Binary and Ternary Inclusion Complexes of Niflumic Acid: Synthesis, Characterization, and Dissolution Profile.
Pharmaceutics
; 16(9)2024 Sep 09.
Article
in En
| MEDLINE
| ID: mdl-39339226
ABSTRACT
Although niflumic acid (NA) is one of the most used non-steroidal anti-inflammatory drugs, it suffers from poor solubility, low bioavailability, and significant adverse effects. To address these limitations, the complexation of NA with cyclodextrins (CDs) is a promising strategy. However, complexing CDs with low molecular weight drugs like NA can lead to low CE. This study explores the development of inclusion complexes of NA with 2-hydroxypropyl-ß-cyclodextrin (2HP-ß-CD), including the effect of converting NA to its sodium salt (NAs) and adding hydroxypropyl methylcellulose (HPMC) on complex formation. Inclusion complexes were prepared using co-evaporation solvent and freeze-drying methods, and their CE and Ks were determined through a phase solubility study. The complexes were characterized using physicochemical analyses, including FT-IR, DSC, SEM, XRD, DLS, UV-Vis, 1H-NMR, and 1H-ROESY. The dissolution profiles of the complexes were also evaluated. The analyses confirmed complex formation for all systems, demonstrating drug-cyclodextrin interactions, amorphous drug states, morphological changes, and improved solubility and dissolution profiles. The NAs-2HP-ß-CD-HPMC complex exhibited the highest CE and Ks values, a 11 host-guest molar ratio, and the best dissolution profile. The results indicate that the NAs-2HP-ß-CD-HPMC complex has potential for delivering NA, which might enhance its therapeutic effectiveness and minimize side effects.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
Pharmaceutics
Year:
2024
Document type:
Article
Affiliation country:
Algeria
Country of publication:
Switzerland