Pharmaceutical composition used for reducing damage caused by free radicals
Inventors
Chen, Chia-Hung • Wang, Chau-Hui • Lin, John-Son • Chiu, Tieh-Hsiung • Chen, Jing-Yi • Liao, Pi-Hung • Su, Chia-Chi • Liao, Wei-Chuan
Assignees
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Publication Number
US-9700623-B2
Publication Date
2017-07-11
Expiration Date
Abstract
The present invention features a pharmaceutical composition used for reducing the damage caused by free radicals, which comprises at least a metal or its ions, at least a drug or an antioxidant that is carrier-protected/modified, and a drug carrier. Said carrier helps to preserve the anti-oxidative activity, and hence, prevents the decrease of the effect of the antioxidant against free radicals produced in the environment or body fluids and prolongs protection, and may be used for reducing damage caused by radiation and adverse effects induced by chemotherapeutic drugs.
Core Innovation
The invention relates to a metal-ion micelle/pharmaceutical composition that encapsulates amifostine within a polymer drug carrier. The composition uses a metal ion as a micelle core while the polymer provides a self-assembled structure that coordinates with the metal.
The composition is formed by self-assembly of iron and poly(ethylene glycol)-b-poly(glutamic acid) via coordinate bonding. The center of the pharmaceutical composition consists of the iron and is enclosed by amifostine, while the outer layer is made of poly(ethylene glycol)-b-poly(glutamic acid). The resulting structure is described as a metal-core micelle structure, referred to in the example as FePA (iron/PEG-b-PGA/amifostine).
The document addresses the reduction of damage caused by free radicals by combining iron with amifostine in a self-assembled polymeric micelle. It emphasizes altered distribution and delayed release, along with prolonged protection against radiation and chemotherapy-induced toxicity.
Claims Coverage
The provided partial content contains 1 independent claim, which specifies a pharmaceutical composition with iron, amifostine, and poly(ethylene glycol)-b-poly(glutamic acid) arranged in a self-assembled coordinate-bonded micelle structure.
Self-assembled coordinate-bonded iron and PEG-b-PGA micelle core
The pharmaceutical composition is formed by self-assembly of iron and poly(ethylene glycol)-b-poly(glutamic acid) via coordinate bonding.
Iron at the center enclosed by amifostine
The center of the pharmaceutical composition consists of iron and is enclosed by amifostine.
Outer layer made of PEG-b-PGA
An outer layer is made of poly(ethylene glycol)-b-poly(glutamic acid).
Pharmaceutical composition for reducing free-radical damage
A pharmaceutical composition used for reducing damage caused by free radicals, comprising iron and amifostine together with poly(ethylene glycol)-b-poly(glutamic acid).
Overall, the claim coverage is limited to a specific structural arrangement: a coordinate-bonded self-assembled micelle with an iron center, amifostine enclosed in the center region, and poly(ethylene glycol)-b-poly(glutamic acid) forming the outer layer, for reducing free-radical damage.
Stated Advantages
Prolonged protection against radiation and chemotherapy-induced toxicity.
Reduced damage caused by free radicals.
Documented Applications
In vitro DNA protection after UVB irradiation, reported using a Comet assay (DNA tail % TDNA).
In vivo acute radiation protection in NMRI mice, reported using WBC counts and survival improvements.
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