Open AccessAN ADDUCT: 5-FLUOROURACIL INCORPORATED β-CD INCLUSION COMPLEX FOR SOLUBILITY AND STABILITY ENHANCEMENT IN DOSAGE FORMS
Author(s) -
Rahul Singh,
ANIRUDH SINGH DEORA
Publication year - 2022
Publication title -
international journal of applied pharmaceutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.238
H-Index - 15
ISSN - 0975-7058
DOI - 10.22159/ijap.2022v14i2.43602
Subject(s) - solubility , dissolution , chemistry , cyclodextrin , moiety , complex formation , dosage form , drug , stability constants of complexes , yield (engineering) , chromatography , organic chemistry , materials science , aqueous solution , inorganic chemistry , pharmacology , metallurgy , medicine
Objective: Current work aimed to enhance solubility and stability of 5-fluorouracil drugs by preparing inclusion complex with β-cyclodextrin.Methods: In this study, inclusion complex preparation ratio selected on the basis of slope and Kc (binding constant) value in between 5-fluorouracil-β-cyclodextrin and best method out of the physical mixture, kneading method, and co-evaporation method for solubility and stability enhancement is selected on the basis of % yield, drug content, dissolution rate study and stability study.Results: Based on the phase solubility graph, a 1:1 ratio was selected for complex formation by Kc value which decided a quite stable form of a complex. The characterization of all three types of inclusion complex was performed by DSC and SEM. It proved that different moiety of the complex was formed, but all are quite stable with negligible interaction. The kneading method as the best inclusion complex at ratio 1:1 was selected after evaluating by performing percent yield and drug content and dissolution rate study for solubility profile and physical appearance, drug content, and drug release study for stability profile.Conclusion: We finally conclude that the Kc value proved that the inclusion complex is quite stable and ready to convert in any dosage form of choice. Inclusion complex formed by kneading method is one of the best options among all three techniques for solubility and stability enhancement of drug, which definitely help for a 5-fluorouracil drug to convert into a better dosage form to treat carcinoma.