Getting into the colon: approaches to target colorectal cancer

Patel, Mayur M.

doi:10.1517/17425247.2014.927440

Cited by 36 publications

(29 citation statements)

References 26 publications

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“…[1,2]. Oral formulations deliv-60 ering chemotherapeutics to the colon are promising to improve 61 treatment of colorectal cancer [3], driven by the principle that tar-62 geted delivery of drugs to their intended cellular targets offers 63 opportunities for increasing treatment efficacy while minimising 64 the administered dose and associated side effects. Novel drug 65 delivery systems based on nanotechnology, such as nanoparticles 66 (NPs) [4] and nanoparticle-in-microcapsule systems [5], have 67 recently been developed for achieving colon-specific delivery of 68 therapeutic agents.…”

mentioning

confidence: 99%

The in vivo fate of nanoparticles and nanoparticle-loaded microcapsules after oral administration in mice: Evaluation of their potential for colon-specific delivery

Fuchs

Boase

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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confidence: 99%

The in vivo fate of nanoparticles and nanoparticle-loaded microcapsules after oral administration in mice: Evaluation of their potential for colon-specific delivery

Fuchs

Boase

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…It is considered as a lifestyle disease. [1] It is also known as bowel cancer and it starts from the epithelium of colon and rectum. In contrary to CRC, occurrence of anal cancer is rare.…”

Section: Olon Cancer or Colorectal Cancer (Crc)mentioning

confidence: 99%

Untitled

Bansal¹

2018

AJP

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Background and Objectives: Colon cancer is one of the leading causes of deaths around the world in human beings. In the present investigation, pharmacokinetic and biodistribution analysis of eudragit-coated chitosan microspheres bearing 5-fluorouracil (5-FU) and celecoxib (Cb) combination (5-FU-Cb-Ch-ES-MSs) was carried out in Wistar rats. Materials and Methods: The tailored microspheres and a suspension of 5-FU and Cb (5-FU-Cb-PS) at the dose of 15 mg/kg of 5-FU and 3.3 mg/kg of Cb, respectively, were administered through oral route of administration. Results and Discussion: 5-FU-Cb-PS exhibited C max of 36.71 ± 3.23 µg/ml at t max of 1 ± 0.17 h for 5-FU. On the other hand, C max of 10.14 ± 1.16 µg/ml at t max of 10.26 ± 0.58 h was noticed for 5-FU released from 5-FU-Cb-Ch-ES-MSs. 5-FU-Cb-PS showed C max of 22.48 ± 5.32 µg/ml at t max of 8 ± 0.00 h for Cb. Correspondingly, C max of 3.18 ± 0.16 µg/ml at t max of 12.39 ± 0.62 h was observed for Cb released from 5-FU-Cb-Ch-ES-MSs. Moreover, at the end of 8 h, 5-FU-Cb-Ch-ES-MSs delivered a substantial amount of 5-FU (56.3 µg/g) and Cb (78.6 µg/g) in the colon, the site of action. Conclusion: This remarkable therapeutic concentration of both the drugs in the colon may be associated with pH-dependent solubility of eudragit S100 and subsequent degradation of Ch core in the colonic milieu due to the presence of polysacharidase enzyme. Therefore, it can be postulated that the 5-FU-Cb-Ch-ES-MSs is a potential candidate for further in vivo study.

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“…In the field of oral modified-release, great efforts have been made since the 1990s to develop drug delivery systems (DDSs) able to release the conveyed drug to specific regions of the gastrointestinal tract [1][2][3][4][5][6][7]. In particular, the colon drew considerable attention as a target site for the treatment of local disorders, such as inflammatory bowel diseases (e.g., ulcerative colitis and Crohn's disease) and irritable bowel syndrome, as well as for the prevention of colorectal adenocarcinoma [8][9][10]. Moreover, the colonic region was investigated as a possible gateway to the systemic circulation, for instance to enhance the oral bioavailability of peptide and protein drugs [11][12][13].…”

Section: Introductionmentioning

confidence: 99%

Injection Molded Capsules for Colon Delivery Combining Time-Controlled and Enzyme-Triggered Approaches

Casati

Melocchi

Moutaharrik

et al. 2020

IJMS

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A new type of colon targeting system is presented, combining time-controlled and enzyme-triggered approaches. Empty capsule shells were prepared by injection molding of blends of a high-amylose starch and hydroxypropyl methylcellulose (HPMC) of different chain lengths. The dissolution/erosion of the HPMC network assures a time-controlled drug release, i.e., drug release starts upon sufficient shell swelling/dissolution/erosion. In addition, the presence of high-amylose starch ensures enzyme-triggered drug release. Once the colon is reached, the local highly concentrated bacterial enzymes effectively degrade this polysaccharide, resulting in accelerated drug release. Importantly, the concentration of bacterial enzymes is much lower in the upper gastrointestinal tract, thus enabling site-specific drug delivery. The proposed capsules were filled with acetaminophen and exposed to several aqueous media, simulating the contents of the gastrointestinal tract using different experimental setups. Importantly, drug release was pulsatile and occurred much faster in the presence of fecal samples from patients. The respective lag times were reduced and the release rates increased once the drug started to be released. It can be expected that variations in the device design (e.g., polymer blend ratio, capsule shell geometry and thickness) allow for a large variety of possible colon targeting release profiles.

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Getting into the colon: approaches to target colorectal cancer

Cited by 36 publications

References 26 publications

The in vivo fate of nanoparticles and nanoparticle-loaded microcapsules after oral administration in mice: Evaluation of their potential for colon-specific delivery

The in vivo fate of nanoparticles and nanoparticle-loaded microcapsules after oral administration in mice: Evaluation of their potential for colon-specific delivery

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Injection Molded Capsules for Colon Delivery Combining Time-Controlled and Enzyme-Triggered Approaches

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