<p>An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles</p>

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 salbutamolloaded 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.

Lung Targeted Lipopolymeric Microspheres of Dexamethasone for the Treatment of ARDS

“…The particle size of the microspheres is the main important factor as it controls the tissue location of the microspheres after intravenous administration. Previous reports have proved that microspheres with the size range of 5–25 μm have a notable lung targeting due to mechanical trapping in the fine blood capillaries of the lung [ 17 , 19 , 20 ].…”

“…The potential of microspheres to effectively deliver carboplatin to the lungs after intravenous administration was also demonstrated [ 19 ]. Recently, Sreeharsha et al [ 20 ] successfully developed salbutamol-loaded PLGA-PEG microspheres for the treatment of asthma. Qu et al [ 21 ] compared two different techniques of microspheres preparation namely, emulsion cross-linking and spray-drying.…”

Pharmaceutical strategies to extend pulmonary exposure of inhaled medicines

“…However, to overcome the hydrophobicity of PLGA or modulate the drug release, hydrophilic polymers such as PEG, PVA, HA can be employed to modify PLGA in the inhaled formulations 108 , 109 , 110 . Various polymeric excipients used in inhaled sustained-release formulations are summarized in Table 1 99 , 111 , 112 , 113 , 114 , 115 , 116 , 117 , 118 , 119 , 120 , 121 .…”

“… 119 PLGA-PEG Biocompatible, amphiphilic, high drug loading capacity – Salbutamol Dry powders 8.24 μm (geometric diameters) A sustained drug release profile with cumulative release of 91.1% over 12 h was achieved. 120 PEG-CS Hydrophilic, biocompatible, biodegradable, non-toxic CS: 190–310 kDa PEG: 5 kDa (Mn) Bovine serum albumin Dry powders 1.02–2.63 μm A tri-phase drug release pattern with a burst release (25%–45%) within the first 2 h, followed by a slow sustained release up to 4 days and an even slower release in late phase. 99 PEG-PLA Biocompatible, biodegradable ∼100 kDa Placebo nanoparticles Nebulized nanoparticulate suspensions 129–141 nm (hydrodynamic diameters) – 121 API, active pharmaceutical ingredient; CS, chitosan; D a , aerodynamic diameters; HA, hyaluronic acid; Mn, number-average molecular weight; MW, molecular weight; PCL, poly- ε -caprolactone; PEG, polyethylene glycol; PK, pharmacokinetics; PLA, polylactic acid; PLGA, poly(lactic- co -glycolic acid); PVA, polyvinyl alcohol; T max , time of maximum concentration; ‒, not applicable.…”

Optical Imaging of Magnetic Particle Cluster Oscillation and Rotation in Glycerol

“…Although there are existing drugs that limit excessive mucus production, there is no cure for excessive mucus production in asthma and other chronic lung diseases. This is likely due to the complex mucus structure that forms a physical barrier, preventing drugs from reaching the diseased airway mucosa (epithelium) [2][3][4]. Nanoparticle systems have been previously investigated for their potential in treating asthma and other lung diseases [4,5].…”