Macromolecular prodrugs

Benzotriazole as a Synthetic Auxiliary

“…Binding of drugs from various therapeutic groups to polymers of polyaspartamide type by benzotriazolide method was performed and described in several papers. The following drugs were used: NSAIDs (ketoprofen, Ket, indomethacin, Ind, fenoprofen, Fen, diclofenac, Dic, ibuprofen, Ibu), 35,37,[46][47][48] antihyperlipemic (gemfibrozil, Gem), 48,57,58 estrogens (estradiol benzoate, EB, estradiol valerate, EV), 59,60 uricosuric (probenecid, Pro) 36 and antimalarian drug primaquine, PQ. 56 Structures of the drugs used in preparation of polymer-drug conjugates are presented in Figure 1.…”

“…35,37,[46][47][48]56,[57][58][59][60] With amino acids (glycine and β-alanine) or ethylenediamine derivatives 67 and 70 with additional functional group useful for further derivatization or binding to polymers were obtained and used in preparation of the conjugates with a spacer between polymer and drug. 46,58 More than twenty polymer-drug conjugates were prepared, which differed in the polymer type, average molecular mass, bound drug, type of polymer-drug bond (ester, amide or carbamate), type of spacer and drugloading.…”

Synthesis and in vitro Modeling and Characterization of Self-AssemblingDrug Conjugates for Targeted Medicinal Application

“…Typically aggregates must accommodate moieties from conjugation of a number of organic entities [9,15,27,[37][38][39] with ease. A complex conjugate of particular activity has been described based on attachment to an immuno-responsive agent [9].…”

“…Conjugates have also been used directly in constructing pharmacologic models for use in mimicking cellular compartmentalization and this has been studied both for dendrimer [16,[23][24][25][26] and colloidal [4,6,25,[27][28][29][30][31][32][33] systems. Dendrimers are used widely in this field as they are polymers with a branch-like configuration [24], in the simplest scenario, but may also be constructed to form an array of architectures, many of which approximate to globules, spheroids or ellipsoidal cages and super-dense spheroids [11,16].…”

Orthogonally functionalizable copolymers based on a novel reactive carbonate monomer

“…The stability of the drug–polymer linkage is crucial in polymer–drug conjugates 50. Based on the stability and cleavage conditions, the carbamate linkage has attracted considerable attention in the area of polymer therapeutics 51–55. Linkers connecting the drug molecule to the polymeric macromolecule require being stable in the plasma while possessing the inherent biodegradability property to release the payload.…”