Eudragit RS Research Articles

FLUID PROPERTIES OF COMPONENTS FOR DEVELOPMENT OF EUDRAGIT RS-BASED IN SITU-FORMING GEL AND MICROPARTICLE AND THEIR PHASE INVERSIONS

Solvent exchange-induced in situ-forming gel (isg) and in situ-forming microparticles (ism) have been currently applied as drug delivery approaches for periodontitis treatment. Doxycycline hyclate-loaded Eudragit RS-based isg and ism were prepared in this study. The basic properties such as density, pH, surface/interfacial tension of their solvents including dimethyl sulfoxide (DMSO), N-methyl pyrrolidone (NMP), and 2-pyrrolidone (PYR) in Eudragit RS solution and oils (olive oil and camellia oil) were assessed. This research also tested for apparent viscosity of solvent and drug-free and doxycycline hyclate-loaded ERS-based isg and ism, and their phase transformation rates. Density of PYR was higher than that of DMSO whereas these solvents exhibited the less wettability than oils on glass slide. All fabricated doxycycline hyclate-loaded Eudragit RS-based ism formulations showed good emulsion physical stability with no phase separation for 1 hour. The apparent viscosity of ism was significantly less than that of isg. DMSO-based isg and ism exhibited a significantly less viscosity than that of PYR-based formulations. Rapid phase inversion was evident after isg and ism exposure to agarose gel indicating fast solvent exchange. The loose barrier of camellia oil from its less viscosity facilitated a water diffusion inward Eudragit RS-based ism easier than using viscous olive oil. Solvent exchange-induced doxycycline hyclate-loaded Eudragit RS-based ism using DMSO as the solvent and camellia oil as the continuous phase exhibited various appropriate physicochemical characteristics for applying as drug delivery system for periodontitis treatment.

Formulation Development and Evaluation of Floating Microspheres of Curcumin

Purpose – There are several approaches that have been developed in order to increase the gastric residence time (GRT) floating drug delivery system is one of them. Floating microspheres improve the bioavailability and releasing for long period of time. In the current investigation curcumin floating microspheres are being developed to extend the drug release. Method - Emulsion solvent evaporation approach is used for development of floating microspheres by using Eudragit RS100, HPMC K100, Ethyl Cellulose as polymers. Acetone and Ethanol was used as a solvent in a ratio of 10:5. Stirring speed of mechanical stirrer was 900rpm. Result - There was no reaction between the drug and excipients according to FTIR analysis. The developed microspheres have virtually spherical shapes and particle size range was between 200 - 420µm. The effectiveness of the drug entrapment was found between 60 - 98.4%. It was found that the buoyancy was between 70 - 92%. The in-vitro drug release was found to be 99.5 of batch 15. The developed microspheres indicated prolonged drug release of 12hrs. The optimized batch was B15. Conclusion - According to results of the research, developing gastro-retentive floating microspheres of curcumin using the emulsion solvent evaporation method with HPMC K100, Eudragit RS100, and ethyl cellulose is a promising method.

Tri-Layer Core-Shell Fibers from Coaxial Electrospinning for a Modified Release of Metronidazole.

Polymers are the backbone of drug delivery. Electrospinning has greatly enriched the strategies that have been explored for developing novel drug delivery systems using polymers during the past two decades. In this study, four different kinds of polymers, i.e., the water-soluble polymer poly (vinyl alcohol) (PVA), the insoluble polymer poly(ε-caprolactone) (PCL), the insoluble polymer Eudragit RL100 (ERL100) and the pH-sensitive polymer Eudragit S100 (ES100) were successfully converted into types of tri-layer tri-polymer core-shell fibers through bi-fluid coaxial electrospinning. During the coaxial process, the model drug metronidazole (MTD) was loaded into the shell working fluid, which was an emulsion. The micro-formation mechanism of the tri-layer core-shell fibers from the coaxial emulsion electrospinning was proposed. Scanning electron microscope and transmission electron microscope evaluations verified the linear morphology of the resultant fibers and their obvious tri-layer multiple-chamber structures. X-ray diffraction and Fourier transform infrared spectroscopy measurements demonstrated that the drug MTD presented in the fibers in an amorphous state and was compatible with the three polymeric matrices. In vitro dissolution tests verified that the three kinds of polymer could act in a synergistic manner for a prolonged sustained-release profile of MTD in the gut. The drug controlled-release mechanisms were suggested in detail. The protocols reported here pioneer a new route for creating a tri-layer core-shell structure from both aqueous and organic solvents, and a new strategy for developing advanced drug delivery systems with sophisticated drug controlled-release profiles.

Moxifloxacin loaded microspheres-composed gel for controlled release and enhanced penetration in ocular tissues: In vitro, ex vivo and in vivo proof of concept

Microspheres-enriched ocular gels are proposed in this work for the loading of a model quinolone antibiotic of broad-spectrum - moxifloxacin hydrochloride (MXF) - as an approach to achieve a controlled release profile and enhance drug's bioavailability in ocular milieu. MXF is a synthetic fluoroquinolone antibacterial agent used for treatment of ocular diseases caused by strains of aerobic gram positive and gram-negative bacteria, besides others. MXF-loaded Eudragit RS microspheres were prepared by emulsion solvent evaporation method, as previously described by us. Optimized microspheres were characterized and then formulated in an ocular gel. Hydrophilic polymeric base HPMC K100 was used as gelling agent. Ocular gel enriched with microspheres was evaluated for its physicochemical parameters, in vitro drug release, ex vivo corneal and scleral permeation and bioadhesion, in vivo primary eye irritation and in vivo efficacy study. The developed MXF microspheres dispersed in an ocular gel showed an in vitro drug release over a period 12 h, improved corneal and scleral penetration and increased therapeutic efficacy with a reduced administration frequency which may contribute to increase patient's compliance to ocular treatment.

Formulation and Evaluation of Topical Microsponge Based Gel of Clotrimazole

The study's overarching goal is to develop a novel medication delivery method based on microsponge gel containing clotrimazole. Clotrimazole is poorly absorbed from the gastrointestinal tract (GIT), has a short half-life of only 2 h, & is metabolized into inert molecules by the liver. Therefore, clotrimazole's drug delivery method must be modified for topical application. Microsponge delivery is a novel approach to sustained drug release. Microsponges were made with a polymer solution of Eudragit RS 100 in dichloromethane (DCM) and ethanol (1:1) using a quasi-emulsion solvent diffusion technique. A number of metrics, including production yield, entrapment efficiency, particle size measurement, and in vitro drug release studies, were used to each microsponge formulation. For topical administration, the optimized microsponge formulation F6 was transformed into a gel formulation. Prepared gel was compared to a commercially available formulation based on physical factors such as pH, viscosity, spreadability, drug content, and an in vitro diffusion investigation. Most of the formulations were discrete and spherical in shape, indicating a satisfactory production yield, suggesting quasi-emulsion solvent diffusion method is a promising methodology for the fabrication of microsponge. Clotrimazole was released steadily over the course of 12 hours from the microsponge gel formulation MGI (F6). Therefore, the medicine in the form of a microsponge can reduce the risk of adverse effects and increase patient compliance by avoiding skin contact.

Development and evaluation of matrix type transdermal patches of Simvastatin

Transdermal patches are a cutting-edge drug delivery technology, as it avoids first-pass metabolism results in increased bioavailability and aid in the delivery of drug molecules into the systemic circulation at predetermined and controlled rate. Aim behind this invention was to formulate a stable, reproducible and non-infringing & examine matrix-type transdermal patches of Simvastatin by using solvent evaporation method and the formulation consist various polymer including HPMC, Ethyl Cellulose, Chitosan, PVPK-30 and Eudragit RS 100, plasticizers like glycerine, propylene glycol, and trietholamine are utilised, along with solvents like octanol and ethanol. The prepared patches are assessed for thickness, weight variation, folding endurance, moisture content, drug content, surface pH and in vitro diffusion studies. The results indicated that the formulation P4 showed better characteristic properties and in vitro drug diffusion. Keywords: Transdermal drug delivery system, Simvastatin, HPMC, Eudragit RS100, Ethyl Cellulose.

Optimization and In Vitro Evaluation of Curcumin-loaded Calcium Alginate Microbeads using Box-Behnken Design for Colorectal Cancer

Background and Objective:: After lung cancer and breast cancer, colorectal cancer (CRC) is the third most common type of cancer and has the second-highest fatality rate. Curcumin is one such naturally occurring dietary compound that demonstrated promise to treat colon cancer. For that, the goal of the current study was to coat curcumin with Eudragit S100 to treat colorectal cancer in the distal intestine release. The multiparticulate dosage form can increase the solubility of curcumin in the colon environment, sustain the drug release, and protect the drug from abrupt degradation in the colon environment. All of these alterations can enhance the colon tissue levels, especially in the colon cancer cells in the patients, and thereby can enhance the utility of the therapy. Methods:: By using the ionotropic gelation technique, the formulations were made. Moreover, Design Expert 13 used a three-factor, three-level Box-Behnken design (BBD) in this work to optimize the formulation for colon-targeted drug delivery. The concentration of potassium alginate, the concentration of calcium chloride, and the curing duration were considered independent variables, and prepared microbeads were refined to study their impacts on entrapment effectiveness and particle size. Eudragit S100 was enteric coated on Calcium alginate beads with an improved core. Results:: Regarding particle size and entrapment effectiveness, respectively, the polymer concentration and curing duration had a substantial impact. The ideal concentrations of calcium chloride and potassium alginate were 15% w/v and 6% w/v, respectively, with a 20-minute curing time. With a drug entrapment efficiency of 88.4%, the improved formulation had particles with a size of 708 μm. After 12 hours, 79.23±0.32% of the drug was released following an enteric coating of Eudragit S100 of optimized calcium alginate microbeads (10% weight gain). Conclusion:: The present study conclusively demonstrates the usefulness of a Box-Behnken design in the optimization of colon-targeted formulations. To effectively treat colorectal cancer, enteric-coated calcium alginate microbeads can be administered orally to deliver curcumin precisely to the colon.

D-optimal mixture design inspired modified release tablet formulation of lamotrigine for the treatment of seizures: An in-depth characterization

Lamotrigine (LTG) an anticonvulsant drug with a dissociation constant (pKa: 5.7), suffers from enhanced blood plasma spike after each dose, when administered as fast release tablet. Being BCS class-II candidate and pH dependent solubility, development of release-controlled tablets of LTG is a major challenge. This investigation aims at designing the release-controlled tablet (RCT) formulation of LTG using a solid dispersion (SD) technique via addressing its solubility and release problems. RCT of LTG was fabricated using SD blend of Eudragit RL and Eudragit RS and PVP K-30 with different polymer blend ratio (1:5 and 1:7). The optimization of RCT of LTG was performed using D-optimal mixture design with three independent variables, three response variables, and one constraint. The dissolution rate was determined and data were then fitted to different mathematical models. Scanning electron microscopy (SEM) and X-ray diffraction (XRD) studies and tableting parameters were analyzed. In vitro studies of predicted optimized batches (POBs) have shown that drug release over a period of 12hours was 88.05±3.4% in media I, 86.10±3.7% in media II and 85.84±4.2% in media III. An in vitro kinetic model equating R2-value for all the tested models indicated that the first order and Higuchi release kinetics model were the most appropriate. Based on the optimized formulation consisting of SD of LTG with Eudragit RL, Eudragit RS and PVP K-30, the release rate was consistently similar throughout the GI tract, regardless of the pH of the environment.

Quality by Design-driven Development of 5-fluorouracil Loaded Mucoadhesive Microparticulate Drug Delivery Systems for Effective Chemotherapy for Colorectal Cancer

Aims: To enhance oral bioavailability and decrease the dosing frequency of 5-Fluorouracil Background: Cancer is one of the most dreadful diseases for which complete cures are not possible, but colorectal cancer is completely curable if diagnosed at an early stage. If diagnosed in late-stage, 5-Fluorouracil (5-FU) is mostly recommended for its effective treatment, but the challenges associated with this drug are short elimination half-life, severe side effects, as well as non-specificity. The challenges can be better addressed by fabricating microbeads using the QbD approach. To enhance the oral bioavailability of 5-FU and to target the colon for the effective treatment of colorectal cancer, the microbeads were fabricated by emulsification crosslinking method using Box-Behnken design. Objective: To target the colon for effective treatment of colorectal cancer with enhanced oral bioavailability. Methods: The microparticulate drug delivery system was fabricated by using the emulsification crosslinking method by implementing a quality design approach with risk assessment followed by characterization such as FTIR, DSC, TGA, XRD, in vitro drug release, in vitro cytotoxicity study and in vivo pharmacokinetic studies. Results: The patient-centric quality target product profile (QTPP) was set. QTPP inspired critical quality attributes (CQAs) were searched out. The critical material attributes (CMAs) and critical process parameters (CPPs) influencing CQAs were distinguished. The seventeen formulations were fabricated employing Box Behnken Design, followed by optimization using numerical and graphical optimization techniques and the optimized microbeads were subjected to in vivo pharmacokinetic and in vitro cytotoxicity studies using HT 29 cell lines. The results revealed that 5-FU-loaded microbeads exhibited significantly more cytotoxic, and bioavailability was found to be nearly doubled as compared to pure drugs. Conclusion: 5-FU-loaded microbeads can be developed and optimized successfully by using quality by design approach and coating with eudragit S100, which can be targeted to the colon for the effective treatment of colorectal cancer.

PH-Sensitive Nanoparticles for Colonic Delivery Anti-miR-301a in Mouse Models of Inflammatory Bowel Diseases.

Though the anti-miR-301a (anti-miR) is a promising treatment strategy for inflammatory bowel disease (IBD), the degradability and the poor targeting of the intestine are a familiar issue. This study aimed to develop a multifunctional oral nanoparticle delivery system loaded with anti-miR for improving the targeting ability and the therapeutic efficacy. The HA-CS/ES100/PLGA nanoparticles (HCeP NPs) were prepared using poly (lactic-co-glycolic acid) copolymer (PLGA), enteric material Eudragit®S100 (ES100), chitosan (CS), and hyaluronic acid (HA). The toxicity of nanoparticles was investigated via the Cell Counting Kit-8, and the cellular uptake and inflammatory factors of nanoparticles were further studied. Moreover, we documented the colon targeting and pharmacodynamic properties of nanoparticles. The nanoparticles with uniform particle size exhibited pH-sensitive release, favorable gene protection, and storage stability. Cytology experiments showed that anti-miR@HCeP NPs improved the cellular uptake through HA and reduced pro-inflammatory factors. Administering anti-miR@HCeP NPs orally to IBD mice markedly reduced their pro-inflammatory factors levels and disease activity indices. We also confirmed that anti-miR@HCeP NPs mostly accumulated in the colon site, and effectively repaired the intestinal barrier, as well as relieved intestinal inflammation. The above nanoparticle is a candidate of the treatment for IBD due to its anti-inflammatory properties.

Colon-Targeted Delivery of Indole Acetic Acid Helps Regulate Gut Motility by Activating the AHR Signaling Pathway.

Intestinal peristalsis is vital for gastrointestinal physiology and host homeostasis and is frequently dysregulated in intestinal disorders. Gut microbiota can regulate gut motility, especially through the tryptophan metabolism pathway. However, the role of indoles as microbial tryptophan metabolites in colonic function requires further exploration. Here, we show that the delivery of indole acetic acid (IAA) targeting the colon can improve gut motility by activating the aryl hydrocarbon receptor (AHR). To achieve colon-targeted delivery, Eudragit S-100 (ES) and chitosan (CS) were used as drug carriers. After optimisation, IAA-loaded ES-coated CS nanoparticles exhibited an encapsulation efficiency of 83% and a drug-loading capacity of 16%. These nanoparticles exhibited pH-dependent characteristics and remained stable in acidic conditions and the upper intestine. In simulated intestinal fluid (pH 7.4) and colonic lumen, considerable amounts of IAA were released after approximately 4 h. Compared with free IAA, the nanoparticles exerted enhanced therapeutic effects on gut movement disorders induced by loperamide. The efficacy of IAA treatment was attributable to the activation of the AHR signalling pathway and increased levels of AHR agonists. Furthermore, the oral administration of IAA-loaded nanoparticles promoted serotonin secretion and maintained the intestinal barrier function. The experimental outcomes demonstrate the efficiency of the proposed colon-specific delivery system and highlight the role of IAA, produced by gut microbiota metabolism, in regulating gut peristalsis through AHR activation.

FORMULATION AND EVALUATION OF GASTRO-RETENTIVE MICROSPHERE OF SAXAGLIPTIN ANTIDIABETIC AGENT

The objective of this study was to develop a gastro-retentive microsphere of Saxagliptin. Saxagliptin is an orally active hypoglycemic drug of the newdipeptidylpeptidase-4(DPP4) inhibitor class of drug. Nine formulations of Saxagliptin microsphere are prepared by Emulsion solvent diffusion method using polymers like Eudragit RS 100 and Ethyl cellulose at different drug to polymer ratios and Polyvinyl Alcohol as Stabilizing agent by Emulsion Solvent Diffusion Method. The formulations were optimized on the basis of percent buoyancy and in vitro drug release. The prepared microspheres were evaluated for physicochemical parameters and found to be within range. KEYWORDS: Gastro retentive, Saxagliptin, Ethyl cellulose, Floating microsphere, Eudragit RS 100, Polyvinyl alcohol

Fabrication, design, and in vivo investigation of mesoporous silica-based docetaxel trihydrate nanoparticles for colonic drug delivery

BackgroundMesoporous silica-loaded docetaxel trihydrate nanoparticles are the potential to target drug delivery toward a specific region with high stability and predictable release at the target region. They have large surface areas and mesoporous structures with large pore volumes, leading to high bioavailability and therapeutic efficacy at the disease site. This study demonstrates how nanoparticles can be prepared using an emulsion technique.ResultsThe ratios of eudragit S100 to eudragit L100 polymers, along with phosphatidylcholine, were varied according to the response surface methodology. Differential scanning colorimetry and fluorinated transmitted infrared spectroscopy studies showed that mesoporous silica particles were successful. All formulations had average particle sizes ranging from 70.65 to 143.01 nm, with a range of zeta potential from 17.6 ± 026 to 21 ± 011. In vitro drug delivery studies were achieved for all formulations with a zeta potential of 17.6 ± 026 to 21 ± 011. As per the statistical optimization by RSM that response model for percentage drug loading (Y1) was found to be 0.0002 which is p-value < 0.05. Hence, the model is significance. Accordingly percentage drug release at 6 h. (Y2) p-value was found to be 0.0001 and percentage drug release at 10 h (Y3) p-value was found to be 0.0002, respectively. So all the models are significant. After oral administration of the docetaxel, plasma levels were measured in vivo bioavailability testing of docetaxel. Docetaxel nanosuspension had a significantly higher Cmax amount than docetaxel microsuspension (98.03 ± 23.40 ng/ml and 213.67 ± 72.21 ng/ml, respectively, with tmax 45 min). Docetaxel was more bioavailable in nanosuspension formulations, according to a bioavailability test of rats.ConclusionThe results suggested that the mesoporous silica could be a great potential nanocarrier in colonic delivery with optimal drug content and controlled release docetaxel trihydrate.

Quality by Design Approach for Optimization of Microbial and pH-Triggered Colon-Targeted Tablet Formulation Using Carboxymethyl Tamarind Gum.

ABSTRACT The purpose of this study was to apply the quality by design (QbD) approach in the development of a microbial and pH-triggered colon-targeted budesonide tablet. A retrospective research strategy was used to select various polysaccharide-based natural gums such as tamarind gum, gellan gum, karaya gum, gum ghutti, and khaya gum, which were then evaluated for their effectiveness in microbial degradation and targeting the colon. Viscosity profiles were generated in the presence of a prebiotic culture medium prepared by using the Velgut capsule that mimicked the impact of 4% rat cecal content and helpful in screening of natural polymer. Based on the cumulative drug release data of preliminary batches, carboxymethyl (CM) tamarind gum was identified as a superior and an excellent polymer over the tamarind gum for formulation development. The presence of water as a bridging agent in wet granulation also played an important role in the retardation of drug release. Tablets were supercoated with the enteric polymer, Eudragit S100. The Box-Behnken design was utilized, where the selected independent variables were the proportion of CM tamarind gum, % water proportion, and % weight gain of Eudragit S 100 to optimize the formulation. The optimized design space was generated with the criteria that a drug release should be of less than 5% within the first 2 h, less than 10% within the first 5 h, and more than 70% within the first 8 h, to achieve colon targeting. The optimized batch F3 was found stable as per International Council for Harmonisation guidelines. The roentgenography study for optimized formulation demonstrated that it remained intact for 5 h and, at 7 h, was disseminated completely. CM tamarind gum is efficient for colon targeting, and its proportion in 100 mg along with an enteric coating of 6% led to the optimized formulation.

QbD: A novel approach for formulation and optimization of colon targeted drug delivery system containing mebeverine HCl

The aim of the work is to study the programmed release of model antispasmodic drug Mebeverine HCl based on pulsatile principle to target colon proximity. Compression coated tablets included core tablet consisting of Croscarmellose as super disintegrant and pulsatile layer comprising impermeable Ethocel cup and mixture of Keltone, Eudragit S100, Ethocel as swellable and rupturable layer. The prepared core tablet was evaluated for weight variation, hardness, thickness, friability, drug content, disintegration time and in vitro dissolution studies. For optimization Box-Behnken design was employed to study the effect of independent variables viz., weight ratio of Keltone (X1), Eudragit S100 (X2), Ethocel (X3) on dependent variables viz., t10 (Y1), t50 (Y2) and Q12 (Y3). Results revealed positive influence of independent factors on responses. The data were statistically analyzed using ANOVA and were found to be statistically significant (P &lt; 0.05). Mathematical modeling for kinetic studies revealed that the release profile after lag time followed first order kinetics. The results concluding that a successful pulsatile drug delivery system of Mebeverine HCl was developed.

Formulation and Evaluation of Colon Targeted Ciprofloxacin Microspheres

In the present study, Colon-targeted Ciprofloxacin hydrochloride microspheres were formulated and their in vitro properties were assessed to determine whether or not the antibiotic could be delivered to the colon. By utilizing span-80 as an emulsifying agent, ciprofloxacin hydrochloride microspheres for colon targeting were prepared using the emulsion-solvent evaporation method. According to the preliminary trial findings, the ratio of drug to polymer had an impact on the microspheres' properties. The Ciprofloxacin: Eudragit S-100+HPMC 6cps ratio of 1:1, 1:2, 1:3, 1:4, 1:5, and 1:6 were used to make the colon targeting microspheres, in which the ratio of Eudragit S-100 to HPMC was always 1:1. The combination of Eudragit S-100 and HPMC demonstrated increased release lag time and regulated release rate, which improved protection of the drug-containing core. For the majority of the formulations examined, zero-order release followed a time delay caused by the hydrogel's swelling/retarding behaviour before the medication started to come out of the microspheres. The colon-targeting microspheres were also tested for micrometrics, particle size and surface properties, percentage drug content, encapsulation effectiveness, and in vitro drug release study in the three different pH environments (0.1 N HCL, Phosphate buffer pH 6.8 and Phosphate buffer pH 7.4) for 12 hours. The kinetics of drug release in vitro and the drug release mechanism of the microspheres were further investigated. With a particle size of 58.9 m, an almost spherical shape, and free-flowing characteristics, the best formulation batch had the highest drug entrapment efficiency of 86.81%. It was followed by a zero-order rate release with a non-fiction-diffusion mechanism, which had an 82.77% drug release rate.

Fabrication, Characterization and in vitro Evaluation of Prednisolone Sustained Release Multiparticulate System for Colonic Targeting

Background: Prednisolone (PRD) is orally prescribed for inflammatory bowel syndrome (IBS) as the upper GIT is the main site of absorption; therefore, long-term PRD dosing decreases therapeutic effectiveness through systemic side effects. Objective: This work focused on formulating sustained-release alginate beads as a multiparticulate system for colon targeting using prednisolone (PRD) to be filled in an HPMC capsule. Methods: PRD beads were prepared by the ionotropic gelation technique using sodium alginate as the primary polymer and inulin, guar gum, and pectin as secondary polymers. In addition to the impact of polymer type and quantity, other factors were investigated: The CaCl2 concentration and tween 80 addition Thirteen formulations were successfully prepared, and their properties, such as bead size, morphology, percentage of encapsulation efficiency, yield, DL, in vitro release study in GIT buffer media, IBS media, SEM, and FTIR, were assessed. Results: The study showed that the beads were close in size, and the size was not an obstacle for loading the beads in HPMC capsules. Further, yield%, EE%, and DL% increased according to the bead’s content increase. Conclusions: The optimum formula was F3 that coated HPMC capsules with Eudragit S-100, which gave sustained release profiles in GIT and IBS simulating media, and F13 that could last the release in different pH media, pH 1.2, 6.8, and 7.4.

Delivery of short chain fatty acid butyrate to overcome Fusobacterium nucleatum-induced chemoresistance

The gut microbiota is closely associated with the progression of colorectal cancer (CRC) in which Fusobacterium nucleatum (F. nucleatum) was found to induce cancer resistance to chemotherapeutics. To relieve F. nucleatum-induced drug resistance, herein, we found that short-chain fatty acid butyrate can inhibit the growth, enrichment and adhesion of F. nucleatum in colorectal cancer tissues by downregulating the expression of adhesion-associated outer membrane proteins, including RadD, FomA, and FadA, to reduce the colonization and invasion of F. nucleatum and relieve the chemoresistance induced by F. nucleatum. Leveraging the killing effect of butyrate on F. nucleatum, sodium butyrate (NaBu) was encapsulated in liposomes or prepared as NaBu tablets with Eudragit S100 coating and administered by intravenous injection or oral administration, respectively. Interestingly, both intravenous administration of NaBu liposomes and oral delivery of NaBu tablets could effectively inhibit the proliferation of F. nucleatum and significantly improve the therapeutic efficacy of oxaliplatin in mice with subcutaneous colorectal tumors, orthotopic colorectal tumors and even spontaneously formed colorectal tumors. Thus, our work provides a simple but effective formulation of NaBu to relieve F. nucleatum-induced chemoresistance, exhibiting ideal clinical application prospects.

Retracted: Development of a hydrogel containing metronidazole-loaded Eudragit RS 100 nanoparticles for buccal drug delivery

This article previously published in Volume 22 Issue 6 of this journal in June 2023 has been retracted in line with the guidelines from the Committee on Publication Ethics (COPE, http://publicationethics.org /resources /guidelines). This was a follow up to the report by somebody identified as VU Nguyen (email: nguyenvu81@protonmail.com) of the duplicate publication of an article earlier published in 2020 (available at http://125.212.201.8:6008 / ViewOnline?bitstid=0d585588-2d02-4839-907a-92998674bb4d &amp; type=1) in Vietnamese where a figure and some text in the article were repeated in the article published in this journal.&#x0D; This action was taken after thorough investigation of the plagiarism report and follow-up comments from both the corresponding author and Nguyen VU against the guidelines of the Committee on Publication Ethics (COPE).&#x0D; Retraction: Ho HN, Nguyen VA, Ho NA, Le HH. Development of a hydrogel containing metronidazole-loaded Eudragit RS 100 nanoparticles for buccal drug delivery. Trop J Pharm Res 2023; 22(6):1147- 1154 doi: 10.4314/tjpr.v22i6.1.

Facile fabrication of an extended-release tablet of Ticagrelor using three dimensional printing technology.

The objective of the study was to fabricate tailored extended-release tablets of blood thinner Ticagrelor as once-daily dosing using additive manufacturing for better compliance in heart failure therapy. The solid work design of the tablet was printed using hot melt extrusion (HME) based 3D printing by optimized mixture of Eudragit RS-100, plasticizer and drug for producing extrudable and printable filaments. FTIR and TGA results showed no covalent interaction among ingredients and no decomposition during HME process, respectively. Friability, weight variation, assay and content uniformity tests met USP requirements, while the mean hardness of the tablets was calculated in a value between 40 and 50 kg. According to DSC and XRD results, the crystallinity state of the Ticagrelor was converted to an amorphous one in the tablet matrix. Smooth surfaces with multiple deposited layers were observed using SEM. In comparison, the maximum Ticagrelor release of 100% after 120 min from Brilinta® tablets was decreased to 97% in 400 min from the 3D tablet at infill of 90%. Korsmeyer-Peppas kinetic model showed the drug release mechanism is affected by diffusion and swelling. In general, fabrication of the extended-release 3D printed tablet of Ticagrelor using HME-based-additive manufacturing has the potential to provide specific doses with tailored kinetic release for personalized medicine, improving adherence at point-of-care.