Preparation and Evaluation of 5 Fluorouracil solid dispersion formulations for therapeutic management of colorectal cancer (CRC)

International Journal of Drug Delivery

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Title Preparation and Evaluation of 5 Fluorouracil solid dispersion formulations for therapeutic management of colorectal cancer (CRC)
Creator Oyeniyi, Yinka; UDUS
Nnamani, Nemeka D
Subject pharmaceutical sciences
Solid dispersion, colorectal cancer and 5-Fluorouracil
Description BackgroundA solid dispersion formulation (SD) involves dispersion of poor water soluble active pharmaceutical ingredients (API) in a solubility enhancing polymer with the uttermost goal of improving the oral bioavailability of the API.ObjectiveThis study is aimed at production and evaluation of 5- Fluorouracil (5- FU) SD formulations for colon delivery using the hot met technique.MethodThe solid dispersions of 5-FU were prepared by hot melting method; The  SD formulations were characterized using a scanning electron microscopy, USP dissolution apparatus type 2, and  MTT assay.ResultsThe SEM revealed that all SD formulations particles were in amorphous state, they rod like shaped with size ranging between 98 -112µm. The FTIR spectral show no chemical interactions between the excipients and 5 FU.  The yield (PY), drug entrapment efficiency (DEE) and the drug loading (DL) values were high enough to support commercial scale up of the technique.SD2 had the highest DEE, cumulative drug released and DL values. This may be responsive for its improved cytotoxicity against HT115 cells. The releases of 5 FU in all the formulations follow both Fickian´s and non-Fickian´s kinetics which are also pH responsive with no sign of dose dumping. ConclusionThis study demonstrated successful production of pH responsive 5 FU solid dispersions, by hot melt technique. The release follows Korymeyer –Peppas kinetic models and selectively delivered 5 FU to the colon which improved cytotoxicity activity against CRC.
Publisher Advanced Research Journals
Contributor nill
Date 2019-07-05
Type info:eu-repo/semantics/article

Source International Journal of Drug Delivery; Vol 11, No 2 (2019): International Journal of Drug Delivery
Language en
Rights Copyright (c) 2019 Yinka Oyeniyi, Nemeka D Nnamani

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