MMX® technology and its applications in gastrointestinal diseases (original) (raw)
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Therapeutic Advances in Gastroenterology
The Multimatrix ® (MMX ® ) preparation MMX ® is a recently obtained drug formulation developed to facilitate release of high concentrations of active drugs into the colon, with a homogeneous distribution along all colonic segments, particularly the most distal ones; the distal colonic tracts, indeed, are the most difficult to reach in significant amounts when a drug is given orally. The MMX ® formulation is characterized by a lipophilic matrix dispersed in a hydrophilic structure. Indeed, in the last few years, MMX ® technology has been widely used in the development of various drugs for the treatment of inflammatory and infectious gastrointestinal diseases localized in the colon. In particular, MMX ® mesalamine, budesonide and parnaparin formulations have been investigated in patients with ulcerative colitis, and the first two have reached worldwide registration for the treatment of this disease. Moreover, MMX ® -rifamycin is being positively tested in the treatment of colonic bacterial infections, including traveler's diarrhea. MMX ® technology is, thus, proving to be a very effective formulation for the treatment of various colonic diseases. This effectiveness has been related not only to specific colonic delivery, but also to its ability to act in a once-daily dosage, thus favouring patients' adherence to prescribed schedules of treatment. The effective delivery of the active molecule to the site of need in the colon is also associated with very low systemic absorption and very low rates of adverse events (AEs). In this paper, we have reviewed all clinical trials performed with an MMX ® -bound drug and all possible real-life reports, in order to give an overall evaluation of MMX ® .
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V, 2015
Coated pellets and mini-tablets were prepared containing a new broad spectrum antibacterial agent: CIN-102, a well-defined, synergistic blend of trans-cinnamaldehyde, trans-2-methoxycinnamaldehyde, cinnamyl acetate, linalool, β-caryophyllene, cineol and benzyl benzoate. The aim was to provide a new treatment method for colitis, especially for Inflammatory Bowel Disease (IBD) patients. Since the simple oral gavage of CIN-102 was not able to reduce the pathogenic bacteria involved in colitis (rat model), the drug was incorporated into multiparticulates. The idea was to minimize undesired drug release in the upper gastrointestinal tract and to control CIN-102 release in the colon, in order to optimize the resulting antibiotic concentration at the site of action. A particular challenge was the fact that CIN-102 is a volatile hydrophobic liquid. Pellet cores were prepared by extrusion-spheronization and coated with polymer blends, which are sensitive to colonic bacterial enzymes. Mini-ta...
Asian Journal of Pharmaceutical and Clinical Research
ABSTRACTObjective: The objective of this research work was to develop a multiparticulate containing chitosan and guar gum for the treatment of ulcerativecolitis.Method: Method for the formulation of multiparticulate was done by extrusion-spheronization method using Eudragit L-100 and Eudragit S-100 as acoating solution and ciprofloxacin as a model drug.Result: Result from preliminary trial batches was previously assessed for physicochemical characterization, in vitro release, ex vivo mucoadhesionstudy, swelling studies, and in vivo evaluation and showed that the formulations appeared to be a good candidate to deliver the drug to the colon.Box-Behnken design was used to statistically optimize the formulation parameters and evaluate the main effects, interaction effects, and quadraticeffects of the process parameters of enteric-coated multiparticulate on drug polymer ratio and coat composition. In this work, the effectivenessof optimized batch (C4) in the treatment of inflammatory bow...
Once-Daily MMX Mesalamine in the Management of Ulcerative Colitis
Clinical Medicine Insights Gastroenterology, 2011
Mesalamine (5-ASA) has been the mainstay therapy of mild to moderate active ulcerative colitis both as an induction and maintenance treatment. Multimatrix system (MMX) 5-ASA is a recently developed formulation of 5-ASA allowing for slow and gradual release of 5-ASA throughout the entire colon. This review article discusses the structure, pharmacokinetics, efficacy and safety of this new 5-ASA formulation.
Multiparticulate Systems of Meloxicam for Colonic Administration in Cancer or Autoimmune Diseases
Pharmaceutics
The aim of this research is the development of new colonic release systems of meloxicam (MLX) a non-steroidal anti-inflammatory drug (NSAIDs) with pH and time-dependent vehicles for cancer or autoimmune diseases. The colon has a higher pH than the rest of the gastrointestinal tract (GIT) and this can be used as a modified release strategy. Eudragit® polymers are the most widely used synthetic products in the design of colonic release formulations because they might offer mucoadhesiveness and pH-dependent release. Colonic delivery systems produced with pH-dependent and permeable polymers (FS-30D) or with pH-independent and low permeability polymers (NM-30D), must dissolve at a pH range of 6.0–7.0 to delay the release of the drug and prevent degradation in the GIT, before reaching the colon. The conditions prepared to simulate a gastrointestinal transit showed the CNM multiparticulate system, composed of Eudragit® NM and cellulose, as the best release option for MLX with a more sustai...
Crohn's & Colitis 360, 2021
Despite recent drug approvals for the treatment of inflammatory bowel diseases (IBDs), there remains a high unmet need for new technologies that can increase drug efficacy by improving site-specific drug delivery while reducing systemic exposure. These technologies must address challenges with formulation; in particular, drugs that are liquid, peptides, or proteins are difficult to formulate using existing delayed and extended oral release technologies. They also have the potential to improve efficacy and reduce systemic exposure for certain drugs by delivering higher doses directly to the site of inflammation. A novel drug delivery system is being developed for delivery at a prespecified part of the gastrointestinal (GI) tract. This autonomous mechanical capsule uses an algorithm based on reflected light to deliver soluble formulations of drugs to the predefined location. This system has significant advantages over other traditional delayed release oral formulations because it func...
Formulation Development and Evaluation of Liposomal Gel for the Treatment of Ulcerative Colitis
Journal of Pharmaceutical & Scientific Innovation, 2018
The present objective for the study as to prepare mesalazine liposomal gel intended for the treatment and management of ulcerative colitis. The aim of this project has been to develop liposomal drug carrier system, able to provide sustained and controlled release of Mesalazine for local rectal therapy. Various liposome formulation was prepared by the thin film hydration technique by using vacuum rotator evaporator by varying the lipid phase composition (lecithin/cholesterol) and evaluated drug content, Particle size analysis, Zeta (z) potential measurement, entrapment efficacy. Liposomal vesicles with good entrapment efficiencies were in corporated in carbopol gel base was evaluated for pH, viscosity, drug content, in-vitro drug release study. Results of all studies suggested that mesalazine liposomal gel formulation was therapeutically effective drug delivery system for treatment of ulcerative colitis.
International Journal of Pharma and Bio Sciences
The aim of present study was to develop colon targeted system for metronidazole using guar gum and xanthan gum. Matrix formulations containing various proportions of guar gum and xanthan gum were prepared by wet granulation technique using 10% starch paste. Later on, multilayer tablets were prepared by using 50 mg and 100 mg of guar gum as release controlling layer on either side of (M5) guar gum matrix tablets of metronidazole. All the formulations were evaluated for in-process quality control tests. The in-vitro drug release study was undertaken at 37±0.5°C in 0.1N HCl for 2 h; followed by pH 7.4 phosphate buffer (3h) finally in, simulated colonic fluid pH 6.8 phosphate buffer containing 4%w/v rat ceacal content for 15 h. Results indicated that guar gum was alone failed to control drug release. M5 (GG: XG, 0:100) formulation seems to quiet promising for colonic drug delivery and only 12.3% drug is released in first 5h wherease, other matrix tablets released 12-33% of metronidazole in physiological environment of stomach and small intestine. When studies were continued in colonic fluids, matrix tablets released almost 100% drug. whereas, metronidazole multilayer formulations did not release drug in stomach and small intestine, but delivered drug to the colon resulting in slow absorption of the drug and making drug available for local action in the colon.
In-vitro and In-vivo Evaluation of Mesalazine–Guar Gum Matrix Tablets for Colonic Drug Delivery
Journal of Drug Targeting, 2004
The aim of this study was to develop colon-specific delivery systems for mesalazine (5-ASA) using guar gum as a carrier. A colon specific matrix tablet of mesalazine with guar gum was evaluated by in vitro and in vivo X-ray studies in humans. Two different types of guar gum were used in the experiments. Tablets were prepared by the slugging method. The physical properties of tablets were tested and in vitro release studies were performed by a flow-through cell apparatus with and without galactomannanase enzyme. The type and the amount of guar gum affected the in vitro release of drug from the matrix tablets. High viscosity guar gum, in the form of a matrix tablet was capable of protecting the drug from being released in the upper region of gastrointestinal (GI) system, i.e. stomach and small intestine. X-ray imaging technique was used to monitor the tablets throughout the GI system on 8 healthy volunteers. Barium sulphate was used as a marker in the tablets for in vivo studies. These results showed that, the matrix tablets reached the colon; not being subjected to disintegration in the upper region of the GI system in all the subjects.