Evidence map›Paper›PMID 33532191›Full record

ArticleActa pharmaceutica Sinica. B2021

A facile and universal method to achieve liposomal remote loading of non-ionizable drugs with outstanding safety profiles and therapeutic effect.

Shuang Zhou, Jinbo Li, Jiang Yu, Liyuan Yang, Xiao Kuang, Zhenjie Wang, Yingli Wang, Hongzhuo Liu, Guimei Lin, Zhonggui He and 2 more

Open access · diamondAbstract read
In one paragraph

Article in Acta pharmaceutica Sinica. B, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.3field-weighted citation impact, top 23% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

10 citing papers in PubMed, 29 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors at 1 institution in 1 country.

Shuang ZhouWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Jinbo LiWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Jiang YuWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Liyuan YangWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Xiao KuangWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Zhenjie WangWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Yingli WangWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Hongzhuo LiuWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Guimei LinSchool of Pharmaceutical Science, Shandong University, Jinan 250012, China.
Zhonggui HeWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Dan LiuKey Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.
Yongjun WangWuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
Shenyang Pharmaceutical University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Liposomes have made remarkable achievements as drug delivery vehicles in the clinic. Liposomal products mostly benefited from remote drug loading techniques that succeeded in amphipathic and/or ionizable drugs, but seemed impracticable for nonionizable and poorly water-soluble therapeutic agents, thereby impeding extensive promising drugs to hitchhike liposomal vehicles for disease therapy. In this study, a series of weak acid drug derivatives were designed by a simplistic one step synthesis, which could be remotely loaded into liposomes by pH gradient method. Cabazitaxel (CTX) weak acid derivatives were selected to evaluate regarding its safety profiles, pharmacodynamics, and pharmacokinetics. CTX weak acid derivative liposomes were superior to Jevtana® in terms of safety profiles, including systemic toxicity, hematological toxicity, and potential central nerve toxicity. Specifically, it was demonstrated that liposomes had capacity to weaken potential toxicity of CTX on cortex and hippocampus neurons. Significant advantages of CTX weak acid derivative-loaded liposomes were achieved in prostate cancer and metastatic cancer therapy resulting from higher safety and elevated tolerated doses.

Indexed as

AUC0‒t, area under the curveCabazitaxelCancerChol, cholesterolCR, creatinineCTX, cabazitaxelDA-CTX, cabazitaxel trans-2-butene-1,4-dicarboxylic acid derivateDA, trans-2-butene-1,4-dicarboxylic acidDSPC, 1,2-dioctadecanoyl-sn-glycero-3-phophocholineDSPE-PEG2000, 2-distearoyl-snglycero-3-phosphoethanolamine-N-[methyl(polyethylene glycol)-2000EE, encapsulation efficiencyEPR, enhanced permeability and retentionGA-CTX, cabazitaxel glutaric acid derivateGA, glutaric anhydridelipo DA-CTX, DA-CTX liposomelipo GA-CTX, GA-CTX liposomelipo SA-CTX, SA-CTX liposomeLung metastasismCRPCa, metastatic castration-resistant prostate cancerMED, minimum effective doseMPS, mononuclear phagocyte systemMTD, maximum tolerated doseNon-ionizable drugsPCa, prostate cancerPSA, prostate-specific antigenRemote loading liposomeSA-CTX, cabazitaxel succinic acid derivateSafetySA, succinic anhydrideTI, therapeutic indexTolerated dosesWeak acid derivatives

Identifiers

PMID33532191
PMCPMC7838024
OpenAlexW3048570719

What OpenQuestion holds

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LicenceCC BY-NC-ND
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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.