Screening paediatric rectal forms of azithromycin as an alternative to oral or injectable treatment

Area of Science:

• Pharmaceutical Sciences
• Tropical Medicine
• Paediatric Pharmacology

Background:

• Developing effective paediatric drug delivery systems is crucial for remote tropical settings.
• Azithromycin is a broad-spectrum antibiotic suitable for various infections but requires accessible administration routes.
• Children in rural tropical areas often face challenges with oral medication adherence and access to healthcare for injectable treatments.

Purpose of the Study:

• To identify a suitable rectal formulation of Azithromycin for paediatric use in resource-limited tropical settings.
• To evaluate different rectal dosage forms for Azithromycin's suitability in emergency and home-based care.
• To assess the in vitro and in vivo performance of candidate Azithromycin rectal formulations.

Main Methods:

• Investigated Azithromycin solubility and stability under physiological conditions.
• Formulated and tested various rectal dosage forms: suspension, gels, polyethylene glycol (PEG) suppository, and hard gelatin capsule (HGC).
• Assessed in vitro dissolution profiles and conducted in vivo bioavailability studies in rabbits.

Main Results:

• The Azithromycin polyethylene glycol (PEG) suppository demonstrated favorable characteristics.
• In vitro dissolution and in vivo bioavailability data supported the PEG suppository as a viable option.
• Other tested formulations, including rectal suspensions and gels, were also evaluated.

Conclusions:

• The Azithromycin PEG suppository is a promising candidate for further development as a rectal paediatric formulation.
• This formulation could offer a viable alternative for treating children in tropical rural settings where oral or injectable administration is challenging.
• Further development is warranted to optimize this rectal delivery system for widespread use.