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Surface-engineered Dendrimers For Dual Drug Delivery: A Receptor Up-regulation And Enhanced Cancer Targeting Strategy

Rakesh K Tekade, T. Dutta, A. Tyagi, A. Bharti, B. Das, N. K. Jain
Published 2008 · Chemistry

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The present study is aimed at developing and evaluating a combined strategy of dual drug delivery, receptor up-regulation, and drug targeting. The dendritic architectures were synthesized and characterized by IR, 1H-NMR, and 13C-NMR spectroscopy. The pH-responsive simultaneous release behavior of the loaded bioactive from the carrier was also explored. The cell line studies for MTT cytotoxicity, receptor blockade, and receptor up-regulation assays were performed on HeLa cells. Treatment of cells with low concentration of all-trans retinoic acid (ATRA, ∼1 μM) caused a selective up-regulation of folate receptors by 2.21-folds when compared with that of untreated control, after 48 h. ATRA showed a lag phase of 12 h in up-regulating the folate receptors. After 48 h, the IC50 value of naked methotrexate (MTX)–ATRA combination and dendrimer-loaded MTX–ATRA combination were found to be ∼0.1 and 10 μM, respectively, while folate-anchored dendrimer loaded with MTX–ATRA showed a selectively lowered IC50 value of 0.04 μM. It was concluded that in allied ailments like cancer, the proposed dual-drug delivery modality bearing anti-cancer bioactive in conjunction with folate receptor up-regulating cargo may prove to be a promising approach toward the development of a flourishing cancer therapy.
This paper references
Peptidemediated release of folate-targeted liposome contents from endosomal compartments
K Vogel (1996)
Investigations on biodistribution of technetium-99m-labeled carbohydrate-coated poly(propylene imine) dendrimers.
H. Agashe (2007)
Dendritic polymer
AK 100594–602. Patri (2002)
Polypropylene imine dendrimer mediated solubility enhancement: effect of pH and functional groups of hydrophobes.
U. Gupta (2007)
Polymeric drugs based on conjugates of synthetic and natural macromolecules. II. Anti-cancer activity of antibody or (Fab')(2)-targeted conjugates and combined therapy with immunomodulators.
B. Říhová (2000)
Apoptosis induced by retinoic acid in Hep 3B cells in vitro.
D. Kim (1996)
Molecular heterogeneity analysis of poly(amidoamine) dendrimer-based mono- and multifunctional nanodevices by capillary electrophoresis.
X. Shi (2006)
Development of a tumor-targeting MR contrast agent using the high-affinity folate receptor: work in progress.
S. Konda (2000)
Targeting and inhibition of cell growth by an engineered dendritic nanodevice.
T. Thomas (2005)
Induction of apoptosis in A549 human lung cancer cells by all-trans retinoic acid incorporated in DOTAP/cholesterol liposomes.
S. Kawakami (2006)
Designing dendrimers for drug
MJ 876–883.Liu (1999)
Differentiation-independent retinoid induction of folate receptor type beta, a potential tumor target in myeloid leukemia.
H. Wang (2000)
Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers
Palanirajan Vijayaraj Kumar (2006)
Starburst Dendrimers: Molecular‐Level Control of Size, Shape, Surface Chemistry, Topology, and Flexibility from Atoms to Macroscopic Matter
D. Tomalia (1990)
Design and Function of a Dendrimer-Based Therapeutic Nanodevice Targeted to Tumor Cells Through the Folate Receptor
A. Quintana (2004)
Polypropylene imine
U Gupta (2007)
Targeting of efavirenz loaded tuftsin conjugated poly(propyleneimine) dendrimers to HIV infected macrophages in vitro.
T. Dutta (2008)
Poly(propylene imine) Dendrimers: Large‐Scale Synthesis by Hetereogeneously Catalyzed Hydrogenations
Ellen Marleen Monique De Brabander-Van Den Berg (1993)
Biodistribution of a 153Gd-Folate Dendrimer, Generation = 4, in Mice With Folate-Receptor Positive and Negative Ovarian Tumor Xenografts
S. Konda (2002)
Delivery of liposomes into cultured KB cells via folate receptor-mediated endocytosis.
R. Lee (1994)
Modulation of the retinoic acid-induced cell apoptosis and differentiation by the human TR4 orphan nuclear receptor.
Y. Lee (2004)
Polymeric drugs based on conjugates of synthetic and natural macromolecules. I. Synthesis and physico-chemical characterisation.
K. Ulbrich (2000)
Dendrimers: novel polymeric nanoarchitectures for solubility enhancement.
U. Gupta (2006)
Targeted drug delivery with dendrimers: comparison of the release kinetics of covalently conjugated drug and non-covalent drug inclusion complex.
A. Patri (2005)
Modulation of the retinoic acid
YF Lee (2004)
Overexpression of Retinoic Acid Receptor β Induces Growth Arrest and Apoptosis in Oral Cancer Cell Lines
K. Hayashi (2001)
Identification of OTX2 as a medulloblastoma oncogene whose product can be targeted by all-trans retinoic acid.
C. Di (2005)
PEGylated peptide-based dendritic nanoparticulate systems for delivery of artemether
D. Bhadra (2005)
Toxicological investigation of surface engineered fifth generation poly (propyleneimine) dendrimers in vivo
T. Dutta (2008)
Preparation, cellular transport, and activity of polyamidoamine-based dendritic nanodevices with a high drug payload.
P. Kolhe (2006)
Nanoparticle targeting of anticancer drug improves therapeutic response in animal model of human epithelial cancer.
J. Kukowska-Latallo (2005)
The development of a tumor targeting magnetic resonance contrast agent using the high affinity folate receptor: Work in progress
SD Konda (2000)
Designing dendrimers for drug delivery.
Liu (1999)
Targeted drug
AK 6466–471. Patri (2005)
Specific targeting of folate–dendrimer MRI contrast agents to the high affinity folate receptor expressed in ovarian tumor xenografts
S. Konda (2007)
Peptide-Mediated Release of Folate-Targeted Liposome Contents from Endosomal Compartments1
K. Vogel (1996)
Starburstr̀ dendrimers — Nanoscopic supermolecules according to dendritic rules and principles
D. Tomalia (1996)
A PEGylated dendritic nanoparticulate carrier of fluorouracil.
D. Bhadra (2003)
Inhibition of tumor growth by biodegradable microspheres containing all‐trans‐retinoic acid in a human head‐and‐neck cancer xenograft
Yongdoo Choi (2003)
Polymer-protein and polymer-drug conjugates in cancer therapy.
M. Thanou (2003)
Poly(propyleneimine) dendrimer and dendrosome mediated genetic immunization against hepatitis B.
T. Dutta (2008)
Poly (propyleneimine) dendrimer based nanocontainers for targeting of efavirenz to human monocytes/macrophages in vitro
T. Dutta (2007)
Strategy for the treatment of acute myelogenous leukemia based on folate receptor beta-targeted liposomal doxorubicin combined with receptor induction using all-trans retinoic acid.
X. Q. Pan (2002)
Exploring dendrimer towards dual drug delivery: pH responsive simultaneous drug-release kinetics
Rakesh K Tekade (2009)
Dendrosome-based gene delivery
T. Dutta (2006)
Simultaneous spectrophotometric estimation of methotrexate and all-trans retinoic acid in mixture
RK Tekade (2008)
Drug Delivery Systems in Cancer Therapy
K. H. K. Kwok (2004)
Dynamics of cellular entry and drug delivery by dendritic polymers into human lung epithelial carcinoma cells
S. Kannan (2004)
Folate-mediated tumor cell targeting of liposome-entrapped doxorubicin in vitro.
R. Lee (1995)
Poly(amidoamine) (PAMAM) dendritic nanostructures for controlled sitespecific delivery of acidic anti-inflammatory active ingredient
Abhay Asthana (2008)
Dendrimers as potential drug carriers; encapsulation of acidic hydrophobes within water soluble PAMAM derivatives
A. Beezer (2003)
Targeting potential and anti-HIV activity of lamivudine loaded mannosylated poly (propyleneimine) dendrimer.
T. Dutta (2007)
Dendritic polymer macromolecular carriers for drug delivery.
A. Patri (2002)
Investigation on biodistribution of technetium-99m labeled carbohydrate coated PPIdendrimers
HB Agashe (2007)
Book Review: The Organic Chemistry of Polycoordinated Iodine. By. A. Varvolis
P. Stang (1993)

This paper is referenced by
Tumor Microenvironment Targeted Nanotherapeutics for Cancer Therapy and Diagnosis: A review.
S. Thakkar (2019)
Dendrimer-based nanodevices for targeted drug delivery applications.
J. Zhu (2013)
Advanced nanoscale carrier-based approaches to overcome biopharmaceutical issues associated with anticancer drug 'Etoposide'.
H. Choudhury (2020)
Advances in combination therapies based on nanoparticles for efficacious cancer treatment: an analytical report.
S. Mignani (2015)
Dendrimer as nanocarrier for drug delivery
P. Kesharwani (2014)
Bioinspired pyrimidine-containing cationic polymers as effective nanocarriers for DNA and protein delivery.
Y. Xiao (2020)
Elegant pH-Responsive Nanovehicle for Drug Delivery Based on Triazine Dendrimer Modified Magnetic Nanoparticles.
Amir Landarani-Isfahani (2017)
Recent advances in exosome-based nanovehicles as RNA interference therapeutic carriers.
Rahul Maheshwari (2017)
RNAi-combined nano-chemotherapeutics to tackle resistant tumors.
Rakesh K Tekade (2016)
Nanomaterial-Based Gene and Drug Delivery: Pulmonary Toxicity Considerations
Mahavir Bhupal Chougule (2014)
Carbon Nanotubes in Targeting and Delivery of Drugs
Rakesh K Tekade (2017)
Exploiting Nanocarriers for Combination Cancer Therapy
Y. W. Kong (2016)
Evaluation of dendrimer safety and efficacy through cell line studies.
P. Kesharwani (2011)
Dendrimers as macromolecular tools to tackle from colon to brain tumor types: a concise overview
S. Mignani (2013)
Dendrimers in combination with natural products and analogues as anti-cancer agents.
S. Mignani (2018)
Synthesis, Characterization and in vivo Evaluation of PEGylated PPI Dendrimer for Safe and Prolonged Delivery of Insulin
Ashish Kumar Parashar (2019)
Dendrimer space concept for innovative nanomedicine: A futuristic vision for medicinal chemistry
S. Mignani (2013)
Impact of pegylation on biopharmaceutical properties of dendrimers
S. Thakur (2015)
Extraction and RP-HPLC determination of taxol
Rakesh K Tekade (2013)
Multifunctional nanoparticle developments in cancer diagnosis and treatment
S. Parvanian (2017)
Nanovehicles for co-delivery of anticancer agents.
M. Zeinali (2020)
Biopolymer-based nanocomposites for transdermal drug delivery
Rakesh K Tekade (2017)
Fabrication of polydopamine-based layer-by-layer nanocomposites for combined pH-sensitive chemotherapy and photothermal therapy
Hongchao Ma (2019)
Solid Lipid Nanoparticles for Targeting and Delivery of Drugs and Genes
Rakesh K Tekade (2017)
Toxicity of nanostructured biomaterials
Rakesh K Tekade (2018)
Smart dendrimers: Synergizing the targeting of anticancer bioactives
Vikrant Saluja (2019)
Materials innovation for co-delivery of diverse therapeutic cargos.
Megan E Godsey (2013)
Nanotechnology for the Development of Nanomedicine
Rakesh K Tekade (2017)
A Review- Emerging Use of Nano-Based Carriers in Diagnosis and Treatment of Cancer-Novel Approaches
Yaqub Khan (2015)
All-trans retinoic acid preconditioning protects against liver ischemia/reperfusion injury by inhibiting the nuclear factor kappa B signaling pathway.
J. Rao (2013)
The use of nanoscaffolds and dendrimers in tissue engineering.
Bapi Gorain (2017)
Recent Advances Of Biomimetic Nano-systems in the Diagnosis and Treatment of Tumor
Anning Li (2019)
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