Multiple response optimisation of processing and formulation parameters of pH sensitive sustained release pellets of capecitabine for targeting colon

Pandey, Sonia; Swamy, Shivakumar; Gupta, Arti; Koli, Akshay R.; Patel, Swagat; Maulvi, Furqan A.; Vyas, Bhavin

doi:10.1080/02652048.2018.1465138

Cited by 32 publications

(11 citation statements)

References 37 publications

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“…Furthermore, for a low water content, the spheroniser speed became more important than the time [39]. Whereby, the time also played a major role for the roundness of the particles also in dependence of the speed [39,44]. In the present study, a longer rotation time led to more spherical particles at a low speed, compared to a shorter time, but this relationship was statistically not significant.…”

Section: Resultsmentioning

confidence: 53%

Modelling the Effect of Process Parameters on the Wet Extrusion and Spheronisation of High-Loaded Nicotinamide Pellets Using a Quality by Design Approach

Theismann

Keppler

Owen³

et al. 2019

Pharmaceutics

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The aim of the present study was to develop an alternative process to spray granulation in order to prepare high loaded spherical nicotinamide (NAM) pellets by wet extrusion and spheronisation. Therefore, a quality by design approach was implemented to model the effect of the process parameters of the extrusion-spheronisation process on the roundness, roughness and useable yield of the obtained pellets. The obtained results were compared to spray granulated NAM particles regarding their characteristics and their release profile in vitro after the application of an ileocolon targeted shellac coating. The wet extrusion-spheronisation process was able to form highly loaded NAM pellets (80%) with a spherical shape and a high useable yield of about 90%. However, the water content range was rather narrow between 24.7% and 21.3%. The design of experiments (DoE), showed that the spheronisation conditions speed, time and load had a greater impact on the quality attributes of the pellets than the extrusion conditions screw design, screw speed and solid feed rate (hopper speed). The best results were obtained using a low load (15 g) combined with a high rotation speed (900 m/min) and a low time (3–3.5 min). In comparison to spray granulated NAM pellets, the extruded NAM pellets resulted in a higher roughness and a higher useable yield (63% vs. 92%). Finally, the coating and dissolution test showed that the extruded and spheronised pellets are also suitable for a protective coating with an ileocolonic release profile. Due to its lower specific surface area, the required shellac concentration could be reduced while maintaining the release profile.

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Section: Resultsmentioning

confidence: 53%

Modelling the Effect of Process Parameters on the Wet Extrusion and Spheronisation of High-Loaded Nicotinamide Pellets Using a Quality by Design Approach

Theismann

Keppler

Owen³

et al. 2019

Pharmaceutics

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“…A total of 1 ml coating solution was atomized by spray coating for 1 min, in time intervals of 1 min to allow sufficient time for solvent evaporation. Likewise, this was repeated 3 times and the resulted formulation was labelled as F11 (Pandey et al, 2018).…”

Section: Preparation Of Coated Pelletsmentioning

confidence: 99%

Development and characterization of pellets for targeted delivery of 5-fluorouracil and phytic acid for treatment of colon cancer in Wistar rat

Kaur

Goyal

Ghosh

et al. 2020

Heliyon

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The present study was designed to investigate the therapeutic efficacy of metal chelator and anticancer drug in the treatment of colorectal cancer (CRC). Pellets containing Phytic acid, 5-Fluorouracil (5-FU), Microcrystalline cellulose (MCC) PH 101, Hydroxypropyl Methylcellulose (HPMC) and Barium sulfate were prepared by using extrusion spheronization technique. Prepared pellets were coated with Eudragit S100 to achieve colon-specific drug delivery. Pellets were characterized for various pharmaceutical and micromeritic attributes. The in vivo therapeutic efficacy comprising of both pharmacokinetic and pharmacodynamic parameters was determined in Ehrlich ascites carcinoma (EAC) induced cancer animal model. Phytic acid and 5-FU combinations seem to exert higher cytotoxic activity via increased reactive oxygen species (ROS) level by chelating manganese. Further pharmacokinetic studies reveled approximately 50% lower C max in the finished formulation, indicates lower systemic exposure to the drug. X-ray radiography ensures the localized delivery of the encapsulated drug. Histopathological studies indicated no significant local toxicity compared to the uncoated formulation. Results inferred that the proposed combination has superior anticancer activity with minimum systemic and local toxicity and it opens a new avenue in the treatment of colorectal cancer.

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“…In this case, Surelease®, an ethylcellulose variant functioned as an inner layer for waterproofing and extended release. Surelease® was also applied as a release rate modulator in pH sensitive pellets intended for effective colon-targeted delivery of capecitabine to avoid frequent high dosing and associated systemic adverse effects (Pandey et al, 2018). Another investigation employed ethylcellulose together with pectin as a coating for oral minispheres that regulated ciclosporin release kinetics within the small intestine, enhanced delivery and uptake in the colon of the porcine model employed indicating improved clinical advantages in the treatment of inflammatory conditions of the large intestines (Keohane et al, 2016).…”

Section: Macro-structured Delivery Systems Fabricated From Ethylcellumentioning

confidence: 99%

Premium ethylcellulose polymer based architectures at work in drug delivery

Adeleke

2019

International Journal of Pharmaceutics: X

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Multiple response optimisation of processing and formulation parameters of pH sensitive sustained release pellets of capecitabine for targeting colon

Abstract: The study demonstrates the potential of optimised Eudragit/Surelease-coated capecitabine-pellets for effective colon-targeted delivery system to avoid frequent high dosing and associated systemic side effects of drug.

Cited by 32 publications

References 37 publications

Modelling the Effect of Process Parameters on the Wet Extrusion and Spheronisation of High-Loaded Nicotinamide Pellets Using a Quality by Design Approach

Modelling the Effect of Process Parameters on the Wet Extrusion and Spheronisation of High-Loaded Nicotinamide Pellets Using a Quality by Design Approach

Development and characterization of pellets for targeted delivery of 5-fluorouracil and phytic acid for treatment of colon cancer in Wistar rat

Premium ethylcellulose polymer based architectures at work in drug delivery

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