Theranostic Nanoemulsions: Codelivery of Hydrophobic Drug and Hydrophilic Imaging Probe for Cancer Therapy and Imaging

Yang, Xinggang; Wang, Dun; Ma, Yan; Zhao, Qiang; Fallon, John K.; Liu, Dan; Xu, Xiaojie; Wang, Yongjun; Zhang, He; Liu, Feng

doi:10.2217/nnm.14.50

Cited by 24 publications

(15 citation statements)

References 43 publications

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“…37,38 FA-PEG-VE was synthesized according to a previous work. 39 The synthetic route and 1 H-NMR characterization of MPEG-PHIS is shown in Figures S2 and S3.…”

Section: Materials and Methods Materialsmentioning

confidence: 99%

pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity

Yan¹,

Li²,

Zhu³

et al. 2017

IJN

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The aim of this study was to simultaneously introduce pH sensitivity and folic acid (FA) targeting into a micelle system to achieve quick drug release and to enhance its accumulation in tumor cells. Paclitaxel-(+)-α-tocopherol (PTX-VE)-loaded mixed micelles (PHIS/FA/PM) fabricated by poly(ethylene glycol) methyl ether-poly(histidine) (MPEG-PHIS) and folic acid-poly(ethylene glycol)-(+)-α-tocopherol (FA-PEG-VE) were characterized by dynamic light scattering and transmission electron microscopy (TEM). The mixed micelles had a spherical morphology with an average diameter of 137.0±6.70 nm and a zeta potential of −48.7±4.25 mV. The drug encapsulation and loading efficiencies were 91.06%±2.45% and 5.28%±0.30%, respectively. The pH sensitivity was confirmed by changes in particle size, critical micelle concentration, and transmittance as a function of pH. MTT assay showed that PHIS/FA/PM had higher cytotoxicity at pH 6.0 than at pH 7.4, and lower cytotoxicity in the presence of free FA. Confocal laser scanning microscope images demonstrated a time-dependent and FA-inhibited cellular uptake. In vivo imaging confirmed that the mixed micelles targeted accumulation at tumor sites and the tumor inhibition rate was 85.97%. The results proved that the mixed micelle system fabricated by MPEG-PHIS and FA-PEG-VE is a promising approach to improve antitumor efficacy.

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“…37,38 FA-PEG-VE was synthesized according to a previous work. 39 The synthetic route and 1 H-NMR characterization of MPEG-PHIS is shown in Figures S2 and S3.…”

Section: Materials and Methods Materialsmentioning

confidence: 99%

pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity

Yan¹,

Li²,

Zhu³

et al. 2017

IJN

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“…S1 †). 7,23 Folic acid (FA) was obtained from Zhengzhou Longsheng Chemical Products Co., Ltd. (China). PEG 2000 was obtained from Jiangsu Haian Petro Chemical Plant (China), while (+)-atocopherol (VE) was obtained from Hubei Prosperity Galaxy Chemical Co., Ltd. (China).…”

Section: Methodsmentioning

confidence: 99%

“…Despite this, as mentioned before, PTX-VE exhibited higher average blood concentration than that of PTX, and longer half-lives and retention times in vivo. 23,34 Furthermore, we evaluated the advantages of co-delivery drugs into novel micelles. The viability of A549 cells aer incubation with free conjugated drug solutions, blank micelles, and drug-loaded micelles for 72 h at four different concentrations (GEM-VE concentrations: 0.925, 9.25, 55.5, and 185 mg mL À1 ; corresponding PTX-VE concentrations: 0.0775, 0.775, 4.65, and 15.5 mg mL À1 ) is shown in Fig.…”

Section: In Vitro Releasementioning

confidence: 99%

Co-delivery of hydrophilic gemcitabine and hydrophobic paclitaxel into novel polymeric micelles for cancer treatment

et al. 2017

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“…Nanoemulsions are the unique choice for intravenous emulsion-based formulations which require specific and strict criteria including controlled droplet sizes (less than 1 or 2 µm) [4], restricted composition, physicochemical and biological stability and sterilized requirement. Parenteral nanoemulsions have been presented in numerous studies [5,6,7,8] and were included in several clinical trials such as treatment of leukemia [9] and diabetic dyslipidemia [10]. Parenteral nanoemulsions are interesting formulations for the delivery of many drugs [4].…”

Section: Introductionmentioning

confidence: 99%

Comparison of Three Processes for Parenteral Nanoemulsion Production: Ultrasounds, Microfluidizer, and Premix Membrane Emulsification

Alliod

Almouazen

Nemer

et al. 2019

Journal of Pharmaceutical Sciences

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Nanoemulsions are of great interest for pharmaceutical applications, including parenteral dosage forms. However, their production is still limited and requires more efficient and adaptive technologies. The more common systems are high-shear homogenization like microfludizers (MF) at industrial scale and ultrasounds at research scale, both based on high energy limiting their application for sensitive drugs. Recently, a process based on premix membrane emulsification (PME) was developed to produce nanoemulsions. These three processes have been compared for the production of a model parenteral nanoemulsion containing all-transretinoic acid, a thermolabile molecule which is used in the treatment of acute promyelocytic leukemia in a parenteral form. Droplet size and active integrity were studied because of their major interest for efficacy and safety assessment. Regarding droplet size, PME produced monodispersed droplets of 335 nm compared to the other processes which produced nanoemulsions of around 150 nm but with the presence of micron size droplets detected by laser diffraction and optical microscopy. No real difference between the three processes was observed on active degradation during emulsifcation. However, regarding stability, especially at 40 o C nanoemulsions obtained with the microfluidizer showed a greater molecule degradation and unstable nanoemulsion with a 4 times droplet size increase under stress conditions.

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Theranostic Nanoemulsions: Codelivery of Hydrophobic Drug and Hydrophilic Imaging Probe for Cancer Therapy and Imaging

Abstract: The LCTNE plays a good therapeutic and diagnostic role for subcutaneous tumors in the living animal.

Cited by 24 publications

References 43 publications

pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity

pH-sensitive and folic acid-targeted MPEG-PHIS/FA-PEG-VE mixed micelles for the delivery of PTX-VE and their antitumor activity

Co-delivery of hydrophilic gemcitabine and hydrophobic paclitaxel into novel polymeric micelles for cancer treatment

Comparison of Three Processes for Parenteral Nanoemulsion Production: Ultrasounds, Microfluidizer, and Premix Membrane Emulsification

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