ArticleJournal of the American Chemical Society2016
Oligo(lactic acid)n-Paclitaxel Prodrugs for Poly(ethylene glycol)-block-poly(lactic acid) Micelles: Loading, Release, and Backbiting Conversion for Anticancer Activity.
Article in Journal of the American Chemical Society, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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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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Who cites it
23 citing papers in PubMed, 65 citations in OpenAlex.
- Precise Ratiometric Drug Delivery for the Treatment of Triple-Negative Breast Cancer.ACS nano · 2025Article
- Crystallization of supersaturated PEG-b-PLA for the production of drug-loaded polymeric micelles.Journal of controlled release : official journal of the Controlled Release Society · 2025Article
- Clinical Applications of Targeted Nanomaterials.Pharmaceutics · 2025Review
- Review
- Self-assembled nanoformulations of paclitaxel for enhanced cancer theranostics.Acta pharmaceutica Sinica. B · 2023Review
- Plasma Stability and Plasma Metabolite Concentration-Time Profiles of Oligo(Lactic Acid)The AAPS journal · 2023Article
- Smart drug delivery systems for precise cancer therapy.Acta pharmaceutica Sinica. B · 2022Review
- Production of paclitaxel-loaded PEG-b-PLA micelles using PEG for drug loading and freeze-drying.Journal of controlled release : official journal of the Controlled Release Society · 2022Article
- Review
- Oligo(Lactic Acid)Nanomaterials (Basel, Switzerland) · 2021Article
- Balancing the stability and drug activation in adaptive nanoparticles potentiates chemotherapy in multidrug-resistant cancer.Theranostics · 2021Article
- Loading-Dependent Structural Model of Polymeric Micelles Encapsulating Curcumin by Solid-State NMR Spectroscopy.Angewandte Chemie (International ed. in English) · 2019Article
- A Photocleavable Amphiphilic Prodrug Self-Assembled Nanoparticles with Effective Anticancer Activity In Vitro.Nanomaterials (Basel, Switzerland) · 2019Article
- Poly(ethylene glycol)-block-poly(d,l-lactic acid) micelles containing oligo(lactic acid)Journal of controlled release : official journal of the Controlled Release Society · 2019Article
- Oligo(Lactic Acid)Pharmaceutical research · 2019Article
- Orthogonal self-assembly of an organoplatinum(II) metallacycle and cucurbit[8]uril that delivers curcumin to cancer cells.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Stereocomplex Prodrugs of Oligo(lactic acid)ACS nano · 2018Article
- Polylactide-tethered prodrugs in polymeric nanoparticles as reliable nanomedicines for the efficient eradication of patient-derived hepatocellular carcinoma.Theranostics · 2018Article
- Pre-clinical evaluation of a themosensitive gel containing epothilone B and mTOR/Hsp90 targeted agents in an ovarian tumor model.Journal of controlled release : official journal of the Controlled Release Society · 2017Article
- Preclinical development of drug delivery systems for paclitaxel-based cancer chemotherapy.Journal of controlled release : official journal of the Controlled Release Society · 2017Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Poly(ethylene glycol)-block-poly(d,l-lactic acid) (PEG-b-PLA) micelles are nanocarriers for poorly water-soluble anticancer agents and have advanced paclitaxel (PTX) to humans due to drug solubilization, biocompatibility, and dose escalation. However, PEG-b-PLA micelles rapidly release PTX, resulting in widespread biodistribution and low tumor exposure. To improve delivery of PTX by PEG-b-PLA micelles, monodisperse oligo(l-lactic acid), o(LA)8 or o(LA)16, has been coupled onto PTX at the 7-OH position, forming ester prodrugs: o(LA)8-PTX and o(LA)16-PTX, respectively. As expected, o(LA)n-PTX was more compatible with PEG-b-PLA micelles than PTX, increasing drug loading from 11 to 54%. While in vitro release of PTX was rapid, resulting in precipitation, o(LA)n-PTX release was more gradual: t1/2 = 14 and 26 h for o(LA)8-PTX and o(LA)16-PTX, respectively. Notably, o(LA)8-PTX and o(LA)16-PTX in PEG-b-PLA micelles resisted backbiting chain end scission, based on reverse-phase HPLC analysis. By contrast, o(LA)8-PTX and o(LA)16-PTX degraded substantially in 1:1 acetonitrile:10 mM PBS, pH 7.4, at 37 °C, generating primarily o(LA)2-PTX. The IC50 value of o(LA)2-PTX was ∼2.3 nM for A549 human lung cancer cells, equipotent with PTX in vitro. After weekly IV injections at 20 mg/kg as PEG-b-PLA micelles, o(LA)8-PTX induced tumor regression in A549 tumor-bearing mice, whereas PTX delayed tumor growth. Surprisingly, o(LA)8-PTX caused less toxicity than PTX in terms of change in body weight. In conclusion, o(LA)n acts as a novel promoiety, undergoing backbiting conversion without a reliance on metabolizing enzymes, and o(LA)n-PTX improves PTX delivery by PEG-b-PLA micelles, providing a strong justification for clinical evaluation.
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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.