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The influence of surface active l-leucine and 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the improvement of aerosolization of pyrazinamide and moxifloxacin co-spray dried powders.
Int J Pharm. 2018 May 05; 542(1-2):72-81.IJ

Abstract

Pharmacotherapy of tuberculosis is potentially more efficient when delivered by the inhaled route than by the current oral and/or parenteral routes due to the higher concentration of drug reaching the primary region of infection in the lungs. This study investigated the influence of the amino acid l-leucine alone and in combination with the phospholipid, 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC), on the aerosolization behaviour of the anti-TB drugs, pyrazinamide and moxifloxacin HCl. Spray dried powders of pyrazinamide (P), moxifloxacin (M) alone and in combination with 10% l-leucine (PL and ML) and 10% DPPC (PLD and MLD) were produced. The particle sizes of all powders except P were in the inhalable size range (<5 µm) but differ in their morphology in presence of the excipients. X-ray photoelectron spectroscopy (XPS) and time-of-flight secondary ion mass spectrometry (ToF-SIMS) revealed the migration of surface active l-leucine and DPPC onto the surface of the particles during the spray drying process. The aerosolization from a dry powder inhaler, Aerolizer®, using a Next Generation Impactor revealed fine particle fraction (FPF) values for P, PL and PLD of 18.7 ± 3.4%, 53.0 ± 3.2% and 74.5 ± 5.3% respectively while FPF values for M, ML and MLD were 55.6 ± 3.3%, 74.7 ± 4.7% and 74.1 ± 1.3% respectively. In conclusion, the differences in the aerosolization behaviours of the pyrazinamide and moxifloxacin spray dried powders with and without excipients was a combination of difference in the surface morphology and surface composition.

Authors+Show Affiliations

School of Pharmacy, University of Otago, P.O. Box 56, Dunedin 9054, New Zealand.School of Pharmacy, University of Otago, P.O. Box 56, Dunedin 9054, New Zealand.The University of Auckland, 20 Symonds Street, Auckland, New Zealand.Future Industries Institute, University of South Australia, Mawson Lakes, SA, Australia.School of Pharmacy, University of Otago, P.O. Box 56, Dunedin 9054, New Zealand. Electronic address: Shyamal.das@otago.ac.nz.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29524618

Citation

Eedara, Basanth Babu, et al. "The Influence of Surface Active L-leucine and 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the Improvement of Aerosolization of Pyrazinamide and Moxifloxacin Co-spray Dried Powders." International Journal of Pharmaceutics, vol. 542, no. 1-2, 2018, pp. 72-81.
Eedara BB, Rangnekar B, Doyle C, et al. The influence of surface active l-leucine and 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the improvement of aerosolization of pyrazinamide and moxifloxacin co-spray dried powders. Int J Pharm. 2018;542(1-2):72-81.
Eedara, B. B., Rangnekar, B., Doyle, C., Cavallaro, A., & Das, S. C. (2018). The influence of surface active l-leucine and 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the improvement of aerosolization of pyrazinamide and moxifloxacin co-spray dried powders. International Journal of Pharmaceutics, 542(1-2), 72-81. https://doi.org/10.1016/j.ijpharm.2018.03.005
Eedara BB, et al. The Influence of Surface Active L-leucine and 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the Improvement of Aerosolization of Pyrazinamide and Moxifloxacin Co-spray Dried Powders. Int J Pharm. 2018 May 5;542(1-2):72-81. PubMed PMID: 29524618.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The influence of surface active l-leucine and 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the improvement of aerosolization of pyrazinamide and moxifloxacin co-spray dried powders. AU - Eedara,Basanth Babu, AU - Rangnekar,Bhamini, AU - Doyle,Colin, AU - Cavallaro,Alex, AU - Das,Shyamal C, Y1 - 2018/03/07/ PY - 2017/12/19/received PY - 2018/03/06/revised PY - 2018/03/06/accepted PY - 2018/3/11/pubmed PY - 2018/9/25/medline PY - 2018/3/11/entrez KW - 1,2-Dipalmitoyl-sn-glycero-3-phosphatidylcholine KW - Aerodynamic performance KW - Moxifloxacin HCl KW - Pyrazinamide KW - Surface composition KW - l-Leucine SP - 72 EP - 81 JF - International journal of pharmaceutics JO - Int J Pharm VL - 542 IS - 1-2 N2 - Pharmacotherapy of tuberculosis is potentially more efficient when delivered by the inhaled route than by the current oral and/or parenteral routes due to the higher concentration of drug reaching the primary region of infection in the lungs. This study investigated the influence of the amino acid l-leucine alone and in combination with the phospholipid, 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC), on the aerosolization behaviour of the anti-TB drugs, pyrazinamide and moxifloxacin HCl. Spray dried powders of pyrazinamide (P), moxifloxacin (M) alone and in combination with 10% l-leucine (PL and ML) and 10% DPPC (PLD and MLD) were produced. The particle sizes of all powders except P were in the inhalable size range (<5 µm) but differ in their morphology in presence of the excipients. X-ray photoelectron spectroscopy (XPS) and time-of-flight secondary ion mass spectrometry (ToF-SIMS) revealed the migration of surface active l-leucine and DPPC onto the surface of the particles during the spray drying process. The aerosolization from a dry powder inhaler, Aerolizer®, using a Next Generation Impactor revealed fine particle fraction (FPF) values for P, PL and PLD of 18.7 ± 3.4%, 53.0 ± 3.2% and 74.5 ± 5.3% respectively while FPF values for M, ML and MLD were 55.6 ± 3.3%, 74.7 ± 4.7% and 74.1 ± 1.3% respectively. In conclusion, the differences in the aerosolization behaviours of the pyrazinamide and moxifloxacin spray dried powders with and without excipients was a combination of difference in the surface morphology and surface composition. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/29524618/The_influence_of_surface_active_l_leucine_and_12_dipalmitoyl_sn_glycero_3_phosphatidylcholine__DPPC__in_the_improvement_of_aerosolization_of_pyrazinamide_and_moxifloxacin_co_spray_dried_powders_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(18)30151-0 DB - PRIME DP - Unbound Medicine ER -