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Int J Pharm X. 2021 Mar 03;3:100074. doi: 10.1016/j.ijpx.2021.100074. eCollection 2021 Dec.

Formulation development of itraconazole PEGylated nano-lipid carriers for pulmonary aspergillosis using hot-melt extrusion technology.

International journal of pharmaceutics: X

Gauri Shadambikar, Sushrut Marathe, Nan Ji, Mashan Almutairi, Suresh Bandari, Feng Zhang, Mahavir Chougule, Michael Repka

Affiliations

  1. Department of Pharmaceutics and Drug Delivery, University of Mississippi, University, MS 38677, USA.
  2. Department of Pharmaceutics, College of Pharmacy, University of Hail, Hail 81442, Saudi Arabia.
  3. College of Pharmacy, The University of Texas at Austin, TX 78712, USA.
  4. Pii Center for Pharmaceutical Technology, University of Mississippi, University, MS 38677, USA.

PMID: 33748741 PMCID: PMC7973123 DOI: 10.1016/j.ijpx.2021.100074

Abstract

Pulmonary delivery is a promising alternative for the oral treatment of pulmonary aspergillosis. This study aimed to develop continuous and scalable itraconazole PEGylated nano-lipid carriers (ITZ-PEG-NLC) for inhalation delivery. The feasibility of preparing NLCs utilizing hot-melt extrusion (HME) coupled with probe sonication was investigated. The process parameters for HME and sonication were varied to optimize the formulation. ITZ-PEG-NLC (particle size, 101.20 ± 1.69 nm; polydispersity index, 0.26 ± 0.01) was successfully formulated. The drug entrapment efficiency of ITZ-PEG-NLC was 97.28 ± 0.50%. Transmission electron microscopy was used to characterize the shape of the particles. The developed formulations were evaluated for their aerodynamic properties for pulmonary delivery. The lung deposition of ITZ-PEG-NLC was determined using an Anderson Cascade Impactor and Philips Respironics Sami the Seal Nebulizer Compressor.

© 2021 The Author(s).

Keywords: Hot-melt extrusion; Inhalation; Itraconazole; Nanostructured lipid carriers; PEGylation; Pulmonary drug delivery

Conflict of interest statement

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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