An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles

Abstract

Background

Chronic diseases such as diabetes, asthma, and heart disease are the leading causes of death in developing countries. Public health plays an important role in preventing such diseases to improve individuals’ quality of life. Conventional dosage schemes used in public health to cure various diseases generally lead to undesirable side effects and renders the overall treatment ineffective. For example, a required concentration of drug cannot reach the lungs using conventional methods to cure asthma. Microspheres have emerged as a confirmed drug-delivery system to cure asthma.

Method

In this paper, a salbutamol-loaded poly lactic acid-co-glycolic acid-polyethylene glycol (PLGA-PEG) microsphere (SPP)-based formulation was prepared using a Buchi B-90 nanospray drier. Face-centered central composite design (CCD) was applied to optimize the spray-drying process.

Results

The drug content and product yield were found to be 72%±0.8% and 86%±0.4%, respectively; drug release (91.1%) peaked for up to 12 hrs in vitro. Microspheres obtained from the spray dryer were found to be shriveled. The experiments were carried out and verified using various groups of rabbits. In our study, the particle size (8.24 µm) was observed to be an essential parameter for drug delivery. The in vivo results indicated that the targeting efficacy and drug concentration in the lung was higher with the salbutamol-loaded PLGA-PEG SPP formulation (1,410.1±10.11 µg/g, 15 mins), as compared to the conventional formulation (92±0.56 µg/g, 10 min). The final product was stable under 5°C±2°C, 25°C±2°C, and 40°C±2°C/75%±5% relative humidity. In addition, these co-polymers have a good safety profile, as determined by testing on human alveolar basal epithelium A549 cell lines.

Conclusion

Our results prove that microspheres are an alternative drug-delivery system for lung-targeted asthma treatments used in public health.

Keywords:

• polylactic acid-co-glycolic acid
• public health
• spray dryer
• microspheres

Acknowledgements

We thank the Deanship of Scientific Research, King Faisal University, Al-Ahsa, Saudi Arabia for funding this project (grant number: 1811018). The authors wish to thank Mr. Tameem M. Alyahian and Mr. Naif Ali Alunssif, who helped to procure chemicals, prepare the formulation, and handle the instruments. English-language editing of this manuscript was provided by Journal Prep Services.

Data Availability

The scanning electron microscopy, particle size determination, in vitro release, optimization, in vivo release, in vitro cytotoxicity studies, DNA fragmentation assay and stability data used to support the findings of this study are included within the manuscript.

Author Contributions

All authors contributed to data analysis, drafting or revising the article, gave final approval of the version to be published, and agree to be accountable for all aspects of the work.

Disclosure

The authors declare no conflicts of interest.