Formulation, characterization and tissue distribution of a novel pH-sensitive long-circulating liposome-based theranostic suitable for molecular imaging and drug delivery

Duan, Yin; Wei, Lihui; Petryk, Julia; Ruddy, Terrence D.

doi:10.2147/ijn.s111274

Cited by 30 publications

(18 citation statements)

References 45 publications

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“…According to the stability test performed at room temperature (25°C), the radiolabeling efficiency was remained stable with some insignificant alterations and degradations carried out at 25°C for 24 h ( Table 1). Any significant difference was not observed in the serum and saline stability of 99m Tc-Levofloxacin and 99m Tc-micelles which were in agreement with the literature [36,55,63,64].…”

Section: In Vitro Stability Studiessupporting

confidence: 92%

99mTc-radiolabeled Levofloxacin and micelles as infection and inflammation imaging agents

Silindir-Gunay

Özer

2020

Journal of Drug Delivery Science and Technology

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A B S T R A C T Easy and early detection of infection and inflammation is essential for early and effective treatment. In this study, PEGylated micelles were designed and both micelles and Levofloxacin were radiolabeled with 99m TcO 4 to develop potential radiotracers for detection of infection/inflammation. Radiolabeling efficiency, in vitro stability and bacterial binding of 99m Tc-Levofloxacin and 99m Tc-micelles were compared. The aim of this study is to formulate and compare 99m Tc-Levofloxacin and 99m Tc-micelles as infection and inflammation agents having different mechanisms for the accumulation at infection and inflammation site. PEGylated micelles were designed with a particle size of 80 ± 0.7 nm and proper characterization properties. High radiolabeling efficiency was achieved for 99m Tc-Levofloxacin (96%) and 99m Tc-micelles (87%). The radiolabeling efficiency was remained stable with some insignificant alterations for both radiotracers at 25°C for 24 h. Although in vitro bacterial binding of 99m Tc-levofloxacine was higher than 99m Tc-micelles, 99m Tc-micelles may also be evaluated potential agent due to long circulation and passive accumulation mechanisms at infection/inflammation site. Both radiopharmaceutical agents exhibit potential results in design, characterization, radiolabeling efficiency and in vitro bacterial binding point of view.

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Section: In Vitro Stability Studiessupporting

confidence: 92%

99mTc-radiolabeled Levofloxacin and micelles as infection and inflammation imaging agents

Silindir-Gunay

Özer

2020

Journal of Drug Delivery Science and Technology

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“…In the first series of Cuphen nanoformulations (F1, F2, F3 and F4), Chol was included in the lipid composition. A second series of pH-sensitive nanoformulations (F5, F6 and F7) was developed to explore Cuphen release at the slightly acidic tumour microenvironment [28,29]. To attain this goal, CHEMS was included in the lipid composition since, when in contact with an acidic milieu, it becomes protonated, leading to bilayer disruption and subsequent drug release [29,[39][40][41].…”

Section: Physicochemical Characterization Of Cuphen Nanoliposomesmentioning

confidence: 99%

“…Tumours' microenvironment, as in the case of melanoma, is slightly acidic, presenting pH values around 6, in contrast to the normal physiological pH of 7.4 [28,29], which heavily impacts cancer development [47,48], and it can be explored as stimuli for triggering local liposomal drug release. In the current work, we developed long circulating pH-sensitive nanoliposomes by including CHEMS in the lipid composition [29,[39][40][41]. To validate pH-sensitive properties of F6, the quantification of the metallodrug still associated to nanoliposomes was assessed upon exposure to different pH conditions.…”

Section: Cuphen Ph-sensitive Nanoliposomesmentioning

confidence: 99%

“…For taking advantage of this effect, long blood circulation times are required, and the drug should remain associated within nanoliposomes [27]. Moreover, the microenvironment of solid tumours, as in the case of melanoma, is slightly acidic, exhibiting pH values around 6, in contrast to pH 7.4 displayed by healthy tissues [28,29]. Combining these two features, a pH-triggered Cuphen release from long circulating nanoliposomes constituted one of the goals of the present work.…”

Section: Introductionmentioning

confidence: 99%

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Copper Complex Nanoformulations Featuring Highly Promising Therapeutic Potential in Murine Melanoma Models

Pinho

Amaral

Castro

et al. 2019

Nanomedicine (Lond.)

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Aim: Preclinical evaluation of a cytotoxic copper (II) complex formulated in long circulating nanoliposomes for melanoma treatment. Materials & methods: Liposomal nanoformulations of the copper complex were characterized in terms of thermodynamic behavior (differential scanning calorimeter), pH-sensitivity (spectrophotometry) and antiproliferative effects against murine melanoma B16F10 cells in vitro. Preclinical studies were performed in a C57BL/6 syngeneic melanoma model. Results: Nanoformulations were thermodynamically stable, and CHEMS-containing nanoliposomes were pH-sensitive and preserved the antiproliferative properties of the copper compound. These nanoformulations significantly impaired tumor progression in vivo, devoid of toxic side effects, compared with control mice or mice treated with the free metallodrug. Conclusion: Copper complex-containing nanoliposomes demonstrate high anticancer efficacy and safety, constituting a step forward to the development of more effective therapeutic strategies against melanoma.

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“…Decrease of pH leads to the neutralization of the CHEMS molecule and causes the liposomal aggregations and the release of the encapsulated compound. 23 Polyelectrolytes, such as polyacrylic acid 24,25 or carboxylated hyaluronic acid, 26 have also been used as pH-sensitive agents for liposomes, as they become hydrophilic with the decrease of pH value and, thus, disrupt a liposomal membrane. The formation of sterically stabilized polyethyleneglycol (PEG)-phenyl vinyl ether (PIVE)-lipid conjugate liposomes was recently reported.…”

Section: Introductionmentioning

confidence: 99%

<p>Modification of fliposomes with a polycation can enhance the control of pH-induced release</p>

Lokova

Zaborova

2019

IJN

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PurposeNowadays, the development of stimuli-sensitive nanocontainers for targeted drug delivery is of great value. Encapsulation of a drug in a pH-sensitive liposomal container not only provides protective and transport functions, but also helps to create a system with a controlled release mechanism.MethodsIn this study, we investigated the influence of a cationic polypeptide on the pH-induced release of anticancer drug doxorubicin (DXR) from the anionic fliposomes – liposomes consisting of a neutral lipid, an anionic lipid (prone to interact with a polycation), and a lipid trigger (imparting the pH-sensitivity).ResultsFirst, we showed the possibility to control the pH-induced release by the simple modification of the anionic fliposomes with linear polylysine. Second, we optimized the fliposomal composition such that the obtained fliposomes responded to the pH changes only when complexed with the polycation (“turning on” the release). Finally, pH-induced release from the polylysine-modified anionic fliposomes was tested on an anticancer drug DXR.ConclusionWe have succeeded in developing “smart” stimuli-sensitive nanocontainers capable of tunable controlled release of a drug. Moreover, based on the data on release of a low molecular salt, one can predict the release profile of DXR.

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Formulation, characterization and tissue distribution of a novel pH-sensitive long-circulating liposome-based theranostic suitable for molecular imaging and drug delivery

Cited by 30 publications

References 45 publications

99mTc-radiolabeled Levofloxacin and micelles as infection and inflammation imaging agents

99mTc-radiolabeled Levofloxacin and micelles as infection and inflammation imaging agents

Copper Complex Nanoformulations Featuring Highly Promising Therapeutic Potential in Murine Melanoma Models

<p>Modification of fliposomes with a polycation can enhance the control of pH-induced release</p>

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