The DOI matches its Crossref record; 13 of the 13 references it cites were found in a registry or an index.
In Vivo Antitumor Activity of the Folate-Conjugated pH-Sensitive Polymeric Micelle Selectively Releasing Adriamycin in the Intracellular Acidic Compartments
Abstract
Cancer treatment efficacy and safety of the environmentally sensitive polymeric micelle drug carriers were significantly increased by optimizing the number of ligands on their surface. These micelles were designed to target the cancerous tumors through the interaction between folate and its receptors that overexpress on the cancer cell membrane while achieving pH-controlled drug release in the intracellular acidic compartments such as endosomes and lysosomes. In order to elucidate the effects of folate on cytotoxicity, biodistribution, anticancer activity, and pharmacological properties, folate concentration on the surface of the micelles was controlled by precise synthesis of two different amphiphilic block copolymers that self-assemble into spherical micelles, folate-poly(ethylene glycol)-poly(aspartate-hydrazone-adriamycin) with gamma-carboxylic acid activated folate and methoxy-poly(ethylene glycol)-poly(aspartate-hydrazone-adriamycin) without folate. It is of significance that, although folate conjugation induced an extremely small change in tumor accumulation of the micelles, folate-conjugated micelles showed lower in vivo toxicity and higher antitumor activity over a broad range of the dosage from 7.50 to 26.21 mg/kg, which was 5-fold broader than free drugs.
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Cites
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Polymers for Drug Delivery Systems
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Self-citationStimuli-Responsive Polymersomes for Programmed Drug Delivery
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Metadata
- Authors
- Bae, Y., Nishiyama, N., & Kataoka, K.
- Venue
- Bioconjugate Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2007-05-09
- Volume
- 18
- Issue
- 4
- Pages
- 1131-1139
- ISSN
- 1043-1802 (ISSN-L)
- 1520-4812
- OpenAlex
- W1982089656
- Cited by
- 278
- References
- 13
- FWCI
- 10.76
- Type
- journal article
- Language
- en
- Open access
- closed
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