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Design of Ion-Pairing Azithromycin liposome for Local Pulmonary Delivery with Prolonged Lung Retention
Mengtong Wu1, Siqi Li1, Hongbing Liu1
1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, 110016, China.
Abstract:
Mycoplasma pneumoniae pneumonia (MPP) is a major cause of community-acquired pneumonia in children, and azithromycin (AZM) is recommended as a first-line macrolide for its treatment. However, current oral and intravenous AZM formulations require high systemic doses to achieve effective pulmonary concentrations, thereby increasing the risk of adverse effects (e.g., gastrointestinal reactions, cardiotoxicity) and antibiotic resistance. In this study, we developed an azithromycin liposomal formulation (AC-Lip) for local pulmonary administration, enabling direct targeting of pulmonary lesions while reducing the required dose and enhancing pulmonary bioavailability. To achieve efficient drug loading, an ion-pairing strategy was employed to increase the lipophilicity of AZM through complexation with cholesteryl hemisuccinate. The resulting AC-Lip displayed a spherical morphology with an average particle size of approximately 120 nm, a high encapsulation efficiency of 89.86%, and favorable long-term stability. Pharmacokinetic analysis demonstrated that, following pulmonary administration, the absolute pulmonary bioavailability of AZM from AC-Lip was 6.52-fold higher than that of intravenous AZM injection. Preliminary nebulization stability studies further supported its feasibility as an inhalable formulation. Collectively, these findings indicate that AC-Lip enables efficient pulmonary-targeted delivery of AZM and holds substantial promise as a novel clinical therapeutic strategy for the treatment of MPP.
Insights
A new liposomal azithromycin formulation (AC-Lip) offers targeted lung delivery for Mycoplasma pneumoniae pneumonia (MPP). This approach enhances pulmonary bioavailability and reduces systemic exposure, promising a safer treatment for pediatric MPP.
Area of Science:
- Pharmacology
- Nanotechnology
- Pediatric Infectious Diseases
Background:
- Mycoplasma pneumoniae pneumonia (MPP) is a common childhood respiratory infection.
- Current azithromycin (AZM) treatments require high doses, leading to potential side effects and antibiotic resistance.
- Effective pulmonary drug delivery remains a challenge for treating MPP.
Purpose of the Study:
- To develop a novel liposomal azithromycin formulation (AC-Lip) for targeted pulmonary delivery.
- To improve azithromycin's pulmonary bioavailability and reduce systemic toxicity for MPP treatment.
- To assess the feasibility of AC-Lip as an inhalable therapeutic agent.
Main Methods:
- Azithromycin was encapsulated into liposomes using an ion-pairing strategy with cholesteryl hemisuccinate.
- The AC-Lip formulation was characterized for morphology, particle size, encapsulation efficiency, and stability.
- Pharmacokinetic studies compared pulmonary bioavailability of AC-Lip versus intravenous AZM.
- Nebulization stability was evaluated to assess inhalable potential.
Main Results:
- AC-Lip exhibited spherical morphology (approx. 120 nm) with high encapsulation efficiency (89.86%) and good stability.
- Pulmonary administration of AC-Lip resulted in a 6.52-fold higher bioavailability compared to intravenous AZM.
- Preliminary studies indicated AC-Lip's stability for nebulization.
Conclusions:
- AC-Lip provides an effective strategy for pulmonary-targeted delivery of azithromycin.
- This novel formulation holds significant potential for improved clinical treatment of pediatric MPP.
- AC-Lip may reduce adverse effects and combat antibiotic resistance associated with conventional AZM therapy.
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