Novel Cationic Copolymers of a Polyasparthylhydrazide: Synthesis and Characterization

Figures & data

TABLE 1 [Values of Y (moles of EDCI/moles of CPTACl)], molecular weight, polydispersity index, and derivatization degree of PAHy-CPTA copolymers and starting batch of PAHy

	Y	Molecular weight	Polydispersity index	Degree of derivatization%	Yield (PAHy)%
PAHy45-CPTA	0.5	11131	1.20	33	90
pH 4.75
	1.0	9931	1.27	48	92
	1.5	9957	1.28	58	96
PAHy45		14460	1.5

For all the reactions considered, X value equals 1.

TABLE 2 Hydrated diameters of polyplexes PAHy-CPTA/DNA calf thymus at different weight ratios after dilution in HEPES solution 25 mM, pH 7.0, after 0.5 and 48 hr

	Size (nm)
PAHy-CPTA/DNAweight ratio	After.5 hr	Polydispersity	After 48 hr	Polydispersity
PAHy-CPTA58%
10/1	154	0.25	153	0.19
5/1	178	0.13	181	0.15
1/1	143	0.27	134	0.23
PAHy-CPTA42%
10/1	186	0.23	186	0.23
5/1	207	0.12	205	0.11
1/1	152	0.42	156	0.20
PAHy-CPTA28%
10/1	165	0.21	165	0.20
5/1	197	0.34	200	0.10
1/1	143	0.58	130	0.15

FIG. 1 Typical ¹HNMR spectrum of a PAHy-CPTA copolymer.

DIAGRAMS The synthesis of PAHy-CPTA copolymers.

FIG. 2 Gel retardation assay PAHy-CPTA (58%), PAHy-CPTA (48%), PAHy-CPTA (28%)/DNA λ Hind III at different ratios w/w 0.8/1, 1/1, 5/1.

FIG. 3 Gel retardation assay of PAHy-CPTA (48%), PAHy-CPTA (33%) at polymer/DNA λ Hind III weight ratios 1/1, 2/1, 3/1, 5/1.

FIG. 4 Gel retardation assay confronting retardation capacity of PAHy-CPTA (48%) and DEAE-Dex ratios w/w 1/1, 2/1, 3/1, 5/1.

TABLE 3 Hydrated diameters and zeta potential of polyplexes PAHy-CPTA/DNA calf thymus at different weight ratios in water

Copolymer/DNA weight ratio	Size (nm)	Polydispersity	potential
Zeta PAHy CPTA 58%
10/1	186	0.19	23.2 ± 1.8
5/1	176	0.25	13.5 ± 1.4
1/1	131	0.17	−26.2 ± 4.1
PAHy CPTA 48%
10/1	193	0.19	24.1 ± 0.3
5/1	109	0.17	16.1 ± 1.1
1/1	206	0.26	−28.1 ± 2.9
PAHy CPTA 33%
10/1	191	0.08	18.8 ± 1.2
5/1	205	0.09	5.3 ± 1.3
1/1	196	0.44	−30.8 ± 0.8

TABLE 4 Hydrated diameters of polyplexes PAHy-CPTA/DNA calf thymus at different weight ratios in 0.9% NaCl p/v solution

PAHy-CPTA/DNA weight ratio	Size (nm)	Polydispersity
PAHy-CPTA58%
10/1	1007	0.19
5/1	1193	0.34
1/1	330	0.50
PAHy-CPTA48%
10/1	1061	0.21
5/1	1134	0.13
1/1	403	0.42
PAHy-CPTA33%
10/1	379	0.42
5/1	378	0.34
1/1	410	0.58

FIG. 5 Percent of degradation of calf thymus DNA and complexes PAHyCPTA/DNA at weight ratio 5/1.

FIG. 6 DNA degradation profile at different PAHy-CPTA 48%/DNA weight ratios.