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. 2014 May 2:9:2117-26.
doi: 10.2147/IJN.S57565. eCollection 2014.

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

Wei Meng Lim  1 , Paruvathanahalli Siddalingam Rajinikanth  2 , Chitneni Mallikarjun  1 , Yew Beng Kang  1
Affiliations

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

Wei Meng Lim et al. Int J Nanomedicine. .

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.

Keywords: brain delivery; lipid nanoparticles; nanostructured lipid carrier.

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Figures

Figure 1
Figure 1
Transmission electron microscope image of itraconazole-loaded nanostructured lipid carriers.
Figure 2
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 3
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 4
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 5
Figure 5
In vivo itraconazole concentration in brain (n=3). Note: *P<0.05. Abbreviations: ITZ, itraconazole; ITZ-NLC, itraconazole-loaded nanostructured lipid carrier.
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References

    1. Wissing SA, Kayser O, Müller RH. Solid lipid nanoparticles for parenteral drug delivery. Adv Drug Deliv Rev. 2004;56(9):1257–1272. - PubMed
    1. Severino P, Andreani T, Macedo AS, et al. Current state-of-art and new trends on lipid nanoparticles (SLN and NLC) for oral drug delivery. J Drug Deliv. 2012;2012:750891. - PMC - PubMed
    1. Müller RH, Mäder K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery – a review of the state of the art. Eur J Pharm Biopharm. 2000;50(1):161–177. - PubMed
    1. Mehnert W, Mäder K. Solid lipid nanoparticles: production, characterization and applications. Adv Drug Deliv Rev. 2001;47(2–3):165–196. - PubMed
    1. Müller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Deliv Rev. 2002;54(Suppl 1):S131–S155. - PubMed

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