Design, optimization and evaluation of mesalamine matrix tablet for colon drug delivery system

Pawar, Pravin; Gautam, Chinanshu

doi:10.1007/s40005-015-0214-z

Cited by 20 publications

(8 citation statements)

References 25 publications

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“…The objectives of such a combination are to minimize the early release of CSA in the stomach and small intestine by using Eudragit FS30D and, at the same time, to prevent complete drug release prior to reaching the inflamed colon mucosa and achieve a sustained release thereafter by using PLGA. 43,44 Results from the in vitro drug-release study in the medium with a gradually changing pH that mimics the environment of the GIT demonstrated that dual-functional E/PNPs minimize the burst CSA release under stomach conditions (pH 1.2) and the complete release under ileum conditions (pH 7.4), showing sustained release thereafter (Figure 2A). Furthermore, size analysis at different pH values revealed that, unlike pH-dependent ENPs, dual-functional E/PNPs maintained their nanoparticulate size at pH 7.4, which demonstrated the presence of PLGA.…”

Section: Discussionmentioning

confidence: 98%

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>®</sup> FS30D/PLGA nanoparticles ameliorates murine experimental colitis

Naeem¹,

Bae²,

Oshi³

et al. 2018

IJN

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BackgroundColon-targeted oral nanoparticles (NPs) have emerged as an ideal, safe, and effective therapy for ulcerative colitis (UC) owing to their ability to selectively accumulate in inflamed colonic mucosa. Cyclosporine A (CSA), an immunosuppressive agent, has long been used as rescue therapy in severe steroid-refractory UC. In this study, we developed CSA-loaded dual-functional polymeric NPs composed of Eudragit® FS30D as a pH-sensitive polymer for targeted delivery to the inflamed colon, and poly(lactic-co-glycolic acid) (PLGA) as a sustained-release polymer.MethodsCSA-loaded Eudragit FS30D nanoparticles (ENPs), PLGA nanoparticles (PNPs), and Eudragit FS30D/PLGA nanoparticles (E/PNPs) were prepared using the oil-in-water emulsion method. Scanning electron microscope images and zeta size data showed successful preparation of CSA-loaded NPs.ResultsPNPs exhibited a burst drug release of >60% at pH 1.2 (stomach pH) in 0.5 h, which can lead to unwanted systemic absorption and side effects. ENPs effectively inhibited the burst drug release at pH 1.2 and 6.8 (proximal small intestine pH); however, nearly 100% of the CSA in ENPs was released rapidly at pH 7.4 (ileum–colon pH) owing to complete NP dissolution. In contrast to single-functional PNPs and ENPs, the dual-functional E/PNPs minimized burst drug release (only 18%) at pH 1.2 and 6.8, and generated a sustained release at pH 7.4 thereafter. Importantly, in distribution studies in the gastrointestinal tracts of mice, E/PNPs significantly improved CSA distribution to the colon compared with PNPs or ENPs. In a mouse model of colitis, E/PNP treatment improved weight loss and colon length, and decreased rectal bleeding, spleen weight, histological scoring, myeloperoxidase activity, macrophage infiltration, and expression of proinflammatory cytokines compared with PNPs or ENPs.ConclusionOverall, this work confirms the benefits of CSA-loaded E/PNPs for efficiently delivering CSA to the colon, suggesting their potential for UC therapy.

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Section: Discussionmentioning

confidence: 98%

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>®</sup> FS30D/PLGA nanoparticles ameliorates murine experimental colitis

Naeem¹,

Bae²,

Oshi³

et al. 2018

IJN

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“…Colon-targeted drug release: Colon-targeted drug delivery systems are required for local treatment of colon-specific diseases such as Crohn’s disease, irritable bowel syndrome (IBS), and colon cancer [ 2 , 52 , 53 ]. In addition, there is great interest in colonic drug release as an effective approach for improving the bioavailability of peptides and protein drugs [ 2 ].…”

Section: Pharmaceutical Application Of Film Coatingmentioning

confidence: 99%

“…As (i) the GI tract undergoes dynamic changes in motility, enzymatic activity, fluid content, and pH from the stomach to the intestine, and (ii) the pathologic condition of a disease site in the colon is markedly different from normal and healthy regions [ 2 ], surface coating for colon targeted drug release is more complex than enteric coating targeting the small intestine. Various film coating approaches have been explored for colonic drug delivery, including pH-dependent film coating, enzymatically degradable coating, and time-dependent film coating [ 53 , 54 ]. However, most of these systems exhibit suboptimal drug release profiles.…”

Section: Pharmaceutical Application Of Film Coatingmentioning

confidence: 99%

Pharmaceutical Application of Tablet Film Coating

et al. 2020

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Tablet film coating is a common but critical process providing various functionalities to tablets, thereby meeting diverse clinical needs and increasing the value of oral solid dosage forms. Tablet film coating is a technology-driven process and the evolution of coated dosage forms relies on advancements in coating technology, equipment, analytical techniques, and coating materials. Although multiple coating techniques are developed for solvent-based or solvent-free coating processes, each method has advantages and disadvantages that may require continuous technical refinement. In the film coating process, intra- and inter-batch coating uniformity of tablets is critical to ensure the quality of the final product, especially for active film coating containing active pharmaceutical ingredients in the coating layer. In addition to experimental evaluation, computational modeling is also actively pursued to predict the influence of operation parameters on the quality of the final product and optimize process variables of tablet film coating. The concerted efforts of experiments and computational modeling can save time and cost in optimizing the tablet coating process. This review provides a brief overview of tablet film coating technology and modeling approaches with a focus on recent advancements in pharmaceutical applications.

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“…Around 19% and 14% drug release were obtained at pH 7.2 after 6 and 8 hours respectively compared to less than 10% at pH 1.2 and pH 6.8 at the same time points. Pawar et al [24] prepared and evaluated matrix tablets of mesalamine for colon triggered delivery, composed of Eudragit RSPO and/or RLPO as rate-controlling matrices, and coated with different concentration of anionic pH dependent copolymers (Eudragit S100). 9 formulations were prepared using different concentrations of Eudragit RSPO, Eudragit RLPO and Eudragit S100.…”

Section: Main Text Time Dependent and Ph Responsive Approachesmentioning

confidence: 99%

Recent advances in mesalamine colonic delivery systems

Bayan

2020

Futur J Pharm Sci

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Background: Increased attention has been focused on the continuous development and improvement of mesalamine colonic specific delivery systems, for the effective treatment of inflammatory bowel diseases; thus enhancing therapeutic efficacy and reducing potential side effects. Mesalamine is a class IV drug, according to the Biopharmaceutics Classification System, used usually to treat inflammation associated with colon related diseases such as Crohn's disease and ulcerative colitis. Main text An ideal colon targeting system aims to deliver a therapeutic agent, selectively and effectively, to the colon. This system should ideally retain the drug release in the upper GI tract (stomach and small intestine); while trigger the drug release in the colon. Several approaches have been used to fabricate formulations to achieve a colon specific delivery of mesalamine such as; time dependent, pH responsive, enzymatic/microbial responsive and ultrasound mediated approaches. This overview outlines the recent advances in mesalamine-colon delivery approaches for the potential treatment of ulcerative colitis and Crohn' disease. Conclusion: A combined pH-time dependent delivery system can improve mesalamine colonic drug delivery via employing carriers capable of retarding mesalamine release in the stomach and delivering it at predetermined time points after entering the intestine. The existence of specific enzymes, produced by various anaerobic bacteria present in the colon advocates the advantage of designing enzyme sensitive systems and combining it with pHtime dependent system to improve mesalamine colonic delivery. The use of ultrasound has shown promises to effectively treat inflammatory bowel diseases.

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Design, optimization and evaluation of mesalamine matrix tablet for colon drug delivery system

Cited by 20 publications

References 25 publications

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>®</sup> FS30D/PLGA nanoparticles ameliorates murine experimental colitis

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>®</sup> FS30D/PLGA nanoparticles ameliorates murine experimental colitis

Pharmaceutical Application of Tablet Film Coating

Recent advances in mesalamine colonic delivery systems

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Design, optimization and evaluation of mesalamine matrix tablet for colon drug delivery system

Cited by 20 publications

References 25 publications

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>&reg;</sup>&nbsp;FS30D/PLGA&nbsp;nanoparticles ameliorates murine experimental colitis

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>&reg;</sup>&nbsp;FS30D/PLGA&nbsp;nanoparticles ameliorates murine experimental colitis

Pharmaceutical Application of Tablet Film Coating

Recent advances in mesalamine colonic delivery systems

Contact Info

Product

Resources

About

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>®</sup> FS30D/PLGA nanoparticles ameliorates murine experimental colitis

Colon-targeted delivery of cyclosporine A using dual-functional Eudragit<sup>®</sup> FS30D/PLGA nanoparticles ameliorates murine experimental colitis