Dendrimers in anticancer drug delivery: mechanism of interaction of drug and dendrimers

Figures & data

Figure 1. Typical architecture of dendrimers.

Figure 2. Terms and nomenclature in dendrimer chemistry.

Figure 3. Schematic representation of divergent method of synthesis of dendrimers.

Figure 4. Schematic representation of convergent method of synthesis of dendrimers.

Figure 5. Schematic presentation of different types of dendrimers.

Table 1. Mechanisms of interactions of various anticancer drugs with dendrimers.

Drugs	MOA	Uses	Drug dendrimer interaction	Applications	References
5-Fluorouracil	5-Fluorouracil is inhibits the formation of thymidylate from uracil	Breast cancer	Chemical conjugation	Enhancement of solubility of 5-Fluorouracil	Longley et al. (2003)
		Colorectal cancer
		Pancreatic cancer
Cisplatin	Attachment of alkyl groups to DNA bases, DNA damage via the formation of cross-links	Bladder cancer	Covalent conjugation	Improved loading efficiency, reduced cytotoxicity but significant anti-proliferative activity against lung cancer cell	Nguyen et al. (2015)
		Cervical cancer
		Ovarian cancer
Doxorubicin Hydrochloride	Doxorubicin HCl inhibits topoisomerase II activity	Breast cancer	Physical encapsulation	Enhancement of solubility of Doxorubicin HCl	Lai et al. (2007)
		Gastric cancer
		Ovarian cancer
		Thyroid cancer
		Wilms tumor
Methotrexate	Inhibiting the metabolism of folic acid and enzymes in the synthesis of purines and pyrimidines required for cell proliferation	Breast cancer	Physical encapsulation	Improve bioavailability and toxicity.	Kozub and Simaljakova (2011)
		Head and neck cancer
		Lung cancer
Paclitaxel	Promotes tubilin assembly, stabilize microtubules	Breast cancer	Physical encapsulation	Enhanced water solubility compared to the pure drug	Ooya et al. (2003)
		Lung cancer
		Ovarian cancer
Cisplatin	Attachment of alkyl groups to DNA bases, DNA damage via the formation of cross-links	Bladder cancer	Physical encapsulation	Reduced toxicity	Fuertes et al. (2003)
		Cervical cancer Ovarian cancer

Figure 6. Drug encapsulation in dendrimers by physical encapsulation.

Figure 7. Drug encapsulation in dendrimers by chemical conjugation.

Table 2. Dendrimer-based-marketed formulations (Menjoge et al. 2010, Mishra 2011).

Marketed product	Dendrimers	Drug/active agents	Company	Application	Clinical trials
VIVAGEL	G4 lysine-based dendrimer	SPL7013 or astodrimer  sodium	Starpharma	Topical vaginal microbicide	Phase 3
Superfect	PAMAM-G6	DNA	Qiagen	Gene delivery and transfection agents	Phase 4
PrioFect	PAMAM	DNA	Starpharma	Gene delivery and transfection agents	Phase 3

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