabbits were killed 72 hours after induction of SAH, at the time of maximal vasospasm. The efficacy of ibuprofen in preventing vasospasm was assessed by measuring lumen patency of the rabbit's BAs. The intracranial controlled release of ibuprofen resulted in a significant inhibition of vasospasm when treatment was initiated at 30 minutes (patency 92.3 +/- 5.1% compared with 52.1 +/- 5.1% in animals given empty EVAc; p < 0.001) and 6 hours (patency 69.5 +/- 3.5% compared with 47.2 +/- 1.5% in animals given empty EVAc; p < 0.03) after blood deposition compared with treatment with empty EVAc. No effect was observed when treatment was begun at either 12 or 24 hours. Local intracranial delivery of ibuprofen accomplished using controlled-release polymers prevents vasospasm in the rabbit BA model of vasospasm when administered within 6 hours after blood exposure.

Controlled release injectable liposomal gel of ibuprofen for epidural analgesia

The epidural administration is used commonly in the treatment of pain. Nonsteroidal anti-inflammatory drugs, especially ibuprofen, would have potential in epidural use. Like many epidurally useful drugs it, however, has a short duration of action, which is a limiting factor. To improve epidural pain treatment, a long-acting, single-dose gel injection is being developed. In the present study, the possibility of using liposomal systems to control the release and dural permeation of ibuprofen was investigated in vitro. Liposomal solutions of ibuprofen·Na (20 mg/ml) were prepared by high-pressure homogenization from egg phosphatidylcholine. The liposomal gel consisted of poloxamer 407 and the liposomal solution. No signs in the 1H-NMR spectroscopy of line broadenings or chemical shifts were observed. The liposomal formulations were reproducible and stable. Ibuprofen release in phosphate buffer, pH 7.4, at 37°C from the liposomal solution and the liposomal gel were prolonged significantly compared with their respective solution and gel controls. The liposomal gel controlled ibuprofen release and dural permeation in vitro and showed a permeation pattern favourable for maintaining constant drug levels. The liposomal poloxamer gel represents a new formulation approach to increase the local epidural availability of ibuprofen. It appeared to be a promising injectable controlled-release drug delivery system.

Inhibition of experimental vasospasm in rats with the periadventitial administration of ibuprofen using controlled-release polymers.

The chronic phase of vasospasm after an aneurysmal subarachnoid hemorrhage may be mediated in part by early leukocyte-endothelial cell interactions. Ibuprofen is an anti-inflammatory agent that inhibits expression of certain cell adhesion molecules and therefore disrupts leukocyte-endothelial cell interactions. Its systemic administration, however, has dose-limiting side effects. We evaluated the effect of the periadventitial delivery of ibuprofen using controlled-release polymers in the rat femoral artery model of chronic posthemorrhagic vasospasm. Before the animal studies, the release pharmacokinetics of the ibuprofen-loaded ethylene-vinyl acetate polymers were determined in vitro. Subsequently, the femoral arteries (n=266) of Fischer 344 rats (n=133) were enclosed in latex pouches bilaterally. In the toxicity study (n=15 rats), the animals were randomized into 5 dose groups in which 0%-, 10%-, 20%-, 30%-, or 50%-loaded ibuprofen polymers were evaluated. In the efficacy study, the animals were randomized into 5 time groups in which 50%-loaded ibuprofen polymers were inserted at 0 (n=58 rats), 6 (n=16), 12 (n=13), 24 (n=11), or 48 hours (n=12) after blood injection into the pouch. The rats were killed 12 days after blood exposure, at the time of maximal vasospasm in this model. Vasospasm was expressed as percent lumen patency. To evaluate the effect of ibuprofen on leukocyte migration, 8 rats were randomized into 2 groups. Macrophages and granulocytes were stained by immunohistochemistry with the use of a mouse OX-41 monoclonal antibody and counted in the periadventitial space 24 hours after blood exposure. In vitro pharmacokinetics showed that the 50%-loaded ibuprofen polymer released its total drug load over a 12-day period. In the toxicity study, a nonsignificant arterial vasodilatation with ibuprofen treatment was seen at higher doses, and no deleterious effects were noted on the vessel wall histologically. In the efficacy study, ibuprofen treatment resulted in significant vasospasm inhibition when treatment was initiated at 0 hour (73.7+/-4.9% versus 94.5+/-3.3% [mean+/-SEM percent lumen patency]; P<0.001) and 6 hours (69.2+/-5.7% versus 98.0+/-3.9%; P=0. 002) after blood exposure, but not at 12, 24, or 48 hours. Leukocyte immunohistochemistry showed that ibuprofen treatment resulted in significantly lower periadventitial macrophage and granulocyte counts of 25.0+/-3.9 cells per high-powered field compared with counts of 140.5+/-18.2 cells per high-powered field in the untreated vessels (P<0.001). The periadventitial, controlled release of ibuprofen from surgically implanted polymers significantly inhibits chronic posthemorrhagic vasospasm in this model when treatment is initiated within 6 hours of blood exposure. Vasospasm inhibition with ibuprofen correlates with a significant decrease in the number of macrophages and granulocytes in the periadventitial space. This study supports the hypothesis that inflammation mediates in part the chronic phase of posthemorrhagic vasospasm and suggests a potential alternative treatment for this condition.

Polymeric drugs derived from ibuprofen with improved antiinflammatory profile.

A new methacrylic monomeric compound bearing Ibuprofen (MIA) and the respective polymethacrylic macromolecular derivative (polyMIA) were evaluated for antiinflammatory properties in order to study their pharmacological activity profile. The macromolecular drug is constituted of Ibuprofen residues linked covalently to a polymethacrylic support, as a side substituent of the repeating unit, by means of a spacer group (p-aminophenoxy) that, in addition, is the most representative metabolite of Paracetamol. The Ibuprofen is slowly released from the polymeric support by hydrolysis of the ester bond in a biological medium. Different antiinflammatory testing methods were used; and the results obtained indicate that the monomeric and polymeric forms display higher potency to inhibit acute inflammatory processes than the traditional Ibuprofen form, even doubling the power of Ibuprofen. In addition, they present higher activity against chronic experimental processes, as well as an excellent antinociceptive behavior to inhibit the pain associated with arthritic diseases. According to previous reports and results presented in this article, we can conclude that the new polymethacrylic structures show higher analgesic, antipiretic, and antiinflammatory activities due to the possible activity of the macromolecular drug as well as to the controlled Ibuprofen release from the macromolecular delivery system. After releasing of the side active residue, a derivate of poly(sodium methacrylate) is formed, which is cleared from the body easily by the normal pathway of kidney metabolism.