Biological properties of adriamycin bound to biodegradable polymeric carriers

Synthesis and biological evaluation of immunoconjugates of adriamycin and a human IgM linked by poly[N5-2-hydroxyethyl)-l-glutamine]

“…The following compounds were prepared as described, y-Benzyl-L-glutamate (BLG 11) [13]; ybenzyl-L-glutamate N-carboxyanhydride (BLG NCA 12) [ 10]; poly(y-benzyl-L-glutamate) containing cystamide groups (S2-PBLG 13a,b), a mixture of bis [ poly (y-benzyl-L-glutamate) ] cystamide (bis-PBLG-cystamide 13a) and poly(y-benzyl-L-glutamate) (PBLG 13b) [ 10]; poly(a-L-glutamic acid) containing cystamide groups (S2-PGA 14a,b), a mixture of bis [ poly (a-L-glutamic acid) ] cystamide (bis-PGA-cystamide 14a) and poly(c~-L-glutamic acid) (PGA 14b) [10]; high-molecular weight PGA 14b [ 14]; cystamine free base from the dihydrochloride [15].…”

“…A conjugate of PHEG and 1,4-diaminobutane designated as PHEG-butyl-NH218 was obtained from high-molecular weight (Mw 73 000) PGA without thiol end groups 14b [ 14,27] and 8 using the method described above. The degree of spacer substitution was 10 mol% as determined by ~H-NMR.…”

“…This procedure was repeated once, and spectra were recorded of solutions of the polymers in D20 (99.96% D). Thin-layer chromatography (TLC) was performed on silica coated onto plastic sheets GF254 ( Merck, Germany) using the following solvent systems: A, toluene/ethanol (8/2; v/v); B, ethyl acetate/hexane ( 1 / 1 ; v/v) ; C, n-butanol/acetic acid/water (4/1 / 1 ; v/v) [ 10,14]. Polyacrylamide gel electrophoresis (PAGE) in the presence of sodium dodecylsulphonate (SDS) was performed as described [10].…”

Renal targeting potential of a polymeric drug carrier, poly-L-glutamic acid, in normal and diabetic rats

“…[15][16][17][18] PG has been utilized as a tumor-targeting drug carrier for various hydrophobic cancer chemotherapeutic agents. [19][20][21][22][23][24][25][26] A significant renal accumulation of PG was observed in several studies on the biodistribution of a PG-paclitaxel conjugate in mice. [27][28][29] Studies on other PG-chemotherapeutic conjugates have shown similar findings.…”

Characteristics of Tissue Distribution of Various Polysaccharides as Drug Carriers: Influences of Molecular Weight and Anionic Charge on Tumor Targeting

“…6) Recently, the N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer-DXR conjugate, called PK1, has entered clinical development in the UK 7,8) and its Phase 1 results 9) showed that by conjugating the drug with a macromolecule, its distribution properties could be altered depending on the properties of the carrier macromolecules. 10,11) Various macromolecules, such as immunoglobulins, 12) albumin, 13) polyaminoacids, [14][15][16][17][18][19] synthetic polymers, 20,21) and polysaccharides, [22][23][24][25] have traditionally been used as drug carriers; however, this approach does not always produce the desired results in vivo since the distribution characteristics of these drug carriers has so far not been characterized and, therefore, is not well known. In particular, there is not enough information about the distribution properties and physicochemical characteristics of polysaccharides to select suitable drug carriers for tumor targeting.…”