Development of an Itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application

Pardeike, Jana; Weber, Sabrina; Haber, Thomas; Wagner, Julian; Zarfl, Hans Peter; Plank, Harald; Zimmer, Andreas

doi:10.1016/j.ijpharm.2011.07.040

Cited by 183 publications

(84 citation statements)

References 39 publications

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“…10 The amount entrapped was determined by subtracting the free drug concentration from the total drug added. The sample was placed in the Amicon Ultra-4 filtration unit with molecular weight cut-off of 30,000 Da and centrifuged for 10 minutes at 3,000 × g. The filtrate was analyzed by HPLC method (1200 HPLC series; Agilent Technologies, Santa Clara, CA, USA) with a C-18 analytical column (5 µm, 4.6 × 150 mm; Phenomenex, Torrance, CA, USA) The mobile phase comprised acetonitrile and deionized water (70:30, v/v%); the flow rate was 1 mL/minute; and the detection wavelength was 262 nm.…”

Section: Determination Of Entrapment Efficiencymentioning

confidence: 99%

“…It has an n-octanol/water partition coefficient of 5.66 at pH 8.1. 10 It is reported to have solubility of 1 ng/mL at pH 7 and of 4 µg/mL at pH 1. 11 To overcome this problem, the current marketed intravenous formulation involves the complexation of ITZ with 2-hydroxypropyl-β-cyclodextrin (HβCD).…”

mentioning

confidence: 99%

“…Chen et al formulated ITZ nanoparticles using human serum albumin for parenteral delivery; 7 Kim et al designed ITZ-loaded lipid nanoparticles to achieve controlled release when administered intravenously; 13 Pardeike et al formulated ITZ-loaded lipid nanoparticles for pulmonary application; 10 and Duret et al embedded ITZ-loaded nanoparticles in inhalable microparticles for the treatment of pulmonary aspergillosis. 22 However, to the best of our knowledge, the preparation of ITZ-loaded lipid nanoparticles for brain-targeted delivery has not yet been evaluated.…”

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confidence: 99%

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

Lim¹,

Rajinikanth²,

Chitneni³

et al. 2014

IJN

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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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Section: Determination Of Entrapment Efficiencymentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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

Lim¹,

Rajinikanth²,

Chitneni³

et al. 2014

IJN

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“…29 It is supported by the high EE when ATO 5 is used to incorporate the lipophilic drug Itraconazole into lipid NPs. 34 The high EE may also be attributed to the massive crystal order disturbance caused by the incorporation of liquid lipid in solid lipid, resulting in a lipid matrix with crystal lattice defects, which provides enough space to accommodate drug molecules in the matrix. 35 Similarly, we also observed high EE of DOX (90%), which might be related to the conversion of DOX hydrochloride into a less soluble free base to facilitate DOX distribution into the oil phase.…”

Section: Physical Characterization Of Dox/ Cur-npsmentioning

confidence: 99%

Codelivery of doxorubicin and curcumin with lipid nanoparticles results in improved efficacy of chemotherapy in liver cancer

Zhao¹,

Chen²,

Liu³

et al. 2014

IJN

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Liver cancer is a leading cause of cancer deaths worldwide. The combination therapy of cytotoxic and chemosensitizing agents loaded in nanoparticles has been highlighted as an effective treatment for different cancers. However, such studies in liver cancer remain very limited. In our study, we aim to develop a novel lipid nanoparticles loaded with doxorubicin (DOX) (an effective drug for liver cancer) and curcumin (Cur) (a chemosensitizer) simultaneously, and we examined the efficacy of chemotherapy in liver cancer. DOX and Cur codelivery lipid nanoparticles (DOX/Cur-NPs) were successfully prepared using a high-pressure microfluidics technique, showing a mean particle size of around 90 nm, a polydispersity index <0.3, and a zeta potential <−10 mV. The encapsulation efficacy was >90% for both DOX and Cur. The blank lipid nanoparticles were nontoxic, as determined by a cell cytotoxicity study in human normal liver cells L02 and liver cancer cells HepG2. In vitro DOX release studies revealed a sustained-release pattern until 48 hours in DOX/Cur-NPs. We found enhanced cytotoxicity and decreased inhibitory concentration (IC) 50 in HepG2 cells and reduced cytotoxicity in L02 cells treated with DOX/Cur-NPs, suggesting the synergistic effects of DOX/Cur-NPs compared with free DOX and DOX nanoparticles (NPs). The optimal weight ratio of DOX and Cur was 1:1. Annexin-V-fluorescein isothiocyanate/propidium iodide double staining showed enhanced apoptosis in HepG2 cells treated with DOX/Cur-NPs compared with free DOX and DOX-NPs. An in vivo experiment showed the synergistic effect of DOX/Cur-NPs compared with DOX-NPs on liver tumor growth inhibition. Taken together, the simultaneous delivery of DOX and Cur by DOX/Cur-NPs might be a promising treatment for liver cancer.

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“…The production of NLC is of low cost with ease for scaling up [22]. Accordingly, NLCs have been investigated for drug delivery through different routes including oral, pulmonary intravenous injection, nose-tobrain, and dermal and ocular applications [23][24][25][26]. However, there has been no report on application of NLCs for Dac delivery.…”

Section: Introductionmentioning

confidence: 99%

Development of nanostructured lipid carrier for dacarbazine delivery

2015

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Dacarbazine (Dac) is one of the most commonly used chemotherapy drugs for treating various cancers. However, its poor water solubility, short half-life in blood circulation, low response rate and high side effect limit its application. This study aimed to improve the drug solubility and prolong drug release by developing nanostructured lipid carriers (NLCs) for Dac delivery. The NLC and Dac-encapsulated NLC were synthesized with precirol ATO 5 and isopropyl myristate as lipids, tocopheryl polyethylene glycol succinate, soybean lecithin and Kolliphor P 188 as co-surfactants. The NLCs with controlled size were achieved using high shear dispersion following solidification of oil-in-water emulsion. For Dac encapsulation, the smallest NLC with 155 ± 10 nm in size, 0.2 ± 0.01 polydispersion index and -43.4 ± 2 mV zeta potential was selected. The resultant DLC-Dac possessed size, polydispersion index and zeta potential of 190 ± 10, 0.2 ± 0.01, and -43.5 ± 1.2, respectively. The drug encapsulation efficiency and drug loading were 98.5 % and 14 %, respectively. In vitro drug release study showed a biphasic pattern, with 50 % released in the first 2 h, and the remaining released sustainably for up to 30 h. This is the first report on the development of NLC for Dac delivery, implying that NLC could be a new potential candidate as drug carrier to improve the therapeutic profile of Dac.

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Development of an Itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application

Cited by 183 publications

References 39 publications

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

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

Codelivery of doxorubicin and curcumin with lipid nanoparticles results in improved efficacy of chemotherapy in liver cancer

Development of nanostructured lipid carrier for dacarbazine delivery

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Development of an Itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application

Cited by 183 publications

References 39 publications

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

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

Codelivery of doxorubicin and curcumin with&nbsp;lipid nanoparticles results in improved efficacy of&nbsp;chemotherapy in liver cancer

Development of nanostructured lipid carrier for dacarbazine delivery

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Codelivery of doxorubicin and curcumin with lipid nanoparticles results in improved efficacy of chemotherapy in liver cancer