The efficiency of a PAMAM dendrimer toward the encapsulation of the antileukemic drug 6-mercaptopurine

Neerman, Michael F.

doi:10.1097/cad.0b013e32809ef9d0

Cited by 22 publications

(16 citation statements)

References 14 publications

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“…In this study, we have demonstrated that similar to the complexation of other hydrophobic drugs using dendrimers,22–24 2-ME can also be complexed within dendrimers having different terminal groups (Scheme 1). The formation of 2-ME/dendrimer complexes is primarily based on hydrophobic interactions between dendrimers and 2-ME drug molecules.…”

Section: Resultsmentioning

confidence: 77%

Influence of dendrimer surface charge on the bioactivity of 2-methoxyestradiol complexed with dendrimers

Shi

Lee²,

Chen

et al. 2010

Soft Matter

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We report the complexation of a potential anticancer agent 2-methoxyestradiol (2-ME) with generation 5 (G5) poly(amidoamine) dendrimers having different surface functional groups for therapeutic applications. The complexation experiment shows that approximately 6–8 drug molecules can be complexed with one dendrimer molecule regardless the type of the dendrimer terminal groups. The bioactivity of 2-ME complexed with dendrimers was found to be significantly dependent on the surface charge of G5 dendrimers. In vitro cell biological assays show that amine, hydroxyl, and acetamide-terminated G5 dendrimers with positive, slightly positive, and close to neutral surface charges, respectively are able to deliver 2-ME to inhibit cancer cell growth. In contrast, 2-ME complexed with carboxyl-terminated G5 dendrimers with negative surface charges does not show its inherent bioactivity. Further molecular dynamics simulation studies show that the compact structure of carboxylated G5 dendrimers complexed with 2-ME does not allow the release of the drug molecules even at a pH of 5.0, which is the typical pH value in lysosome. Our findings indicate that the surface modification of dendrimers with different charges is crucial for the development of formulations of various anticancer drugs for therapeutic applications.

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Section: Resultsmentioning

confidence: 77%

Influence of dendrimer surface charge on the bioactivity of 2-methoxyestradiol complexed with dendrimers

Shi

Lee²,

Chen

et al. 2010

Soft Matter

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“…3 4 Several reports indicated that anticancer drugs (camptothecin, 6-mercaptopurin, methotrexate, adriamycin, 5-fluorouracil, and paclitaxel) were encapsulated into the PAMAM dendrimer exhibiting a significant enhancement of its water solubility, storage stability, and anti-tumor activity. [5][6][7][8][9][10] However, there are a few disadvantages accompanied with PAMAM dendrimer drug-delivery system including hemolytic toxicity and cell lysis due to a strong interaction of the positively charged dendrimer and the negatively charged cell membrane resulting in membrane disruption. 9 11-13 Like other cationic polymers such as polylysine and poly(ethyleneimine), these disadvantages have been solved by conjugating biocompatible and hydrophilic polymers into amine group-terminated dendrimer.…”

Section: Introductionmentioning

confidence: 99%

Pegylated Dendrimer and Its Effect in Fluorouracil Loading and Release for Enhancing Antitumor Activity

Ly¹,

Trân²,

Hoang³

et al. 2013

j biomed nanotechnol

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Dendrimer, a new class of hyper-branched polymer with predetermined molecular weight, is being received much attention in nano biomedical applications such as anticancer drug delivery, gene therapy, disease diagnosis and etc. In this study, polyamidoamine (PAMAM)-based dendrimer generation 3.0 (G 3.0) was synthesized and subsequently pegylated. Obtained results showed that pegylation degree of the dendrimer was around 31% for its external amine groups. TEM image of the pegylated dendrimer exhibited spherical shape and nano sizes ranging from 30 to 40 nm. The fluorouracil (5-FU)-loaded pegylated dendrimer showed a slow release profile of the drug. In vitro study, at the primary screening concentration of 100 microg/mL, the PAMAM dendrimer presented higher toxicity in MCF-7 cells as compared to its pegylated counterpart. Meanwhile, the (5-FU)-loaded pegylated dendrimer exhibited the antiproliferative activity against the cell line with the IC50 of 9.92 +/- 0.19 microg/mL. In vivo tumor xenograft study, we succeeded in generating MCF-7 cells-derived cancer tumors on mice that was well-confirmed by using flow cytometer assay. The 5-FU encapsulated pegylated dendrimer exhibited a significant decrement in volume of the tumors which was generated by MCF-7 cancer cells.

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“…mercaptopurin, methotrexate, 5-FU, and paclitaxel) were encapsulated into the PAMAM dendrimer exhibiting a significant enhancement of its water solubility, storage stability, reduction of side-effects, and anti-tumor activity [17][18][19][20][21]. However, there are a few disadvantages accompanied with the amine-terminated dendrimer-based carriers including hemolytic toxicity and cell lysis due to a strong interaction of its positively charge and a negative charge on cell membrane resulting in disruption of the cellular membrane [22][23][24][25][26].…”

Section: Introductionmentioning

confidence: 99%

Highly lipophilic pluronics-conjugated polyamidoamine dendrimer nanocarriers as potential delivery system for hydrophobic drugs

Nguyen

Nguyen³

et al. 2017

Materials Science and Engineering: C

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The efficiency of a PAMAM dendrimer toward the encapsulation of the antileukemic drug 6-mercaptopurine

Cited by 22 publications

References 14 publications

Influence of dendrimer surface charge on the bioactivity of 2-methoxyestradiol complexed with dendrimers

Influence of dendrimer surface charge on the bioactivity of 2-methoxyestradiol complexed with dendrimers

Pegylated Dendrimer and Its Effect in Fluorouracil Loading and Release for Enhancing Antitumor Activity

Highly lipophilic pluronics-conjugated polyamidoamine dendrimer nanocarriers as potential delivery system for hydrophobic drugs

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