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Published on: April 6, 2017
Single vs Dual Lactose-Polyethylene Glycol 3000 Microcarrier Systems for Pulmonary Salmeterol and Fluticasone
Muhammad Waseem Akram1,2, Badrul Hisyam Zainudin3, Mohamed Effendi Mohamed Tenang4
1Non-Destructive Biomedical and Pharmaceutical Research Centre, Smart Manufacturing Research Institute, Universiti Teknologi MARA Selangor, Puncak Alam, 42300, Malaysia.
Dual-microcarriers improve pulmonary delivery of salmeterol (SX) and fluticasone (FP) for asthma. This dual-drug system enhances lung targeting and reduces inflammation more effectively than single-drug carriers.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Respiratory Medicine
Background:
- Single-vehicle agglomeration of salmeterol (SX) and fluticasone (FP) hinders pulmonary drug redispersion and targeting.
- Developing advanced microcarrier systems is crucial for efficient delivery of anti-asthmatic and anti-inflammatory agents.
Purpose of the Study:
- To design and evaluate externally drug-coated dual-microcarrier systems against single-microcarrier systems for improved pulmonary delivery of SX and FP.
- To investigate the pulmonary drug delivery and targeting profiles of novel dual-microcarrier formulations.
Main Methods:
- Spray-dried lactose-polyethylene glycol 3000 microcarriers were prepared, with magnesium stearate added as a lubricant.
- Both single- and dual-microcarrier systems were analyzed using cascade impactors to assess particle size and formulation attributes.
- In vivo pharmacokinetic and pharmacodynamic profiles were evaluated.
Main Results:
- Smaller microcarriers (~5 µm) facilitated SX targeting to the upper airways, while magnesium stearate improved inhalation by reducing aggregation.
- The dual-microcarrier system enabled targeted release of SX in the upper lung and FP in the lower lung.
- Dual-microcarriers enhanced FP deposition in the lower lung, increased pulmonary drug retention, reduced inflammatory markers, and alleviated bronchoconstriction.
Conclusions:
- Externally drug-coated dual-microcarrier systems demonstrate superior efficiency in pulmonary delivery of SX and FP compared to single-microcarrier systems.
- The dual-microcarrier approach offers a promising strategy for optimizing inhaled corticosteroid and long-acting beta-agonist combination therapy.
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