PREPARATION AND EVALUATION OF 5-FLUOROURACIL SOLID DISPERSION FORMULATIONS FOR THERAPEUTIC MANAGEMENT OF COLORECTAL CANCER (CRC)
Oyeniyi YJ*1, Nnamani ND2
1. Department of Pharmaceutics and Pharm.Microbiology, Faculty of Pharmaceutical Sciences, Usmanu Danfodiyo University, Sokoto
2. Department of Pharmaceutics and Pharm.Technology, College of Pharmacy, Igbinedion University, Okada, Edo state.
Afr. J Pharm Res Dev; Volume 10(2): 127-134 ; 2018
ABSTRACT
Solid dispersion technology (SD) involves dispersion of poor water soluble active pharmaceutical ingredients (API) in a solubility enhancing polymer with the uttermost goal of improving oral bioavailability of the API. This is study is aimed at production and evaluation of SD formulations of 5- Fluorouracil (5- FU) for colon delivery using hot met solid dispersion method (SD). The 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. The SEM revealed that all SD formulations particles were in amorphous state, non-spherically 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 the improve 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. This 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.
Email of correspondence:drdeyinkaoyeniyi@gmail.com;
KEYWORDS: SOLID DISPERSION, COLORECTAL CANCER AND 5-FLUOROURACIL