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Development of levofloxacin-loaded PLGA microspheres of suitable properties for sustained pulmonary release
Marisa C Gaspar1, Alberto A C C Pais2, João J S Sousa3
1Chemical Process Engineering and Forest Products Research Centre (CIEPQPF), Department of Chemical Engineering, University of Coimbra, Rua Sílvio Lima, Pólo II, Pinhal de Marrocos, 3030-790 Coimbra, Portugal; Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal; Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal.
Abstract:
Aerosol antibiotics are an interesting alternative to oral or intravenous therapy in Cystic Fibrosis lung infections. Levofloxacin (LVX) inhaled solution is already an effective option. In this study, the aim was the development of LVX-loaded PLGA microspheres (MS) for pulmonary administration as a dry powder. MS were prepared, for the first time, by a modified double emulsion solvent evaporation method with premix membrane homogenization. Aqueous phases were saturated with LVX and a fatty acid (lauric acid) was added to avoid the drug escaping from the organic phase. MS were characterized in terms of size, drug content, morphology and in vitro release properties. X-ray diffraction, Fourier-transform infrared spectroscopy, differential and gravimetric thermal analysis, and cytotoxicity analyses were performed. Results showed this new method increased the drug loading while maintaining an adequate (∼5 µm) particle size and controlled release. Compared to a solution for inhalation, these properties combined with the dry-powder nature of these MS will improve patient compliance. The incorporation of lauric acid was not advantageous because the particle size was higher and no improvements concerning the sustained release occurred. LVX was molecularly dispersed in the matrix, or it was in amorphous state, as confirmed by the physico-chemical analyses. Calu-3 cell viability assays demonstrated no cytotoxicity for these MS, making them a promising system for LVX pulmonary delivery.
Insights
This study developed novel levofloxacin (LVX) microspheres for Cystic Fibrosis lung infections. These dry powder microspheres offer improved drug loading and patient compliance compared to inhaled solutions.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Biotechnology
Background:
- Aerosol antibiotics present an alternative to conventional therapies for Cystic Fibrosis lung infections.
- Levofloxacin (LVX) inhaled solution is an established treatment option.
- Pulmonary drug delivery aims to enhance therapeutic efficacy and patient compliance.
Purpose of the Study:
- To develop levofloxacin (LVX)-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres (MS) for pulmonary administration as a dry powder.
- To optimize the preparation method for improved drug loading and controlled release.
- To evaluate the physico-chemical properties and cytotoxicity of the developed microspheres.
Main Methods:
- A modified double emulsion solvent evaporation method with premix membrane homogenization was employed for MS preparation.
- Microspheres were characterized for particle size, drug content, morphology, and in vitro release.
- Physico-chemical analyses included X-ray diffraction, FTIR, thermal analysis, and cytotoxicity assays.
Main Results:
- The novel method successfully increased drug loading while maintaining an optimal particle size (∼5 µm) and controlled release profile.
- Physico-chemical analyses confirmed molecular dispersion or amorphous state of LVX within the PLGA matrix.
- Incorporation of lauric acid did not provide additional benefits regarding particle size or sustained release.
Conclusions:
- Developed LVX-loaded PLGA microspheres are a promising dry powder formulation for pulmonary delivery in Cystic Fibrosis.
- The formulation offers potential for improved patient compliance due to its dry powder nature and controlled release.
- Cytotoxicity assays confirmed the safety of the microspheres for pulmonary administration.
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