Nimesulide/methyl β-cyclodextrin inclusion complexes: physicochemical characterization, solubility, dissolution, and...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Nimesulide (NIM) is a poorly soluble nonsteroidal anti-inflammatory drug (NSAID).
• Low solubility limits the therapeutic efficacy of many drugs, including NIM.
• Developing strategies to enhance drug solubility is crucial for improving bioavailability.

Purpose of the Study:

• To improve the solubility and dissolution rate of Nimesulide (NIM).
• To investigate the complexation of NIM with methyl β-cyclodextrin (MβCD).
• To characterize the physicochemical properties and evaluate the in vitro performance of NIM-MβCD inclusion complexes.

Main Methods:

• Complexation of NIM with MβCD using a coevaporation technique at various molar ratios (1:1, 1:2, 1:3).
• Physicochemical characterization using powder X-ray diffraction (PXRD) and infrared spectroscopy (IR).
• Quantitative solubility and in vitro dissolution studies in phosphate buffer (pH 5.5 and 7.4).

Main Results:

• Coevaporation successfully formed NIM-MβCD inclusion complexes.
• PXRD and IR analyses indicated molecular interactions between NIM and MβCD.
• Inclusion complexes significantly enhanced NIM solubility and dissolution rate compared to pure NIM.
• Improved solubility and dissolution were observed at higher MβCD ratios.

Conclusions:

• Methyl β-cyclodextrin complexation is an effective strategy to enhance the solubility and dissolution of Nimesulide.
• The developed inclusion systems offer a promising approach for improving the delivery and therapeutic potential of Nimesulide.
• The study confirms molecular interactions facilitating improved drug performance.