Advanced interpenetrating polymer networks for innovative gastroretentive formulations targeting Helicobacter pylori gastric colonization.

The escalating challenges of Helicobacter pylori-induced gastric complications, driven by rising antibiotic resistance and persistent cancer risks, underscore the demand for innovative therapeutic strategies. This study addresses this urgency through the development of tailored semi-interpenetrating polymer networks (semi-IPN) serving as gastroretentive matrices for amoxicillin (AMOX). They are biodegradable, absorb significant volume of simulated gastric fluid (swelling index > 360 %) and exhibit superporous microstructures, remarkable mucoadhesion, and buoyancy. The investigation includes assessment at pH 1.2 for comparative analysis with prior studies and, notably, at pH 5.0, reflecting the acidic environment in H. pylori-infected stomachs. The semi-IPN demonstrated gel-like structures, maintaining integrity throughout the 24-hour controlled release study, and disintegrating upon completing their intended function. Evaluated in gastroretentive drug delivery system performance, AMOX release at pH 1.2 and pH 5.0 over 24 h (10 %-100 %) employed experimental design methodology, elucidating dominant release mechanisms. Their mucoadhesive, buoyant, three-dimensional scaffold stability, and gastric biodegradability make them ideal for accommodating substantial AMOX quantities. Furthermore, exploring the inclusion of the potassium-competitive acid blocker (P-CAB) vonoprazan (VONO) in AMOX-loaded formulations shows promise for precise and effective drug delivery. This innovative approach has the potential to combat H. pylori infections, thereby preventing the gastric cancer induced by this pathogen.

A Systematic Investigation of the Kinetic Models Applied to the Transport Behaviors of Aromatic Solvents in Unfilled Hydrogenated Nitrile Rubber/Ethylene Propylene Diene Monomer Composites.

Kinetic models of solvent transport behaviors are widely used in rubber-solvent systems, and some key points are still worthy of attention. In this work, the Korsmeyer-Peppas and Peppas-Sahlin models were chosen to fit the transport behaviors of three aromatic solvents, benzene, toluene and p-xylene, in the hydrogenated nitrile rubber (HNBR)/ethylene propylene diene monomer (EPDM)-based vulcanizates. The different effects of the various selected transport times (ti) used for fitting on the results of the mathematical models were compared. Moreover, a method to obtain the n parameter for the Korsmeyer-Peppas model and the m parameter for the Peppas-Sahlin model at ti = 0 was discussed. It was found that the differences in values of ti greatly influenced the impact on the fitting results of all the parameters for the two models. In addition, the n parameter for the Korsmeyer-Peppas model along with the m parameter for the Peppas-Sahlin model, which can characterize the transport mechanism, showed differing applicability. But the n and m parameters at ti = 0 obtained by linear fitting showed similar rules with some differences in values. These discussions give important guidance for the application of kinetic transport models in rubber-solvent systems.

Hyaluronic Acid-Alginate Homogeneous Structures with Polylactide Coating Applied in Controlled Antibiotic Release.

The use of a controlled-release drug carrier is an innovative solution for the treatment of local infections, in particular in dentistry, skin diseases, and in open wounds. The biocompatibility, biodegradability, the possibility of a large amount of drug adsorbed (especially those with hydrophilic properties), and the ability to create structures of any shape and size are the reasons for hydrogels to be frequently studied. The main disadvantage of hydrogel carriers is the rapid rate of drug release; hence, in this study, an attempt was made to additionally chemically cross-link 1-ethyl-3-(3-dimethyl aminopropyl)-1-carbodiimide hydrochloride (EDC) with the hyaluronic acid-alginate (HA-SAL) structure. The answer to significantly reduce the mass flux typical for hydrogel structure was to surround it with a polymer layer using a dry cover. By coating the carriers with polylactide, the release time was increased by around forty times. As the carriers were designed to reduce local bacterial infections, among others in dentistry, the released antibiotics were amoxycillin, metronidazole, and doxycycline.

Estimation of the Controlled Release of Antioxidants from ß-Cyclodextrin/Chamomile (Matricaria chamomilla L.) or Milk Thistle (Silybum marianum L.), Asteraceae, Hydrophilic Extract Complexes through the Fast and Cheap Spectrophotometric Technique.

This is the first study on the modeling of the controlled release of the estimated antioxidants (flavonoids or flavonolignans) from ß-cyclodextrin (ß-CD)/hydrophilic vegetable extract complexes and the modeling of transdermal pharmaceutical formulations based on these complexes using an overall estimation by the spectrophotometric method. The Korsmeyer-Peppas model was chosen for evaluating the release mechanisms. ß-CD/chamomile (Matricaria chamomilla L., Asteraceae) ethanolic extract and ß-CD/milk thistle (Silybum marianum L., Asteraceae) ethanolic extract complexes were obtained by the co-crystallization method with good recovering yields of 55-76%, slightly lower than for ß-CD/silibinin or silymarin complexes (~87%). According to differential scanning calorimetry (DSC) and Karl Fischer water titration (KFT), the thermal stability of complexes is similar to ß-CD hydrate while the hydration water content is lower, revealing the formation of molecular inclusion complexes. In the Korsmeyer-Peppas model, ß-CD/M. chamomilla flower extract complexes reveal Case II transport mechanisms, while the corresponding complexes with leaf extracts indicate non-Fickian diffusion for the controlled release of antioxidants in ethanol 60 and 96%. The same non-Fickian diffusion was revealed by ß-CD/S. marianum extract and ß-CD/silibinin complexes. On the contrary, almost all model transdermal pharmaceutical formulations based on ß-CD/M. chamomilla extract complexes and all those based on ß-CD/S. marianum extract complexes revealed non-Fickian diffusion for the antioxidant release. These results indicate that H-bonding is mainly involved in the diffusion of antioxidants into a ß-CD based matrix, while the controlled release of antioxidants in model formulations is mainly due to hydrophobic interactions. Results obtained in this study can be further used for studying the particular antioxidants (namely rutin or silibinin, quantified, for example, by liquid chromatographic techniques) for their transdermal transport and biological effects in innovatively designed pharmaceutical formulations that can be obtained using "green" methods and materials.

Nanosponges-based Drug Delivery System for the Cosmeceutical Applications of Stabilized Ascorbic Acid.

BACKGROUND: L-Ascorbic acid (AA) is a highly unstable compound, thus, limiting its use in pharmaceutical and cosmetic products, particularly at higher concentrations. OBJECTIVE: This study aimed to stabilize the highly sensitive molecule (AA) by encapsulating it in ß- cyclodextrin nanosponges (ß-CD NS) that can be used further in preparing cosmeceuticals products with higher AA concentrations and enhanced stability. METHODS: The NS has been synthesized by the melting method. The AA was encapsulated in ß-CD NS by the freeze-drying process. The prepared NS were characterized by FTIR spectrometry, SEM, Atomic Force Microscopy (AFM), zeta sizer, Differential Scanning Calorimetry (DSC), and the physical flow characteristics were also studied. The in vitro drug release was carried out on the Franz apparatus using a combination of two methods: sample & separate and dialysis membrane. The assay was performed using a validated spectrometric method. RESULTS: The entrapment efficiency of AA in ß-CD NS indicated a good loading capacity (83.57±6.35%). The FTIR, SEM, AFM, and DSC results confirmed the encapsulation of AA in ß-CD NS. The particle size, polydispersity index, and zeta potential results ascertained the formation of stabilized monodisperse nanoparticles. The physical flow characteristics showed good flow properties. Around 84% AA has been released from the NS in 4 h following the Korsmeyer-Peppas model. The AA-loaded NS remained stable for nine months when stored at 30±2°C/65±5% RH. CONCLUSION: It is concluded that the prepared NS can protect the highly sensitive AA from degradation and provide an extended-release of the vitamin. The prepared AA-loaded ß-CD NS can be used to formulate other cosmeceutical dosage forms with better stability and effect.

Drug-Polymers Composite Matrix Tablets: Effect of Hydroxypropyl Methylcellulose (HPMC) K-Series on Porosity, Compatibility, and Release Behavior of the Tablet Containing a BCS Class I Drug.

The purpose of this research was to see how the physicochemical properties and porosity of matrix tablets containing various types of hydroxypropyl methylcellulose (HPMC) K series affected the release of propranolol hydrochloride (PNL). PNL is a class I drug (high solubility and permeability) according to the Biopharmaceutics Classification System (BCS), making it an excellent model drug used for studying extended-release drug products. The direct compression method was used to prepare the HPMC-based matrix tablets. PNL and the excipients were found to be compatible using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). The surfaces of all the compressed HPMC-based matrix tablets were rough, with accumulated particles and small holes. The compressed HPMC-based matrix tablet porosity was also determined by using mercury porosimetry. The compressed HPMC-based matrix tablets made of low viscosity HPMC had tiny pores (diameter < 0.01 µm). The shorter polymeric chains are more prone to deformation, resulting in a small pore proportion. The compressed HPMC-based matrix tablets sustained the release of PNL for over 12 h. The release exponent values (n), which reflect the release mechanism of the drug from the tablets, ranged from 0.476 to 0.497. These values indicated that the release was governed by anomalous transport. The compressed HPMC-based matrix tablets have the potential for a sustained release of PNL.

Effect of squalane-based emulsion on polyphenols skin penetration: Ex vivo skin study.

Polyphenols have gained attractiveness as ingredients in cosmetic formulations as result of their ability to delay the aging process. However, different factors limit their use, including low solubility and poor skin permeability. In this sense, this study describes the potential of squalane to increase the polyphenols ex vivo skin penetration, incorporated into a water-in-oil emulsion. Polyphenols skin permeation followed the Fick's first law and, p-coumaric acid, vitexin, schaftoside and ferulic acid had the higher permeability coefficients (Kp = 6.0-8.0 × 10-3 cm-2 h-1). Addition of squalane to phenolic compounds decreased the permeability coefficients (Kp = 4.1-5.9 × 10-3 cm-2 h-1), indicating that squalane increased the retention of polyphenols in the skin. Gentisic acid, ferulic acid, and p-coumaric acid were the only compounds permeating from water-in-oil emulsion, in the first 8 h of study and, according Krosmeyer-Peppas model, its n value was > 1 indicating a high transport resistance from the formulation and throughout the skin. Results suggest squalane as an efficient vehicle to increase the dermal availability increasing phenolic compounds physiological functions, by enhancing the skin retention time where they should exert antiaging effect.

Characterization and release kinetics model of thymol from starch-based nanocomposite film into food simulator.

To improve the performance of potato starch films and solve the problems of high volatility and low stability of thymol (Thy), thymol was loaded into the channel of SBA-15 to prepare Thy-SBA-15, and the Thy-SBA-15/potato starch film was prepared. The results showed thymol was successfully loaded into the pores of SBA-15. The addition of Thy-SBA-15 enhanced the tensile strength of potato starch film (3.93 Mpa), reduced the water vapor permeability (1.56 × 10-12  g·d-1  m-1  Pa-1 , WVP) and moisture absorption (80.97%, MA), which enhanced the barrier properties of the films. Thy-SBA-15 had good compatibility with potato starch films. Notably, the thymol released from Thy-SBA-15/potato starch film was initially explosive, and then continuous, which showed this film could effectively slow down the release rate of thymol and prolong the fresh-keeping period of food. The Korsmeyer-Peppas model M t M ∞ = k t n (R2  > .96) had the best fit for the release curve of thymol. PRACTICAL APPLICATIONS: This work offers a new method for the preparation of potato starch sustained-release antibacterial film, and provides a theoretical basis and technical support for the development of intelligent packaging.

Silver-fluoropolymer (Ag-CFX) films: Kinetic study of silver release, and spectroscopic-microscopic insight into the inhibition of P. fluorescens biofilm formation.

Silver-fluoropolymer (Ag-CFX) composed of encapsulated bioactive nanophases within a thin polymer coating are promising antimicrobial films with excellent bioactivity. In this contribution, we report on Ag-CFX thin films obtained by ion beam co-sputtering, accurately tuning film thickness, and inorganic loading. The Ag-CFX films were characterized by spectroscopic and scanning probe microscopy techniques with respect to composition and swelling behavior. Next to electrothermal atomic absorption spectroscopy (ETAAS) studies, scanning electrochemical microscopy (SECM) experiments in combination with anodic stripping voltammetry (ASV) were carried out to study the release mechanism of silver(I) from the embedded silver nanoparticles (AgNPs). Silver(I) concentration profiles at the Ag-CFX films in contact with water resulted in a release of 1310 ± 50 µg L-1 (n = 3) after 27 h of immersion and corresponded well to the swelling of the films. The antimicrobial properties towards biofilm formation of P. fluorescens were studied by attenuated total reflection Fourier-transform infrared (ATR-FTIR) spectroscopy during a period of 48 h. The obtained IR data revealed biofilm inhibition due to the presence of the antimicrobial layer but also indicated potential surface re-colonization after 30 h of contact with the bacteria-containing solution. The occurrence of cyclic changes in the characteristic IR bands correlated with apparent stress of bottom-layered bacteria, along with re-colonization on top of dead biomass, indicative of potential cannibalism events.

Mild Hyperthermia Responsive Liposomes for Enhanced In Vitro and In Vivo Anticancer Efficacy of Doxorubicin against Hepatocellular Carcinoma.

The current study is aimed to fabricate doxorubicin (Dox) loaded mild temperature responsive liposomes (MTLs) by thin film hydration technique for enhanced in vitro and in vivo anticancer efficacy against hepatocellular carcinoma. The aforementioned Dox loaded MTLs were developed and optimized with extrusion and drug loading techniques. The optimized MTLs were in optimum size range (118.20 ± 2.81-187.13 ± 4.15 nm), colloidal stability (-13.27 ± 0.04 to -32.34 ± 0.15 mV), and enhanced entrapment of Dox (28.71 ± 2.01-79.24 ± 2.16). Furthermore, the optimized formulation (MTL1-E(AL)) embodied improved physicochemical stability deducted by Fourier transform infra-red (FTIR) spectroscopy and mild hyperthermia-based phase transition demonstrated from differential scanning calorimetry (DSC). An in vitro drug release study revealed mild hyperthermia assisted rapid in vitro Dox release from MTLs-E(AL) (T100% ≈ 1 h) by Korsmeyer-Peppas model based Fickian diffusion (n < 0.45). Likewise, an in vitro cytotoxicity study and lower IC50 values also symbolized mild hyperthermia (40.2 °C) based quick and improved cytotoxicity of MTL1-E(AL) in HepG2 and MCF-7 cells than Dox. The fluorescence microscopy also represented enhanced cellular internalization of MTL1-E(AL) at mild hyperthermia compared to the normothermia (37.2 °C). In addition, an in vivo animal study portrayed the safety, improved anticancer efficacy and healing of hepatocellular carcinoma (HCC) through MTL1-E(AL). In brief, the Dox loaded MTLs could be utilized as safe and effective therapeutic strategy against HCC.

Ion release from hydroxyapatite and substituted hydroxyapatites in different immersion liquids: in vitro experiments and theoretical modelling study.

Multi-substituted hydroxyapatites (ms-HAPs) are currently gaining more consideration owing to their multifunctional properties and biomimetic structure, owning thus an enhanced biological potential in orthopaedic and dental applications. In this study, nano-hydroxyapatite (HAP) substituted with multiple cations (Sr2+, Mg2+ and Zn2+) for Ca2+ and anion ( Si O 4 4 - ) for P O 4 3 - and OH-, specifically HAPc-5%Sr and HAPc-10%Sr (where HAPc is HAP-1.5%Mg-0.2%Zn-0.2%Si), both lyophilized non-calcined and lyophilized calcined, were evaluated for their in vitro ions release. These nanomaterials were characterized by scanning electron microscopy, field emission-scanning electron microscopy and energy-dispersive X-ray, as well as by atomic force microscope images and by surface specific areas and porosity. Further, the release of cations and of phosphate anions were assessed from nano-HAP and ms-HAPs, both in water and in simulated body fluid, in static and simulated dynamic conditions, using inductively coupled plasma optical emission spectrometry. The release profiles were analysed and the influence of experimental conditions was determined for each of the six nanomaterials and for various periods of time. The pH of the samples soaked in the immersion liquids was also measured. The ion release mechanism was theoretically investigated using the Korsmeyer-Peppas model. The results indicated a mechanism principally based on diffusion and dissolution, with possible contribution of ion exchange. The surface of ms-HAP nanoparticles is more susceptible to dissolution into immersion liquids owing to the lattice strain provoked by simultaneous multi-substitution in HAP structure. According to the findings, it is rational to suggest that both materials HAPc-5%Sr and HAPc-10%Sr are bioactive and can be potential candidates in bone tissue regeneration.

Antibiotic Loaded Nano Rod Bone Cement for the Treatment of Osteomyelitis.

BACKGROUND: Polymethyl Methacrylate (PMMA) bone cement is the clinical gold standard biomaterial for local antibiotic therapy in osteomyelitis. However, it releases 50% of the antibiotic within the first three days. It generates excessive heat during polymerization and is non-biodegradable. It must be removed by another operation. The best-known alternative for PMMA is hydroxyapatite. OBJECTIVES: The present patented work is focused on synthesizing the biodegradable hydroxyapatite in nano form for slow and sustained release of antibiotics and studying the release kinetics of antibiotics. METHODS: Nano-hydroxyapatite was synthesized by co-precipitation method and characterized by particle size analyser, transmission electron microscopy, fourier transform infrared spectroscopy and energy dispersive X-Ray analysis. Antibiotic loaded nano-hydroxyapatite was prepared as 7 mm beads. The efficiency of drug-loaded nano-hydroxyapatite beads against osteomyelitic isolates was evaluated by well diffusion assay. Zero-order, first order, second order, Higuchi model, Korsmeyer-Peppas and Gompertz models were fit into the release kinetics of antibiotics from hydroxyapatite. RESULTS: Average size of nano-hydroxyapatite was 5 nm. The bactericidal activity exhibited by antibiotic- loaded micro-sized hydroxyapatite was therapeutic until 10 days only, whereas antibiotic-loaded nano-hydroxyapatite was therapeutic until 8 weeks. This confirms the burst release of antibiotics from micro-sized hydroxyapatite beads. In contrast, the release was slow and sustained up to 8 weeks from nano-hydroxyapatite. Korsmeyer-Peppas model fits into the release kinetics of antibiotics from nanohydroxyapatite. CONCLUSION: Nano-hydroxyapatite with a Ca/P ratio of 1.78 is suitable for the slow and sustained delivery of antibiotics for 8 weeks.

Understanding the burst release phenomenon: toward designing effective nanoparticulate drug-delivery systems.

Burst release of encapsulated drug with release of a significant fraction of payload into release medium within a short period, both in vitro and in vivo, remains a challenge for translation. Such unpredictable and uncontrolled release is often undesirable, especially from the perspective of developing sustained-release formulations. Moreover, a brisk release of the payload upsets optimal release kinetics. This account strives toward understanding burst release noticed in nanocarriers and investigates its causes. Various mathematical models to explain such untimely release were also examined, including their strengths and weaknesses. Finally, the account revisits current techniques of limiting burst release from nanocarriers and prioritizes future directions that harbor potential of fruitful translation by reducing such occurrences.

Interpreting non-linear drug diffusion data: Utilizing Korsmeyer-Peppas model to study drug release from liposomes.

The aim of this work was to clarify the dynamics behind the influence of ionic strength on the changes in drug release from large unilamellar vesicles (LUVs). For this purpose, we have investigated the transport of two different model drugs (caffeine and hydrocortisone) formulated into liposomes through different types of barriers with different retention properties (regenerated cellulose and the newly introduced biomimetic barrier, Permeapad®). Drug release from liposomes was studied utilizing the standard Franz diffusion cells. LUV dispersions were exposed to the isotonic, hypotonic and hypertonic environment (difference of 300 mOsm/kg between the initial LUVs and the environment) and experimental data treated with both linear and non-linear (Korsmeyer-Peppas) regression models. To alter the rigidity of the liposomal membranes, cholesterol was introduced in the liposomal barriers (up to 25% w/w). Korsmeyer-Peppas model was proven to be suited to analyse experimental data throughout the experimental time frame, providing important additive information in comparison to standard linear approximation. The obtained results are highly relevant as they improve the interpretation of drug release kinetics from LUVs under osmotic stress. Moreover, the findings can be utilized in the development of liposomal formulations intended for nose-to-brain targeted drug delivery.

Monodisperse Fe3O4/SiO2 and Fe3O4/SiO2/PPy Core-Shell Composite Nanospheres for IBU Loading and Release.

The magnetic targeting drug delivery system is an effective way of targeting therapy. In this study, the monodisperse Fe3O4 nanoparticles with a particles size of about 180 nm were first prepared via a solvothermal method. Subsequently, the core-shell structure Fe3O4/SiO2 and Fe3O4/SiO2/polypyrrole (PPy) composite nanospheres were successfully synthesized by coating Fe3O4 nanoparticles with SiO2 shell layer using the Stöber method and PPy shell by solvothermal method in turn. The as-prepared nanoparticles were characterized using transmission electron microscopy (TEM), X-ray diffraction (XRD), Fourier transform-infrared spectroscopy (FT-IR), vibrating sample magnetometer (VSM), thermogravimetric analysis (TGA), and Ultraviolet-Visible spectrophotometer (UV-Vis). The results indicated that the as-prepared composite nanospheres displayed a well-defined core-shell structure and monodispersity. The thicknesses of SiO2 shell and PPy shell were ~6 nm and ~19 nm, respectively. Additionally, the as-prepared nanoparticles exhibited high saturation magnetization of 104 emu/g, 77 emu/g, and 24 emu/g, and have great potential applications in drug delivery. The drug loading and drug release of the Fe3O4/SiO2 and Fe3O4/SiO2/PPy composite nanospheres to ibuprofen (IBU) under stirring and ultrasonication were investigated. Their drug loading efficiency and drug release efficiency under ultrasonication were all higher than 33% and 90%, respectively. The drug release analyses showed sustained release of IBU from nanospheres and followed the Korsmeyer-Peppas model.

In-vitro release of fragrant l-carvone from electrospun poly(ϵ-caprolactone)/wheat cellulose scaffold.

The release kinetics of l-carvone loaded from electrospun poly(ϵ-caprolactone) (PCL) and Wheat cellulose (WC) blend were studied. WC was extracted from wheat straw, a cost effective agricultural waste by the acid hydrolysis method. A homogeneous solution of PCL-WC (13:3wt%) was optimized to produce beadless electrospun PCL-WC blend nanofibers. Further, WC and the prepared electrospun PCL-WC blend fibers were systematically characterized by ATR-FTIR, SEM, XRD, TGA, DTGA, and DSC measurements. The hydrophilic character of the blend fibers was analysed using swelling tests and contact angle measurements. The loading efficiency of l-carvone into the electrospun PCL-WC blend fibers was evaluated to be ∼70%. The in-vitro release of l-carvone from PCL-WC blend fibers followed Korsmeyer-Peppas kinetic model indicating the diffusion mechanism and the maximum release of l-carvone was found to be ∼84% over a period of 30h. These results would offer the prepared PCL-WC blend as an ideal fibrous mesh for fragrant antimicrobial textile applications.

Determination and characterization of metronidazole-kaolin interaction.

The needs for safe, therapeutically effective antidiarrheal combination continuously lead to effective treatment. When administered simultaneously, metronidazole-kaolin interactions have been reported by FDA but not studied. This paper is the first to study metronidazole-kaolin interactions. Adsorption isotherms of a metronidazole-kaolin antidiarrheal combination from aqueous solutions at an in vivo simulated pH conditions were obtained at 37 ± 0.5 °C. Langmuir constants for the adsorption are 10.8225, 41.3223 mg g(-1) and 11.60, 2.56 l g(-1) aimed at the monolayer capacity, and the equilibrium constant at pH 1.2 and 6.8, respectively. pH effect on adsorption of known concentration of metronidazole by kaolin was also studied over the range 1.2-8. A gradual increase in the adsorbed amount was noted with increasing the pH. Elution studies by different eluents showed that drug recovery from adsorbent surface was pH-dependent via competitive mechanism. The elution followed the sequence: 0.1 M HCl > 0.1 M NaCl > H2O. Adsorption-desorption studies revealed physical adsorption. The equilibrium concentration of metronidazole decreased as the adsorbent concentration was increased in the systems. The dissolution profiles (USP) of commercially available tablets (Riazole® 500 mg) were obtained alone and in the presence of either (ORS®) rehydration salts and 9 or 18 g of kaolin powder. The percentage drug released versus time: 95.01% in 25 min, 101.02% in 30 min, 67.63% in 60 min, 60.59% in 60 min, respectively. The percentage drug released versus time was increased with ORS® due to common ion effect [Cl(-)], while, it was decreased with kaolin due to adsorption. The mechanism of reaction of Riazole® (500 mg) tablets in the different dissolution media, confirms with Korsmeyer-Peppas model. The interaction between metronidazole and kaolin was characterized by melting point determinations, differential scanning calorimetry analysis and infrared spectroscopy. The results obtained were suggestive of physical interaction between metronidazole and kaolin.

Formulation of a modified release metformin. HCl matrix tablet: influence of some hydrophilic polymers on release rate and in-vitro evaluation / A formulação de uma matriz de libertação modificada de comprimido de metformin.HCl: influência de alguns polímeros hidrofílicos sobre a taxa de libertação e de avaliação in-vitro

Metformin hydrochloride is an antidiabetic agent which improves glucose tolerance in patients with type 2 diabetes and reduces basal plasma levels of glucose. In this study, a simplex centroid experimental design with 69 runs was used to select the best combination of some hydrophilic polymers that rendered a 24 h in-vitro release profile of metformin.HCl. The Korsmeyer-Peppas model was used to model the dissolution profiles since it presented the best fit to the experimental data. Further, a cubic model predicted the best formulation of metformin.HCl containing polyvinyl pyrrolidone, ethyl cellulose, hydroxypropyl methyl cellulose, carrageenan, sodium alginate, and gum arabic at 6.26, 68.7, 6.26, 6.26, 6.26 and 6.26 percent levels, respectively. The validation runs confirmed the accuracy of the cubic model with six components for predicting the best set of components which rendered a once-a-day modified release hydrophilic matrix tablet in compliance with the USP specifications.

O cloridrato de metformina é um agente antidiabético que melhora a tolerância à glicose em pacientes com diabetes tipo 2 e reduz os níveis plasmáticos basais de glicose. Neste estudo, um projeto experimental do tipo "centróide simplex" com 69 tomadas foi usado para selecionar a melhor combinação de alguns polímeros hidrofílicos que gerou um perfil de liberação da metformina.HCl de 24 horas. O modelo Korsmeyer-Peppas foi usado para modelar os perfis de dissolução, uma vez que apresentou os melhores ajustes aos dados experimentais. Além disso, um modelo cúbico previu a melhor formulação de metformina.HCl sendo aquela contendo polivinilpirrolidona, etilcelulose, hidroxipropilmetil celulose, carragena, alginato de sódio e goma arábica nos níveis 6.26, 68.7, 6.26, 6.26, 6.26 e 6.26 por cento, respectivamente. As corridas de validação confirmaram a precisão do modelo cúbico com os seis componentes para prever o melhor conjunto de componentes que originou uma libertação do tipo "uma vez ao dia" em conformidade com as especificações da USP, a partir de comprimidos matriciais.