Radioisotope carrying polyethylene oxide–polycaprolactone copolymer micelles for targetable bone imaging

Park, Yoon Jeong; Lee, Jue Yeon; Chang, Young Soo; Jeong, Jae Min; Chung, Jun Key; Lee, Myung Chul; Park, Kyoung Bae; Lee, Seung Jin

doi:10.1016/s0142-9612(01)00196-x

Cited by 47 publications

(23 citation statements)

References 26 publications

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“…Alterations in their properties (hydrophilic to hydrophobic) help them accumulate in tumor sites, which results in prolongation of radioisotope retention time. 128 Very few studies have been conducted using polymeric nanoparticles labeled radioisotopes for anti-tumor treatment. 129 Conventional polymeric nanoparticles from amphiphilic block or random copolymers possess insufficient functional groups for radioisotope labeling, which results in lower labeling efficiency.…”

Section: Radioisotope Loaded Nanoparticles For Tumor Targetingmentioning

confidence: 99%

Radiolabelled Nanoparticles for Diagnosis and Treatment of Cancer

Chopra¹

2011

Radioisotopes - Applications in Bio-Medical Science

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Section: Radioisotope Loaded Nanoparticles For Tumor Targetingmentioning

confidence: 99%

Radiolabelled Nanoparticles for Diagnosis and Treatment of Cancer

Chopra¹

2011

Radioisotopes - Applications in Bio-Medical Science

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“…17 A prolonged circulation time is particularly beneficial when the target of drug action is represented by circulating and bone marrow cells, as in the case of erythroid differentiating drugs. 18 Another advantage of PMs that could be important for differentiating drugs is related to the enhanced permeation retention effect. 19 This effect favors the accumulation of nanoparticles in tissues characterized by increased vascular permeability and impaired lymphatic drainage.…”

Section: Introductionmentioning

confidence: 99%

Mithramycin encapsulated in polymeric micelles by microfluidic technology as novel therapeutic protocol for beta-thalassemia

Capretto

Mazzitelli

Brognara³

et al. 2012

IJN

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This report shows that the DNA-binding drug, mithramycin, can be efficiently encapsulated in polymeric micelles (PM-MTH), based on Pluronic ® block copolymers, by a new microfluidic approach. The effect of different production parameters has been investigated for their effect on PM-MTH characteristics. The compared analysis of PM-MTH produced by microfluidic and conventional bulk mixing procedures revealed that microfluidics provides a useful platform for the production of PM-MTH with improved controllability, reproducibility, smaller size, and polydispersity. Finally, an investigation of the effects of PM-MTH, produced by microfluidic and conventional bulk mixing procedures, on the erythroid differentiation of both human erythroleukemia and human erythroid precursor cells is reported. It is demonstrated that PM-MTH exhibited a slightly lower toxicity and more pronounced differentiative activity when compared to the free drug. In addition, PM-MTH were able to upregulate preferentially γ-globin messenger ribonucleic acid production and to increase fetal hemoglobin (HbF) accumulation, the percentage of HbF-containing cells, and their HbF content without stimulating α-globin gene expression, which is responsible for the clinical symptoms of β-thalassemia. These results represent an important first step toward a potential clinical application, since an increase in HbF could alleviate the symptoms underlying β-thalassemia and sickle cell anemia. In conclusion, this report suggests that PM-MTH produced by microfluidic approach warrants further evaluation as a potential therapeutic protocol for β-thalassemia.

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“…PCL is an extremely attractive polymer for drug delivery due to the biocompatible nature of the degradation products [26] and PCL is currently approved by the FDA for use in humans. The advantage with mPEG-b-PCL micelles is that they are usually characterized by low critical micelle concentrations (CMCs) which are indicative of high stability leading to sustained drug release in the plasma [27,28], and are kinetically stable in vivo following i.v. injections into animals [29,30].…”

Section: Introductionmentioning

confidence: 99%

Formulation of a geldanamycin prodrug in mPEG-b-PCL micelles greatly enhances tolerability and pharmacokinetics in rats

Xiong

Yáñez

Remsberg

et al. 2008

Journal of Controlled Release

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Geldanamycin (GA) and its analogues inhibit heat shock protein 90 (Hsp90) and have shown significant antitumor activity in vivo; however, clinical development of GA has been hampered by its poor solubility and severe hepatotoxicity. More soluble analogues, such as 17-DMAG and 17-AAG, are easier to formulate, and have progressed through early clinical trials. However the large volume of distribution and systemic toxicity associated with these analogues may limit their distribution into tumors, thereby severely reducing efficacy and increasing nonspecific toxicities. We have evaluated a formulation of a lipophilic GA prodrug, 17′GAC 16 Br encapsulated in methoxycapped poly(ethylene glycol)-block-poly(ε-caprolactone) (mPEG-b-PCL) micelles, by comparing it to free 17-DMAG at 10 mg/kg in rats. mPEG-b-PCL micelles reported herein demonstrated substantial sustained release and conversion of 17′GAC 16 Br into 17′GAOH at significantly greater levels in all tissues analyzed compared to the free drug, allowing for a 72-fold enhancement in the AUC, a 21-fold decrease in V d , an 11-fold decrease in CL tot , and a 2-fold and 7-fold enhancement in the overall MRT of 17′GAC 16 Br and 17′GAOH, respectively. Importantly, the micellar formulation exhibited lower systemic toxicity than 17-DMAG, with a MTD > 200 mg/kg and a 2000-fold enhancement in the AUC. 17′GAC 16 Br in micelles were poorly cleared renally, in contrast to 17-DMAG and 17′GAOH, but showed preferential accumulation and prodrug conversion in reticuloendothelial organs of normal animals. Overall, the data indicates that this nanocarrier system is a promising alternative to the current 17-DMAG formulation and offers excellent potential for further pre-clinical and clinical cancer studies.

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Radioisotope carrying polyethylene oxide–polycaprolactone copolymer micelles for targetable bone imaging

Cited by 47 publications

References 26 publications

Radiolabelled Nanoparticles for Diagnosis and Treatment of Cancer

Radiolabelled Nanoparticles for Diagnosis and Treatment of Cancer

Mithramycin encapsulated in polymeric micelles by microfluidic technology as novel therapeutic protocol for beta-thalassemia

Formulation of a geldanamycin prodrug in mPEG-b-PCL micelles greatly enhances tolerability and pharmacokinetics in rats

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