ArticlePharmaceutical research2018
Physico-Chemical Properties, Aerosolization and Dissolution of Co-Spray Dried Azithromycin Particles with L-Leucine for Inhalation.
Article in Pharmaceutical research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 89 citations in OpenAlex.
- Design of Ion-Pairing Azithromycin liposome for Local Pulmonary Delivery with Prolonged Lung Retention.AAPS PharmSciTech · 2026Article
- Engineering Inhalable Carboxymethyl Chitosan-Swellable Microgels for Pulmonary Delivery of Charged Hydrophilic Molecules.Gels (Basel, Switzerland) · 2025Article
- Improved Encapsulation and Potential of Liposomal Tosufloxacin via Inclusion in Cyclodextrin.AAPS PharmSciTech · 2025Article
- Influence of Different Amino Acids on the Aerosolization, Stability and Cytotoxicity of Spray-Dried Cannabidiol Dry Powder for Inhalation.Pharmaceutics · 2025Article
- Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections.Pharmaceutics · 2025Article
- Optimization, In Vitro, and In Silico Characterization of Theophylline Inhalable Powder Using Raffinose-Amino Acid Combination as Fine Co-Spray-Dried Carriers.Pharmaceutics · 2025Article
- Impact of Co-Spray Drying with Leucine or Trileucine on Aerosol Performance, In Vitro Dissolution, and Cellular Uptake of Colistin Powder Formulations for Inhalation.Pharmaceutics · 2025Article
- A Novel Inhalable Dry Powder to Trigger Delivery of Voriconazole for Effective Management of Pulmonary Aspergillosis.Pharmaceutics · 2024Article
- Preparation and Evaluation of Inhalable Microparticles with Improved Aerodynamic Performance and Dispersibility Using L-Leucine and Hot-Melt Extrusion.Pharmaceutics · 2024Article
- Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles.Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques · 2024Article
- Pharmacokinetic Considerations for Optimizing Inhaled Spray-Dried Pyrazinoic Acid Formulations.Molecular pharmaceutics · 2023Article
- Bulk Flow Optimisation of Amorphous Solid Dispersion Excipient Powders through Surface Modification.Pharmaceutics · 2023Article
- Recent Advances in Pharmaceutical Approaches of Antimicrobial Agents for Selective Delivery in Various Administration Routes.Antibiotics (Basel, Switzerland) · 2023Review
- Article
- On the Physical Stability of Leucine-Containing Spray-Dried Powders for Respiratory Drug Delivery.Pharmaceutics · 2023Article
- Enhancing bioavailability of natural extracts for nutritional applications through dry powder inhalers (DPI) spray drying: technological advancements and future directions.Frontiers in nutrition · 2023Review
- Local Delivery of Azithromycin Nanoformulation Attenuated Acute Lung Injury in Mice.Molecules (Basel, Switzerland) · 2022Article
- Manipulation of Spray-Drying Conditions to Develop an Inhalable Ivermectin Dry Powder.Pharmaceutics · 2022Article
- Excipient-Free Inhalable Microparticles of Azithromycin Produced by Electrospray: A Novel Approach to Direct Pulmonary Delivery of Antibiotics.Pharmaceutics · 2021Article
- Hyaluronic Acid Hydrogels for Controlled Pulmonary Drug Delivery-A Particle Engineering Approach.Pharmaceutics · 2021Article
Corrections and comments
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Authors and funding
7 authors at 5 institutions in 3 countries.
Funding
Abstract
purposeInhalation therapy is popular to treat lower respiratory tract infections. Azithromycin is effective against some bacteria that cause respiratory tract infections; but it has poor water solubility that may limit its efficacy when administrated as inhalation therapy. In this study, dry powder inhaler formulations were developed by co-spray drying azithromycin with L-leucine with a purpose to improve dissolution.
methodsThe produced powder formulations were characterized regarding particle size, morphology, surface composition and in-vitro aerosolization performance. Effects of L-leucine on the solubility and in-vitro dissolution of azithromycin were also evaluated.
resultsThe spray dried azithromycin alone formulation exhibited a satisfactory aerosol performance with a fine particle fraction (FPF) of 62.5 ± 4.1%. Addition of L-leucine in the formulation resulted in no significant change in particle morphology and FPF, which can be attributed to enrichment of azithromycin on the surfaces of composite particles. Importantly, compared with the spray-dried amorphous azithromycin alone powder, the co-spray dried powder formulations of azithromycin and L-leucine demonstrated a substantially enhanced in-vitro dissolution rate. Such enhanced dissolution of azithromycin could be attributed to the formation of composite system and the acidic microenvironment around azithromycin molecules created by the dissolution of acidic L-leucine in the co-spray dried powder. Fourier transform infrared spectroscopic data showed intermolecular interactions between azithromycin and L-leucine in the co-spray dried formulations.
conclusionsWe developed the dry powder formulations with satisfactory aerosol performance and enhanced dissolution for a poorly water soluble weak base, azithromycin, by co-spray drying with an amino acid, L-leucine.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.