Poly(ethylene glycol)-Prodrug Conjugates: Concept, Design, and Applications
نویسندگان
چکیده
Poly(ethylene glycol) (PEG) is the most widely used polymer in delivering anticancer drugs clinically. PEGylation (i.e., the covalent attachment of PEG) of peptides proteins, drugs, and bioactives is known to enhance the aqueous solubility of hydrophobic drugs, prolong circulation time, minimize nonspecific uptake, and achieve specific tumor targetability through the enhanced permeability and retention effect. Numerous PEG-based therapeutics have been developed, and several have received market approval. A vast amount of clinical experience has been gained which has helped to design PEG prodrug conjugates with improved therapeutic efficacy and reduced systemic toxicity. However, more efforts in designing PEG-based prodrug conjugates are anticipated. In light of this, the current paper highlights the synthetic advances in PEG prodrug conjugation methodologies with varied bioactive components of clinical relevance. In addition, this paper discusses FDA-approved PEGylated delivery systems, their intended clinical applications, and formulations under clinical trials.
منابع مشابه
Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: design, synthesis and biological evaluation.
Poly (ethylene glycol)s (PEGs) are potential drug carriers for improving the therapeutic index of anticancer agents. In this work, a novel methodology for constructing PEG prodrug of anthracycline anticancer drugs was developed based on N-Mannich base of salicylamide and its 2-acyloxymethylated derivative. The resultant conjugates first subjected to in vitro hydrolysis testing, which revealed t...
متن کاملStudy of Surface Tension of Binary Mixtures of Poly (Ethylene Glycol) in Water and Poly (Propylene Glycol) in Ethanol and its Modeling Using Neural Network
متن کامل
Poly(Ethylene glycol)-based backbones with high peptide loading capacities.
Polymer-peptide conjugates are a promising class of compounds, where polymers can be used to overcome some of the limitations associated with peptides intended for therapeutic and/or diagnostic applications. Linear polymers such as poly(ethylene glycol) can be conjugated through terminal moieties and have therefore limited loading capacities. In this research, functionalised linear poly(ethylen...
متن کاملB-Domain deleted recombinant coagulation factor VIII modified with monomethoxy polyethylene glycol.
Recombinant coagulation factor VIII (r-VIII SQ) was chemically modified with monomethoxy poly(ethylene glycol) (mPEG). Three mPEG derivatives were used for coupling to the r-VIII SQ lysines, a mixed anhydride of monomethoxy poly(ethylene glycol) succinic acid (mPEG-SAH), monomethoxy poly(ethylene glycol) succinimidyl succinate (mPEG-SS), and monomethoxy poly(ethylene glycol) tresylate (mPEG-TRE...
متن کاملPromising potency of retinoic acid-poly(ethylene glycol)-thiol gold nanoparticle conjugates for cervical cancer treatment.
We investigated the effect of synthesized retinoic acid-poly(ethylene glycol)-thiol gold nanoparticle conjugates on cervical carcinoma cells. Cervical cancer is the major cause of deaths for the women of reproductive age in the developing countries. Compared to retinoic acid, the nanoparticle conjugates exhibited better activity against cervical carcinoma. Selective delivery of gold nanoparticl...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
دوره 2012 شماره
صفحات -
تاریخ انتشار 2012