Development and Characterization of Pharmaceutical Systems Containing Rifampicin.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Antimicrobial Research

Background:

• Rifampicin exhibits suboptimal pharmaceutical properties including poor solubility and stability.
• Variable bioavailability of rifampicin necessitates formulation improvements for enhanced therapeutic efficacy.

Purpose of the Study:

• To prepare and characterize a multicomponent complex of rifampicin, gamma-cyclodextrin, and arginine.
• To evaluate the impact of this complex on rifampicin's solubility, dissolution, stability, and antimicrobial activity.

Main Methods:

• Phase-solubility studies were conducted to assess solubility enhancement.
• Proton nuclear magnetic resonance spectroscopy and molecular modeling elucidated the interaction mechanism.
• Fourier transform-infrared spectroscopy, powder X-ray diffraction, and scanning electron microscopy provided physicochemical characterization.
• Antimicrobial activity (antibacterial, antibiofilm, antileishmanial) and dissolution properties were evaluated.

Main Results:

• The multicomponent complex significantly improved rifampicin's water solubility and dissolution rate.
• Physicochemical characterization confirmed the formation of the complex.
• Enhanced antibacterial and antileishmanial activities were observed for the complexed rifampicin.
• The complex demonstrated suitable stability for pharmaceutical applications.

Conclusions:

• Complexation of rifampicin with gamma-cyclodextrin and arginine is a promising strategy to overcome its formulation challenges.
• This approach leads to improved solubility, dissolution, and augmented antimicrobial efficacy.
• The developed rifampicin complex offers an attractive avenue for novel pharmaceutical dosage forms with enhanced therapeutic potential.