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Cited by 103Advancements in Transdermal Drug DeliveryAdvanced Drug Delivery SystemsNanoparticle-Based Drug Delivery

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Formulation and delivery of itraconazole to the brain using a nanolipid carrier system

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Lim, Weimeng, RAJINIKANTH, Paruvathanahalli Siddalingam, Mallikarjun, Chitneni, KANG, Yew Beng·2014·International Journal of Nanomedicine
DOI 10.2147/ijn.s57565PMC PMC4014385
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Abstract

The objectives of this study were to develop and characterize itraconazole (ITZ)-loaded nanostructured lipid carriers (NLCs) and to study their potential for drug delivery into the brain. Precirol(®) ATO 5 and Transcutol(®) HP were selected as the lipid phase, and Tween(®) 80 and Solutol(®) HS15 as surfactants. The ITZ-NLCs were prepared by a hot and high-pressure homogenization method. The entrapment efficiency for the best formulation batch was analyzed using high-performance liquid chromatography and was found to be 70.5%±0.6%. The average size, zeta potential, and polydispersity index for the ITZ-NLCs used for animal studies were found to be 313.7±15.3 nm, -18.7±0.30 mV, and 0.562±0.070, respectively. Transmission electron microscopy confirmed that ITZ-NLCs were spherical in shape, with a size of less than 200 nm. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ was encapsulated in the lipid matrix and present in the amorphous form. The in vitro release study showed that ITZ-NLCs achieved a sustained release, with cumulative release of 80.6%±5.3% up to 24 hours. An in vivo study showed that ITZ-NLCs could increase the ITZ concentration in the brain by almost twofold. These results suggest that ITZ-NLCs can be exploited as nanocarriers to achieve sustained release and brain-targeted delivery.

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Figure 1 Transmission electron microscope image of itraconazole-loaded nanostructured lipid carriers.
Figure 1 Transmission electron microscope image of itraconazole-loaded nanostructured lipid carriers.CC BY-NC · PubMed Central
Figure 2 Differential scanning calorimetry analysis for ITZ, Precitol ATO 5, blank NLCs and ITZ-NLCs. Notes: (A) Itraconazole; (B) Precirol® ATO 5 (Gattefossé Lyon, France); (C) blank nanostructured lipid carriers; (D) itraconazole-loaded nanostructured lipid carriers. Abbreviations: ITZ, itraconazole; ITZ-NLCs, itraconazole loaded nanostructured lipid carriers; NLCs, nanostructured lipid carriers.
Figure 2 Differential scanning calorimetry analysis for ITZ, Precitol ATO 5, blank NLCs and ITZ-NLCs. Notes: (A) Itraconazole; (B) Precirol® ATO 5 (Gattefossé Lyon, France); (C) blank nanostructured lipid carriers; (D) itraconazole-loaded nanostructured lipid carriers. Abbreviations: ITZ, itraconazole; ITZ-NLCs, itraconazole loaded nanostructured lipid carriers; NLCs, nanostructured lipid carriers.CC BY-NC · PubMed Central
Figure 3 X-ray diffractogram for ITZ-NLCs, blank NLCs and ITZ. Notes: (A) Itraconazole-loaded nanostructured lipid carriers; (B) blank nanostructured lipid carriers; (C) itraconazole. Abbreviations: ITZ, itraconazole; ITZ-NLCs, itraconazole loaded nanostructured lipid carriers; NLCs, nanostructured lipid carriers.
Figure 3 X-ray diffractogram for ITZ-NLCs, blank NLCs and ITZ. Notes: (A) Itraconazole-loaded nanostructured lipid carriers; (B) blank nanostructured lipid carriers; (C) itraconazole. Abbreviations: ITZ, itraconazole; ITZ-NLCs, itraconazole loaded nanostructured lipid carriers; NLCs, nanostructured lipid carriers.CC BY-NC · PubMed Central
Figure 4 In vitro release profile for ITZ solution and ITZ-NLC formulation batch F12 (n=3). Abbreviations: ITZ, itraconazole; ITZ-NLC, itraconazole-loaded nanostructured lipid carrier.
Figure 4 In vitro release profile for ITZ solution and ITZ-NLC formulation batch F12 (n=3). Abbreviations: ITZ, itraconazole; ITZ-NLC, itraconazole-loaded nanostructured lipid carrier.CC BY-NC · PubMed Central
Figure 5 In vivo itraconazole concentration in brain (n=3). Note: *P<0.05. Abbreviations: ITZ, itraconazole; ITZ-NLC, itraconazole-loaded nanostructured lipid carrier.
Figure 5 In vivo itraconazole concentration in brain (n=3). Note: *P<0.05. Abbreviations: ITZ, itraconazole; ITZ-NLC, itraconazole-loaded nanostructured lipid carrier.CC BY-NC · PubMed Central

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Metadata

Authors
Lim, W., RAJINIKANTH, P. S., Mallikarjun, C., & KANG, Y. B.
Affiliations
  • IMU University (MY)
  • Taylor's University (MY)
Corresponding author
Lim, Weimeng
ORCID
Venue
International Journal of Nanomedicine
Publisher
Informa UK Limited
Published
2014-05
Volume
9
Pages
2117
ISSN
  • 1176-9114 (ISSN-L)
  • 1178-2013
DOI
10.2147/ijn.s57565
PMC
PMC4014385
OpenAlex
W1976348972
Cited by
103
References
46
Citations by year
2026: 5 · 2025: 7 · 2024: 6 · 2023: 14 · 2022: 7 · 2021: 16 · 2020: 15 · 2019: 7 · 2018: 11 · 2017: 4 · 2016: 6 · 2015: 5
FWCI
2.84
Type
journal article
Language
en
Open access
Licence
Locations
  • International Journal of Nanomedicine (publishedVersion, cc-by-nc)
  • Europe PMC (PubMed Central) (publishedVersion, cc-by-nc)
  • PubMed Central (publishedVersion, cc-by-nc)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
  • Dove Medical Press (Taylor and Francis Group) (submittedVersion, cc-by-nc)
Funders
International Medical University
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
itraconazole, nanostructured lipid carriers, brain drug delivery, brain-targeted delivery, antifungal agents, sustained drug release, encapsulation efficiency, amorphous drug encapsulation, nanocarriers, nanoparticle characterization
MeSH terms
Animals, Antifungal Agents, Blood-Brain Barrier, Diglycerides, Drug Compounding, Ethylene Glycols, Particle Size, Polyethylene Glycols, Polysorbates, Stearic Acids, Tissue Distribution, Itraconazole, Mice, Nanocapsules

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CoChat. (2026). Citation check: Formulation and delivery of itraconazole to the brain using a nanolipid carrier system. https://app.cochat.ai/papers/10.2147/ijn.s57565
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Lim, W., RAJINIKANTH, P. S., Mallikarjun, C., & KANG, Y. B. (2014). Formulation and delivery of itraconazole to the brain using a nanolipid carrier system. International Journal of Nanomedicine. https://doi.org/10.2147/ijn.s57565