Drug-Polymer Interaction, Pharmacokinetics and Antitumor Effect of PEG-PLA/Taxane Derivative TM-2 Micelles for Intravenous Drug Delivery

Wang, Qiao; Liu, Yi; Pu, Chenguang; Zhang, Hongjuan; Tan, Xinyi; Gou, Jingxin; He, Haibing; Yin, Tian; Wang, Yanjiao

doi:10.1007/s11095-018-2477-3

Cited by 14 publications

(7 citation statements)

References 33 publications

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“…Also, the incorporation of 5 wt% PDLLA 10K resulted in enhanced drug loading of mPEG 2k -b-PDLLA 2.4k micelles(Table I, F1-F2). However, longer PDLLA blocks were considered to have poorer compatibility with TM-2 in the previous publication (19). Similarly, such a phenomenon also appeared in our experiments, where the incorporation of more PDLLA 10k reduced the drug loading (Table I, F3-F6).…”

Section: Preparation and Characterization Of Micellessupporting

confidence: 83%

“…The mPEG 2k -b-PDLLA 2.4k micelles with or without 5 wt% PDLLA 10k were diluted to contain approximately 200 μg/ml of TM-2. The experimental method was in accordance with our previous study, in which the temperatures were set at 20°C and 45°C (19). (Details of the measurements is described in the Supplementary Material).…”

Section: Stability Of Micellesmentioning

confidence: 99%

“…(Figure S4) The particle size changes of micelles before and after lyophilization were measured by DLS to evaluate the efficacy of lyophilization protectants. In addition, XRD (D/MAX-2400, Japan), DSC (DSC-60, Japan), and FTIR (Bruker IFS 55, Germany) were used to study the potential mechanism of lyophilization protectants (19,20). (Details of the measurements is described in the Supplementary Material).…”

Section: Screening Of Lyophilization Protectantmentioning

confidence: 99%

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Improved Core Viscosity Achieved by PDLLA10kCo-Incorporation Promoted Drug Loading and Stability of mPEG2k-b-PDLLA2.4k Micelles

et al. 2022

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Purpose This study aims to investigate the effect of poly(D, Llactic acid) 10K (PDLLA 10K ) incorporation on the drug loading and stability of poly(ethylene glycol) 2K -block-poly(D, Llactide) 2.4K (mPEG 2k -b-PDLLA 2.4k ) micelles. In addition, a suitable lyophilization protector was screened for this micelle to obtain favorable lyophilized products. Methods The incorporation ratios of PDLLA 10k were screened based on the particle size and drug loading. The dynamic stability, core viscosity, drug release, stability in albumin, and in vivo pharmacokinetic characteristics of PDLLA 10k incorporated micelles were compared with the original micelles. In addition, the particle size variation was used as an indicator to screen the most suitable lyophilization protectant for the micelles. DSC, FTIR, XRD were used to illustrate the mechanism of the lyophilized protectants. Results After the incorporation of 5 wt% PDLLA 10K , the maximum loading of mPEG 2k -b-PDLLA 2.4k micelles for TM-2 was increased from 26 wt% to 32 wt%, and the in vivo half-life was increased by 2.25-fold. Various stability of micelles was improved. Also, the micelles with hydroxypropyl-β-cyclodextrin (HP-β-CD) as lyophilization protectants had minimal variation in particle size. Conclusions PDLLA 10k incorporation can be employed as a strategy to increase the stability of mPEG 2k -b-PDLLA 2.4k micelles, which can be attributed to the viscosity building effect. HP-β-CD can be used as an effective lyophilization protectant since mPEG and HP-β-CD form the pseudopolyrotaxanesque inclusion complexes.

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Section: Preparation and Characterization Of Micellessupporting

confidence: 83%

Section: Stability Of Micellesmentioning

confidence: 99%

Section: Screening Of Lyophilization Protectantmentioning

confidence: 99%

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Improved Core Viscosity Achieved by PDLLA10kCo-Incorporation Promoted Drug Loading and Stability of mPEG2k-b-PDLLA2.4k Micelles

et al. 2022

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“…PMs are definition via the capacity of the co-polymer to selfassemble into nanoscale aggregates that have a hydrophilic shell and hydrophobic core. The hydrophobic core of PMs provided a home for water-insoluble drugs and the hydrophilic shell could be well isolated the external environment and avoid cargo drugs being quickly degraded [19,20]. However, ideal PMs not only co-loaded multidrug but also possessed excellent physical properties such as suitable size distribution, morphology and blood stability.…”

Section: Polymer Micellesmentioning

confidence: 99%

Intelligent polymeric micelles for multidrug co-delivery and cancer therapy

Ning

et al. 2019

Artificial Cells, Nanomedicine, and Biotechnology

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Polymeric micelles (PMs) play a vital role in multidrug co-delivery and cancer treatment. However, development of intelligent PMs further allows PMs to accurately target tumour, selectively release cargo multidrug and increase uptake. Therefore, targets, controlled release and uptake of intelligent PMs should be paid more attention to improvement of synergistic therapeutic outcomes and minimize side effects. In this review, tumour targeting of co-delivery intelligent PMs and its intracellular trafficking mechanisms were overviewed. And this review provides a comprehensive summarization of several intelligent co-delivery PMs. Such a system could control the multidrug to be released simultaneously or sequentially by special properties of tumour microenvironment (TME) (including acidic PH, redox, overexpressed enzyme, excessive temperature) and external environment trigger. Additionally, limitations, clinical translation and future perspectives of intelligent co-delivery PMs were also being discussed in this article.

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“…Moreover, the final sample may contain traces of organic solvents. The successful attempts to obtain narrowly distributed mixed micelles with relatively small size were successful either by use of oligomers of polylactide or by exclusion of polydisperse large fractions by nanofiltration [ 61 ]. There exists a direct dissolution approach and, if the copolymer is relatively water soluble, this approach can be used to form micelles.…”

Section: Introductionmentioning

confidence: 99%

Ultrasonic Film Rehydration Synthesis of Mixed Polylactide Micelles for Enzyme-Resistant Drug Delivery Nanovehicles

et al. 2022

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A facile technique for the preparation of mixed polylactide micelles from amorphous poly-D,L-lactide-block-polyethyleneglycol and crystalline amino-terminated poly-L-lactide is described. In comparison to the classical routine solvent substitution method, the ultrasonication assisted formation of polymer micelles allows shortening of the preparation time from several days to 15–20 min. The structure and morphology of mixed micelles were analyzed with the assistance of electron microscopy, dynamic and static light scattering and differential scanning calorimetery. The resulting polymer micelles have a hydrodynamic radius of about 150 nm and a narrow size distribution. The average molecular weight of micelles was found to be 2.1 × 107 and the aggregation number was calculated to be 6000. The obtained biocompatible particles were shown to possess low cytotoxicity, high colloid stability and high stability towards enzymatic hydrolysis. The possible application of mixed polylactide micelles as drug delivery vehicles was studied for the antitumor hydrophobic drug paclitaxel. The lethal concentration (LC50) of paclitaxel encapsulated in polylactide micelles was found to be 42 ± 4 µg/mL—a value equal to the LC50 of paclitaxel in the commercial drug Paclitaxel-Teva.

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Drug-Polymer Interaction, Pharmacokinetics and Antitumor Effect of PEG-PLA/Taxane Derivative TM-2 Micelles for Intravenous Drug Delivery

Abstract: TM-2 micelles with high drug loading increased drug solubility, improved tolerance, antitumor effects and reduced toxicity.

Cited by 14 publications

References 33 publications

Improved Core Viscosity Achieved by PDLLA10kCo-Incorporation Promoted Drug Loading and Stability of mPEG2k-b-PDLLA2.4k Micelles

Improved Core Viscosity Achieved by PDLLA10kCo-Incorporation Promoted Drug Loading and Stability of mPEG2k-b-PDLLA2.4k Micelles

Intelligent polymeric micelles for multidrug co-delivery and cancer therapy

Ultrasonic Film Rehydration Synthesis of Mixed Polylactide Micelles for Enzyme-Resistant Drug Delivery Nanovehicles

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