ArticlePharmaceutical research2000
Formulation development and antitumor activity of a filter-sterilizable emulsion of paclitaxel.
Article in Pharmaceutical research, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers, 2 of them syntheses that pooled it.
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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.
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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.
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Who cites it
27 citing papers in PubMed, 2 syntheses or guidelines pooled it, 130 citations in OpenAlex.
- Improvement of Paclitaxel-Associated Adverse Reactions (ADRs) via the Use of Nano-Based Drug Delivery Systems: A Systematic Review and Network Meta-Analysis.International journal of nanomedicine · 2020Pooled it
- Meta-analysis of nanoparticulate paclitaxel delivery system pharmacokinetics and model prediction of associated neutropenia.Pharmaceutical research · 2012Pooled it
- Nanoemulsions a Delivery System in the Making for Tumor Targeting Therapeutics: Evaluation and Characterization to Meet Clinical Challenges.Current pharmaceutical biotechnology · 2025Review
- Article
- Paclitaxel loaded EDC-crosslinked fibroin nanoparticles: a potential approach for colon cancer treatment.Drug delivery and translational research · 2020Article
- Development and in-vitro characterization of nanoemulsions loaded with paclitaxel/γ-tocotrienol lipid conjugates.International journal of pharmaceutics · 2018Article
- Synthesis, characterization, and in-vitro antitumor activity of the polyethylene glycol (350 and 1000) succinate derivatives of the tocopherol and tocotrienol isomers of Vitamin E.International journal of pharmaceutics · 2017Article
- Developments in Methods for Measuring the Intestinal Absorption of Nanoparticle-Bound Drugs.International journal of molecular sciences · 2016Review
- Pharmacokinetics of quercetin-loaded nanodroplets with ultrasound activation and their use for bioimaging.International journal of nanomedicine · 2015Article
- Duel-acting subcutaneous microemulsion formulation for improved migraine treatment with zolmitriptan and diclofenac: formulation and in vitro-in vivo characterization.The AAPS journal · 2014Article
- A critical review of lipid-based nanoparticles for taxane delivery.Cancer letters · 2013Review
- Paclitaxel Nano-Delivery Systems: A Comprehensive Review.Journal of nanomedicine & nanotechnology · 2013Article
- Designing Paclitaxel drug delivery systems aimed at improved patient outcomes: current status and challenges.ISRN pharmacology · 2012Article
- Development of lipid-based nanoparticles for enhancing the oral bioavailability of paclitaxel.AAPS PharmSciTech · 2011Article
- Physicochemical properties and biocompatibility of a polymer-paclitaxel conjugate for cancer treatment.International journal of nanomedicine · 2011Article
- Injectable lipid emulsions-advancements, opportunities and challenges.AAPS PharmSciTech · 2010Review
- Development of new lipid-based paclitaxel nanoparticles using sequential simplex optimization.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2009Article
- A novel camptothecin derivative incorporated in nano-carrier induced distinguished improvement in solubility, stability and anti-tumor activity both in vitro and in vivo.Pharmaceutical research · 2009Article
- Micellar nanocarriers: pharmaceutical perspectives.Pharmaceutical research · 2007Review
- Advances in the use of tocols as drug delivery vehicles.Pharmaceutical research · 2006Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposePaclitaxel is currently administered i.v. as a slow infusion of a solution of the drug in an ethanol:surfactant:saline admixture. However, poor solubilization and toxicity are associated with this drug therapy. Alternative drug delivery systems, including parenteral emulsions, are under development in recent years to reduce drug toxicity, improve efficacy and eliminate premedication.
methodsPaclitaxel emulsions were prepared by high-shear homogenization. The particle size of the emulsions was measured by dynamic light scattering. Drug concentration was quantified by HPLC and in vitro drug release was monitored by membrane dialysis. The physical stability of emulsions was monitored by particle size changes in both the mean droplet diameter and 99% cumulative distribution. Paclitaxel potency and changes in the concentration of known degradants were used as chemical stability indicators. Single dose acute toxicity studies were conducted in healthy mice and efficacy studies in B 16 melanoma tumor-bearing mice.
resultsQW8184, a physically and chemically stable sub-micron oil-in-water (o/w) emulsion of paclitaxel, can be prepared at high drug loading (8-10 mg/mL) having a mean droplet diameter of <100 nm and 99% cumulative particle size distribution of <200 nm. In vitro release studies demonstrated low and sustained drug release both in the presence and absence of human serum albumin. Based on single dose acute toxicity studies, QW8184 is well tolerated both in mice and rats with about a 3-fold increase in the maximum-tolerated-dose (MTD) over the current marketed drug formulation. Using the B16 mouse melanoma model, a significant improvement in drug efficacy was observed with QW8184 over Taxol.
conclusionsQW8184, a stable sub-micron o/w emulsion of paclitaxel has been developed that can be filter-sterilized and administered i.v. as a bolus dose. When compared to Taxol, this emulsion exhibited reduced toxicity and improved efficacy most likely due to the composition and dependent physicochemical characteristics of the emulsion.
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Registered trials
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.