Abstract：
:There are an increasing number of studies showing the order of drug presentation plays a critical role in achieving optimal combination therapy. Here, a nanoparticle design is presented using ion pairing and drug-polymer conjugate for the sequential delivery of gefitinib (Gi) and doxorubicin (Dox) targeting epidermal growth factor receptor (EGFR) signaling applicable for the treatment of triple negative breast cancers. To realize this nanoparticle design, Gi complexed with dioleoyl phosphatidic acid (DOPA) via ion paring was loaded onto the nanoparticle made of Dox-conjugated poly(l-lactide)-block-polyethylene glycol (PLA-b-PEG) and with an encapsulation efficiency of ∼90%. The nanoparticle system exhibited a desired sequential release of Gi followed by Dox, as verified through release and cellular uptake studies. The nanoparticle system demonstrated approximate 4-fold and 3-fold increases in anticancer efficacy compared to a control group of Dox-PLA-PEG conjugate against MDA-MB-468 and A549 cell lines in terms of half maximal inhibitory concentration (IC50), respectively. High tumor accumulation of the nanoparticle system was also substantiated for potential in vivo applicability by noninvasive fluorescent imaging.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Zhou Z,Jafari M,Sriram V,Kim J,Lee JY,Ruiz-Torres SJ,Waltz SEdoi
10.1021/acs.molpharmaceut.7b00669subject
Has Abstractpub_date
2017-12-04 00:00:00pages
4551-4559issue
12eissn
1543-8384issn
1543-8392journal_volume
14pub_type
杂志文章abstract：:The purpose of this study was to determine the effect of PEGylation on the interaction of poly(amidoamine) (PAMAM) dendrimer nanocarriers (DNCs) with in vitro and in vivo models of the pulmonary epithelium. Generation-3 PAMAM dendrimers with varying surface densities of PEG 1000 Da were synthesized and characterized. ...
journal_title：Molecular pharmaceutics
pub_type： 杂志文章
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abstract：:Colistin has been increasingly used for the treatment of respiratory infections caused by Gram-negative bacteria. Unfortunately parenteral administration of colistin can cause severe adverse effects. This study aimed to develop an inhaled combination dry powder formulation of colistin and rifapentine for the treatment...
journal_title：Molecular pharmaceutics
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doi：10.1021/mp500586p
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abstract：:Resveratrol (RES) is a nutraceutical with promising anti-inflammatory properties for the treatment of inflammatory bowel diseases (IBD). However, the clinical effectiveness of resveratrol as an oral anti-inflammatory agent is hindered by its extremely poor solubility and poor stability. In this study, we encapsulated ...
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doi：10.1021/acs.molpharmaceut.0c00048
更新日期：2021-02-01 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/acs.molpharmaceut.5b00805
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更新日期：2017-11-06 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/mp300633f
更新日期：2014-02-03 00:00:00
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doi：10.1021/acs.molpharmaceut.7b00662
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
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更新日期：2012-03-05 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/mp300476z
更新日期：2013-04-01 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/mp4000184
更新日期：2013-04-01 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/mp500464b
更新日期：2015-04-06 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/mp500290f
更新日期：2014-09-02 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/mp400104b
更新日期：2013-09-03 00:00:00
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pub_type： 杂志文章
doi：10.1021/acs.molpharmaceut.9b00458
更新日期：2019-09-03 00:00:00
abstract：:Lipid-based drug delivery systems have been vastly investigated as a pharmaceutical method to enhance oral absorption of lipophilic drugs. However, these vehicles not only affect drug bioavailability but may also have an impact on gastric emptying, drug disposition, lymphatic absorption and be affected by lipid digest...
journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/acs.molpharmaceut.0c00141
更新日期：2020-06-01 00:00:00
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journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/acs.molpharmaceut.6b00788
更新日期：2017-01-03 00:00:00
abstract：:Rho-GTPases are small GTP-binding proteins that contribute to the epithelial-to-mesenchymal transition by regulating several cellular processes including organization of the actin cytoskeleton, cell motility, transcription, and cell proliferation. Overexpression of RhoC-GTPases (RhoC) in breast cancer has been implica...
journal_title：Molecular pharmaceutics
pub_type： 杂志文章
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更新日期：2015-07-06 00:00:00
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journal_title：Molecular pharmaceutics
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更新日期：2017-07-03 00:00:00
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doi：10.1021/mp500056d
更新日期：2014-11-03 00:00:00
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更新日期：2013-06-03 00:00:00
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更新日期：2015-03-02 00:00:00
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更新日期：2014-09-02 00:00:00
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更新日期：2015-03-02 00:00:00
abstract：:Contrast-enhanced ultrasound imaging has shown promise in the field of molecular imaging. This technique relies upon the adhesion of ultrasound contrast agent (UCA) to targeted molecular markers of disease. This is accomplished by coating the surface of the contrast agent with a ligand that specifically binds to the i...
journal_title：Molecular pharmaceutics
pub_type： 杂志文章
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更新日期：2006-09-01 00:00:00
abstract：:Interest in the use of 225Ac for targeted alpha therapies has increased dramatically over the past few years, resulting in a multitude of new isotope production and translational research efforts. However, 225Ac radioimmunoconjugate (RIC) research is still in its infancy, with most prior experience in hematologic mali...
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doi：10.1021/acs.molpharmaceut.0c00703
更新日期：2020-11-02 00:00:00
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journal_title：Molecular pharmaceutics
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更新日期：2013-08-05 00:00:00
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更新日期：2017-06-05 00:00:00
abstract：:We investigated the effects of the hot-melt extrusion (HME) process on the properties of itraconazole (ITZ) amorphous solid dispersions made by thin film freezing (TFF) technology. The ITZ-HPMCAS L (1:2) TFF composition exhibited limited drug release in acidic media. HME of the ITZ-HPMCAS TFF composition with hydrophi...
journal_title：Molecular pharmaceutics
pub_type： 杂志文章
doi：10.1021/mp4003706
更新日期：2014-01-06 00:00:00
