Polyamidoamine (PAMAM) dendrimers as biocompatible carriers of quinolone antimicrobials: An in vitro study

Bioconjugates of PAMAM dendrimers with trans-retinal, pyridoxal, and pyridoxal phosphate

“…Vitamin B 6 and vitamin A readily form conjugates with third-generation PAMAM dendrimers as Schiff bases. Condensation of 13-cis and 13-trans -retinal with G3 resulted in formation of conjugates with variable degrees of PAMAM substitution.…”

“…In terms of potential dermatological application, bioconjugates of folate, 11 biotin, 12 riboflavin, 13 cholic acid, 14 and phosphorylcholine 15 have been synthesized and tested as membrane permeability enhancers, increasing the cellular uptake of the drug. Here we report on bioconjugates obtained from third-generation PAMAM dendrimers, retinal ([Ret] vitamin A), pyridoxal ([Pyr] vitamin B 6 ), or pyridoxal phosphate ([PLP] metabolically active coenzyme of vitamin B 6 ). The G3 dendrimer was chosen in accordance with our previously reported results for optimization of dendrimer size as a transdermal carrier for vitamins B 2 and C. The important issue concerning application of bioconjugates carrying biologically active molecules is their bioavailability, which was tested here in vitro.…”

“…1 These monodispersed dendritic molecules have a strictly defined shape and size and are able to encapsulate drug molecules, resulting in formation of host-guest complexes. [2][3][4][5][6][7][8][9][10] On the other hand, full-generation PAMAM dendrimers have surface amine groups (32 amine groups in the third-generation PAMAM dendrimer, G3), offering an easy route for formation of conjugates with drugs. [11][12][13][14][15][16][17][18][19][20][21] Due to the relatively low toxicity of PAMAM dendrimers, [22][23][24][25] they are frequently used as transdermal diffusion promoters.…”

Dendrimers as tunable vectors of drug delivery systems and biomedical and ocular applications

“…It was shown that the presence of PAMAM-based dendrimers increases the water solubility and the antimicrobial activities of nadifloxacin and prolifloxacin. 43 There are many more paradigms employing dendrimers as antimicrobial agents and therapeutics. The creation of the SPL7013 Gel (VivaGel; Starpharma, Preston, Melbourne, Victoria, Australia) Platform is one such example.…”

“…The fourth-generation SPL7013 dendrimer afforded broad anti-HIV activity, provided at least 12-hour protection against HSV-2 in mouse retina and was not toxic. 43 Efficacious topical microbicides, such as SPL7013 and VivaGel, are essential for the prevention of the transmission of HIV and HSV-2 and other genital infections in women. The data presented in the study by Tyssen et al, 47 in addition to those of previous studies presented earlier in this review, support the need for further evaluation of VivaGel in clinical trials for the assessment of its therapeutic potential as an efficacious topical microbicide in women with genital infections, when administered intravaginally, either alone or in conjunction with other antiviral agents.…”