Development and evaluation of novel itraconazole-loaded intravenous nanoparticles

Chen, Wei; Gu, Bing; Wang, Hao; Pan, Jun; Lu, Weiyue; Hou, Huimin

doi:10.1016/j.ijpharm.2008.05.039

Cited by 70 publications

(37 citation statements)

References 32 publications

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“…5 The presence of large amounts of HP-β-CD limited the use of higher doses and led to the exploration for the alternative parenteral formulations of ITZ. Several intravenous formulations of ITZ, such as the albumin-bound nanoparticles, 6 lipid nanoparticles, 5 nanosuspension, 7,8 and nanocrystal, 9 have been produced without HP-β-CD; high doses of these formulations (approximately 20-80 mg/kg) have been used to obtain a therapeutic efficacy. 6,8 However, ITZ itself may cause negative inotropic effects.…”

mentioning

confidence: 99%

Development of PLGA-based itraconazole injectable nanospheres for sustained release

Bian¹,

Liang²,

John³

et al. 2013

IJN

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Purpose Itraconazole (ITZ) is a synthetic triazole antifungal agent, which is widely used for treatment and prevention of fungal infections. The purpose of this study is to develop ITZ-loaded poly(lactic-co-glycolic acid) (PLGA) nanospheres (PLGA-ITZ-NS) as a new sustained-release formulation for intravenous ITZ administration. Materials and methods PLGA-ITZ-NS were prepared by a nanoprecipitation method and optimized by modifying the surfactant poloxamer 188 concentration and PLGA:ITZ ratio. Their physicochemical properties, including size, zeta potential, external morphology and encapsulation efficiency, were characterized by dynamic light scattering (DLS), scanning electron microscopy (SEM) and high performance liquid chromatography (HPLC). The effect of the different selected lyoprotectants with various concentrations on NS particles size and surface charge were also assessed. Rapid and sensitive HPLC and liquid chromatography-tandem mass spectrometry (LC-MS/MS) methods were developed to determine ITZ concentrations in formulation and in rat plasma, respectively. Pharmacokinetics of the optimum PLGA-ITZ-NS formulation was compared with the former commercial Sporanox® injection formulation using rats as the animal model. Noncompartmental pharmacokinetic parameters were obtained by WinNonlin® software. Results Optimal PLGA-ITZ-NS had a mean particle size of about 200 nm with a high homogeneity (polydispersity index ≈0.2), favorable zeta potential (approximately −20 to −30 mV) and encapsulation efficiency (72%). In addition, 2% w/v sucrose was selected as a lyoprotectant for NS freeze-drying. The newly developed LC-MS/MS assay was validated and found to be accurate and precise. The in vivo study showed that the NS formulation has a similar systemic bioavailability to Sporanox® while providing a sustained plasma level (> 100 ng/mL) for up to 24 hours after intravenous administration. Conclusion Our newly developed PLGA-ITZ-NS has shown great sustained release and comparable bioavailability with Sporanox®, therefore having the potential to be an alternative injectable formulation of ITZ.

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mentioning

confidence: 99%

Development of PLGA-based itraconazole injectable nanospheres for sustained release

Bian¹,

Liang²,

John³

et al. 2013

IJN

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“…Blood was immediately centrifugated at 4,000 rpm for 10 min to isolate the plasma, then 100 µl of the plasma and 3 ml of supernatant was mixed together and centrifuged at 3,000 rpm for 10 min. Then organic phase was processed in a similar manner to the above, blow drying with nitrogen at 60˚C water bath was carried out, and HPLC was used for the determination (34).…”

Section: Cellular Uptake Of Coumarin 6(c6)-loaded Spm (C6-spm)mentioning

confidence: 99%

A comparative study on the effect of docetaxel-albumin nanoparticles and docetaxel-loaded PEG-albumin nanoparticles against non-small cell lung cancer

Gao¹,

Jin²,

Yin³

et al. 2015

International Journal of Oncology

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Abstract. The present study mainly compared the effect of docetaxel-albumin nanoparticles (DANPs) and docetaxelloaded PEG-albumin nanoparticles (PEG-DANPs) against non-small cell lung cancer (NSCLC). We made systematic assessments on these three drugs against NSCLC both in vitro and in vivo. With the purpose of eliminating side-effects of the commercial formulation (Tween-80) and prolonging the blood circulation time, we used emulsion-evaporation crosslink method to prepare DANPs and PEG-DANPs. The DANPs had an average particle size of 163.4±3.76 nm, a zeta potential of -19.4±0.18 mV, a polydispersity index of 0.143±0.03, a drug loading of 8.71±0.98%, and an encapsulation efficiency of 93.58±0.86%; the average particle size of PEG-DANPs is 169.19±2.36 nm, zeta potential is -18.2±0.21 mV, with a polydispersity index of 1.56±0.05, a drug loading of 8.72±1.05% and an encapsulation efficiency of 95.4±5.5%. PEG-DANPs showed a dose-and time-dependent efficacy in cytotoxicity studies in vitro; the hemolysis test indicated that PEG-DANPs had less hemocytolysis than Aisu ® and DANPs; in addition, a more prolonged circulation time and sustained in vitro release behavior were observed in the PEG-DANPs compared with Aisu ® and DANPs; the cellular uptake test in vitro demonstrated that PEG-DANPs could be absorbed easier into the nucleus; furthermore, the tumor growth of NSCLC-bearing nude mice in vivo was reduced the most by PEG-DANPs. In conclusion, the PEG-DANPs have the lowest side-effects, the highest antitumor activity with the longest blood circulation time of the three drugs, and it will provide an alternative to patients with NSCLC. IntroductionLung cancer is a very common malignant tumor with incidence and mortality rates the first worldwide, almost one million patients are diagnosed with lung cancer each year all over the world. NSCLC accounts for 75-85% among the total number of lung cancer, and elderly patients aged >65 years accounted for >50% (1). It is always at the late stage when patients were discovered (stage III or IV) and the 5-year survival rate is only 12-15% (2,3), thus, these patients cannot receive surgical treatment (4,5).For elderly advanced NSCLC patients, chemotherapy is still the first choice of treatment (6,7), it is a relatively effective treatment for elderly NSCLC patients who cannot tolerant surgical operation. It can effectively reduce the progress of lung cancer and the recurrence, enhance the effect of clinical treatment, prolong patient survival rate and improve their quality of life (8).There are some chemotherapy regimens and drugs for elderly NSCLC patients, such as cisplatin, VP-16, gemcitabine, paclitaxel and docetaxel (9). However, there is lack of a mature and effective way for NSCLC because most of the elderly patients refuse or are unable to complete the treatment. So how to choose a drug with good effect and little side reaction is a hot spot in tumor research (10,11). Docetaxel is a cell cycle specific antitumor drug which is applied to cells at the M phase. It is a relative...

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“…This indicated that DPT was loaded in the micelles and therefore appeared in an amorphous state. 44 stability of DPT-PcM and DPT-PM As shown in Figure 4A, the particle size of DPT-PCM was sustained at 40.8 nm at 4°C in the first 7 d. The particle size increased gradually and reached 81.2 nm on the 15th day. However, the size of DPT-PM increased from the 2nd day and reached 789.2 nm on the 15th day.…”

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confidence: 91%

Electrostatic interactions between polyglutamic acid and polylysine yields stable polyion complex micelles for deoxypodophyllotoxin delivery

Wang

Huang

Shen

et al. 2017

IJN

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To achieve enhanced physical stability of poly(ethylene glycol)-poly( d , l -lactide) polymeric micelles (PEG-PDLLA PMs), a mixture of methoxy PEG-PDLLA-polyglutamate (mPEG-PDLLA-PLG) and mPEG-PDLLA-poly( l -lysine) (mPEG-PDLLA-PLL) copolymers was applied to self-assembled stable micelles with polyion-stabilized cores. Prior to micelle preparation, the synthetic copolymers were characterized by 1 H-nuclear magnetic resonance (NMR) and infrared spectroscopy (IR), and their molecular weights were calculated by 1 H-NMR and gel permeation chromatography (GPC). Dialysis was used to prepare PMs with deoxypodophyllotoxin (DPT). Transmission electron microscopy (TEM) images showed that DPT polyion complex micelles (DPT-PCMs) were spherical, with uniform distribution and particle sizes of 36.3±0.8 nm. In addition, compared with nonpeptide-modified DPT-PMs, the stability of DPT-PCMs was significantly improved under various temperatures. In the meantime, the pH sensitivity induced by charged peptides allowed them to have a stronger antitumor effect and a pH-triggered release profile. As a result, the dynamic characteristic of DPT-PCM was retained, and high biocompatibility of DPT-PCM was observed in an in vivo study. These results indicated that the interaction of anionic and cationic charged polyionic segments could be an effective strategy to control drug release and to improve the stability of polymer-based nanocarriers.

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Development and evaluation of novel itraconazole-loaded intravenous nanoparticles

Cited by 70 publications

References 32 publications

Development of PLGA-based itraconazole injectable nanospheres for sustained release

Development of PLGA-based itraconazole injectable nanospheres for sustained release

A comparative study on the effect of docetaxel-albumin nanoparticles and docetaxel-loaded PEG-albumin nanoparticles against non-small cell lung cancer

Electrostatic interactions between polyglutamic acid and polylysine yields stable polyion complex micelles for deoxypodophyllotoxin delivery

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