2016
DOI: 10.1080/21691401.2016.1236805
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Comparison study of the effect of alkyl-modified and unmodified PAMAM and PPI dendrimers on solubility and antitumor activity of crocetin

Abstract: Poor water solubility of hydrophobic drugs is one of the major problems in pharmaceutical sciences. Herein, in order to address the poor solubility of crocetin, the 30% of primary amines of PAMAM G4 and PPI G4 were alkylated and evaluated as drug delivery vectors. According to the results, this modification could improve the drug delivery efficiency in term of drug solubility, release pattern and cytotoxicity; however, the encapsulation yield was decreased. Accordingly, it can be concluded that the designed al… Show more

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Cited by 20 publications
(10 citation statements)
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“…Then, the efficiency of the synthetized vectors for the delivery of TRAIL plasmid was evaluated in mouse colon cancer cell line, in vitro and in vivo. Mouse TRAIL R2, also called DR5, TRICK 2, TNFRSF10B, and MKDR5 shares 43 and 49% sequence homology with human TRAIL-R1 and TRAIL-R2, respectively [24]. The ability of dendrimers to condense DNA is an essential requirement for successful gene delivery.…”
Section: Discussionmentioning
confidence: 99%
See 1 more Smart Citation
“…Then, the efficiency of the synthetized vectors for the delivery of TRAIL plasmid was evaluated in mouse colon cancer cell line, in vitro and in vivo. Mouse TRAIL R2, also called DR5, TRICK 2, TNFRSF10B, and MKDR5 shares 43 and 49% sequence homology with human TRAIL-R1 and TRAIL-R2, respectively [24]. The ability of dendrimers to condense DNA is an essential requirement for successful gene delivery.…”
Section: Discussionmentioning
confidence: 99%
“…The effect of synthetized vector containing TRAIL plasmid on induction of apoptosis was evaluated as described previously [24,25]. Briefly, C26 cells were seeded in 24-well plates at a density of 4 Â 10 4 cells/well and incubated for 24 h. Polyplexes with C/P ratio 2 and 4 were prepared and added into each well (equivalent of 800 ng TRAIL plasmid/well).…”
Section: Sub-g1 Apoptosis Assay Using Flow Cytometrymentioning
confidence: 99%
“… Dormancy state: CSCs enter dormancy to evade the attack by the immune system, awaiting new signals from the environment to re-enter the cell cycle [ 22 ]. Changes in morphology or biological function, such as the over-expression of anti-apoptotic proteins that block the cell from entering the type I apoptosis cycle [ 1 , 22 , 24 ]. Elevated expression of ATP-binding cassette (ABC) pumps and detoxifying enzymes to increase the drug’s efflux, which is considered to be an important mechanism for multi-drug resistance (MDR).…”
Section: Cancer Stem Cell Biologymentioning
confidence: 99%
“…Changes in morphology or biological function, such as the over-expression of anti-apoptotic proteins that block the cell from entering the type I apoptosis cycle [ 1 , 22 , 24 ].…”
Section: Cancer Stem Cell Biologymentioning
confidence: 99%
“…This is in part due to their high aqueous solubility and biocompatibility, low immunogenicity, and the presence of modifiable peripheral functional groups [23, 24]. The high density of terminal groups and internal cavities in the PAMAM and PPI dendrimers promotes drug association, resulting in the improvement of aqueous solubility of lipophilic therapeutic compounds [25] such as candersatan cilexetil [26], hydrochlorothiazide [27], crocetin [28] and doxorubicin [29]. Also, several ionic drugs such as mycophenolic acid [30], daidzein [31] phenobarbital and zulfamethoxazole [32] have been associate to dendrimeric carriers.…”
Section: Introductionmentioning
confidence: 99%