Drug Design, Development and Therapy (Dec 2019)
An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles
Abstract
Nagaraja SreeHarsha,1,2 Katharigatta N Venugopala,1,3 Anroop B Nair,1 Teeka S Roopashree,4 Mahesh Attimarad,1 Jagadeesh G Hiremath,2 Bandar E Al-Dhubiab,1 Chandramouli Ramnarayanan,5 Pottathil Shinu,6 Mukund Handral,7 Micheline Haroun,1 Christophe Tratrat1 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 2Department of Pharmaceutics, Vidya Siri College of Pharmacy, Bengaluru, India; 3Department of Biotechnology and Food Technology, Durban University of Technology, Durban 4001, South Africa; 4Department of Pharmacognosy, Government College of Pharmacy, Bengaluru, India; 5Department of Quality Assurance, Krupanidhi College of Pharmacy, Bengaluru, India; 6Department of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 7Department of Pharmacology, Faculty of Pharmaceutical Sciences, PES University, Bengaluru, IndiaCorrespondence: Nagaraja SreeHarshaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, PO Box 400, Al-Ahsa, Saudi ArabiaTel +96-653-548-5322Email [email protected]: 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
