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Updated: Jun 8, 2025

Disposable Dosators for Pulmonary Insufflation of Therapeutic Agents to Small Animals
Published on: March 30, 2017
Spray dried polymyxin B liposome for inhalation against gram-negative bacteria
Thaddeus Harrison Gugu1,2, Emmanuel Maduabuchi Uronnachi2,3, Ekawat Thawithong2
1Department of Pharmaceutical Microbiology and Biotechnology, University of Nigeria, Nsukka, Nigeria.
Abstract:
This study aimed to provide an alternative and effective delivery system to combat polymyxin B (PMB) toxicity and bacterial resistance through inhalation therapy. PMB was formulated as liposomal dry powder for inhalation using thin-film hydration and spray-dried methods. PMB formulations were characterized physically. The aerodynamic properties were determined using next-generation impactor (NGI). In vitro drug release was done in a phosphate buffer pH 7.4 for 2 h. Cytotoxicity was evaluated by the MTT cell viability assay. Antimicrobiological activities were done using bioassay and flow cytometry. Particle sizes of the spay-dried formulations were between 259.83 ± 9.91 and 518.73 ± 27.08 nm while the zeta potentials ranged between 3.07 ± 0.27 and 4.323 ± 0.36 mV. The Fourier-transform infrared spectroscopy shows no interaction between PMB and other excipients. Differential scanning calorimetry thermograms revealed amorphousness of the formulated powders and SEM revealed spherical PMB formulations. Similarly, mass media aerodynamic diameter results were 1.72-2.75 nm, and FPF was 25%-26%. The cumulative release of the PMB formulations was 90.3 ± 0.6% within 2 h. The killing kinetics revealed total cell death at 12 and 24 h for Pseudomonas aeruginosa and Escherichia coli, respectively. The PMB inhalation liposome showed better activity and was safe for lung-associated cell lines.
Insights
This study developed liposomal dry powder inhalation for polymyxin B (PMB), reducing toxicity and combating resistance. The novel formulation demonstrated safety and efficacy against bacteria in lung models.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Antimicrobial Research
Background:
- Polymyxin B (PMB) exhibits significant toxicity and bacterial resistance, limiting its clinical application.
- Inhalation therapy offers a promising route for localized drug delivery to the lungs, potentially mitigating systemic toxicity.
Purpose of the Study:
- To develop and characterize liposomal dry powder formulations of polymyxin B (PMB) for inhalation.
- To evaluate the safety and efficacy of inhaled liposomal PMB against bacterial infections in the lungs.
Main Methods:
- Liposomal dry powder formulation of PMB using thin-film hydration and spray-drying.
- Characterization of physical properties, aerodynamic performance (NGI), and in vitro drug release.
- Assessment of cytotoxicity (MTT assay) and antimicrobial activity (bioassay, flow cytometry).
Main Results:
- Spray-dried liposomes exhibited particle sizes between 259.83–518.73 nm and positive zeta potentials.
- No chemical interactions were observed between PMB and excipients (FTIR); powders were amorphous (DSC) and spherical (SEM).
- Aerodynamic diameter was 1.72–2.75 nm with 25–26% fine particle fraction (FPF); 90.3% PMB release within 2 hours; effective killing of *Pseudomonas aeruginosa* and *Escherichia coli*.
Conclusions:
- Liposomal dry powder inhalation is an effective delivery system for PMB.
- The formulation demonstrated reduced toxicity and potent antimicrobial activity against key lung pathogens.
- This approach offers a promising strategy to overcome PMB toxicity and bacterial resistance in respiratory infections.
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