PRE-FORMULATION STUDY ON 5-FLUOROURACIL AND CERTAIN LIPIDS FOR SOLID LIPID NANOPARTICLES PREPARATION

Authors

DOI:

https://doi.org/10.22159/ijap.2022v14i2.43491

Keywords:

5-fluorouracil; glycerol monostearate; stearic acid; compritol®; cholesterol.

Abstract

Objective: The study's objective involved compatibility studies to investigate the possible interactions between 5-fluorouracil (5-FU) and four different lipids, and the most appropriate lipid was chosen. 

  Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier Transform Infrared spectroscopy (FT-IR) are used for the compatibility study between 5-FU and several excipients as cholesterol, compritol®, stearic acid, and glycerol monostearate (GMS).

Methods: The physical mixture between 5-FU and each lipid was made by mixing of a certain amount of drug with the same amount of lipid. Drug lipid blended mixtures were made by solvent evaporation casting method. 5-FU alone, physical mixture and blended mixture were measured using Differential scanning calorimetry (DSC) to investigate melting peak of drug and effect of each lipid on this melting point, X-ray diffraction (XRD) to observe the crystalline or amorphous state of drug and Fourier Transform Infrared (FT-IR) to determine any chemical interaction between drug and these lipids by observing any shift happened to characteristic peaks related to the drug.

Results: 5-FU Tm (280.04 °C) peak appeared in drug-lipid physical mixtures with minor changes in position while this peak disappeared in 5-FU-compritol® and 5-FU-cholesterol blended mixture indicating that the drug is molecular dispersed. XRD result showed that the crystalline structure of 5-FU was present in physical mixtures with four lipids while in the 5-FU-compritol® blended mixture, the crystalline state of the drug was disappeared confirming the DSC result.

    The FT-IR spectrum of the 5-FU-physical mixtures with four lipids showed that all characteristic peaks of the drug appeared with minor changes. In the case of 5-FU-blended mixtures with mentioned lipids, no chemical interaction occurred between the drug and mentioned lipids except in the drug-stearic acid blended mixture, the N-H peak at 3136.25cm-1 was disappeared due to amide ester formation.

Conclusion: The most appropriate lipids suitable for the preparation of 5-FU solid lipid nanoparticles were GMS and cholesterol.

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Published

15-12-2021

How to Cite

ELKHATIB, M. M., ALI, A. I., ABDELRAZEK, S. A., & AL-BADRAWY, A. S. (2021). PRE-FORMULATION STUDY ON 5-FLUOROURACIL AND CERTAIN LIPIDS FOR SOLID LIPID NANOPARTICLES PREPARATION. International Journal of Applied Pharmaceutics, 14(2). https://doi.org/10.22159/ijap.2022v14i2.43491

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