Dendrimers are nanoscale, tree-branching polymers that have potential applications as drug delivery agents. They are synthesized in a stepwise process that builds up branches around a core molecule. Dendrimers can encapsulate or conjugate to drug molecules, releasing them in a controlled manner. They have properties like water solubility and low toxicity that make them promising for targeted drug delivery. However, further research is still needed to address challenges like toxicity at high generations and scale up for commercialization before dendrimer-based drugs can be developed.

1. PRESENTED BY
PUJA BANIK
M.PHARM, (1st YEAR), PHARMACEUTICS
ISFCP, MOGA
DENDRIMERS

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 Introduction
 Types of dendrimers
 Ideal properties of dendrimers
 Structure of dendrimer
 Synthesis of dendrimers
 Mechanisms of drug loading
 Formulations of dendrimers
 Characterization of dendrimers
 Evaluation of dendrimers
 Benefits of dendrimers
 Toxicity and safety concerns
 Applications
 Conclusions
 References

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 The name comes from Greek word “dendron” which means ‘tree’. Also
called as “arborols /cascade molecules”
 Dendrimers are three-dimensional, immensely branched, well-organized
nanoscopic molecules have displayed an essential role in the emerging
field of nanomedicine.
 Dendrimers were for the first time synthesized during 1970-1990 by two
different groups; Buhleier et al. and Tomalia et al.
 In 1978, Vogtle and co-workers was first introduced chemistry of
Dendrimers
 One of the very first dendrimers, the
Newkome dendrimer, was synthesized
in 1985

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 PAMAM dendrimers
 PPI dendrimers
 Liquid crystalline dendrimers
 Tecto dendrimers
 Chiral dendrimers
 Peptide dendrimers
 Glycodendrimers
 Ampiphilic dendrimers
 Multiple antigen dendrimers
PAMAM dendrimer PPI dendrimer
Liquid crystalline
dendrimer
Tecto dendrimer
Peptide dendrimer GlycodendrimerAmpiphilic dendrimer
Chiral
dendrimer

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Dendrimers
Monodisperse and
Biodegradable
Inert and nontoxic
Able to cross
barriers
Able to target
specific structures
Must protect the drug
until it reaches to the
desired site of action
and release the drug
Compatible with
guest molecule
Non immunogenic

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 The starting material of dendrimer is nitrogen atom. Then carbon and
other element added by chemical reaction.
 Dendrimers possess three distinguished components, namely
♦ An interior core
♦ Interior layers :- composed of repeating units, radically attached
to the interior core(generations)
♦ Exterior layers :- attached to the outermost interior generations
(terminal functionality)
3D Structure of Dendrimers

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 It is the hyperbranching when going from the centre of the dendrimer
towards the periphery, resulting in homostructural layers between the focal
points (branching points).
 Generation number is the number of focal points present in the dendrimer
counting from the core towards the dendrimer surface.
Dendrimer Dendron

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 Divergent Method :- In this method, the synthesis starts from the
core of the dendrimer to which the arms are attached by adding
building blocks in exhaustive and stepwise manner.
● Merit : Large quantity of dendrimers can be produced by this
method
● Demerit : To prevent problem during synthesis large quantity of
reagent required
 Convergent Method :- In these method , synthesis starts from the
exterior, beginning with the molecular structure that ultimately
becomes the outermost arm of the final dendrimer .
● Merit : Defects in the final structure are less. Product easily
purified
● Demerit : Due to steric hindrance higher generation dendrimer
cannot be formed

10. CONTD...
10

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 Dendrimer are particularly attractive as they offer a high drug-loading
capacity. The two methods of dendrimer drug delivery are-
 Encapsulation of drugs
 Dendrimer-drug conjugates
 Encapsulation of drugs:- Interaction between the dendrimer and drug to
trap the drug inside the dendrimer. Such system can be used to encapsulate
drugs and provide controlled delivery.
eg: DNA was complexed with PAMAM dendrimers for gene delivery
applications and hydrophobic drugs and dye molecules were incorporated
into various cores.
 Dendrimer drug conjugates:- In dendrimer-drug conjugates, the drug is
attached through a covalent bond either directly or via a linker/spacer to the
surface group of a dendrimer.
Dendrimers have been conjugated to various biologically active molecules
such as drugs, antibodies, sugar moieties and lipids.

12. S.No. Brand Name Type of dendrimer Company Application
1 VivaGel (R) Multiple antigen Star Pharma HIV prevention, Bacterial
vaginosis.
2 Alert ticket PAMAM US army research
laboratory
Anthrax detection
3 SuperFectTM Ampiphilic Qiagen Gene transfection
4 Stratus CS Tecto Dade Behring Cardiac diagnostic testing
5 PriofectTM,
PriostarTM
Tecto Star Pharma Cancer prevention
6 AstramolTM PPI DSM Cancer prevention
8 Starburst PAMAM Targeted diagnostic,
therapeutic delivery for
cancer cells
12

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Dendrimer
characterization
techniques
Spectroscopic
techniques
Chromatography
Rheology and
physical
properties
Electrical
techniques
Microscopy
Size exclusion
or gel
permeation
chromatograph
y
Differential scanning
calorimatry(DSC)
Dielectric spectroscopy
UV, IR, Mass spectroscopy;
fluorescence, X-ray diffraction
Scanning
electron
microscopy,
Transmission
electron
microscopy
Electrophoresis
Electrochemistry

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Stability studies
In vitro drug release studies
Toxicity studies
 Nano particle drug delivery systems are most popular one. However, RES
(reticuloendothelial system) uptake, drug leakage, immunogenicity,
haemolytic toxicity, cytotoxicity, restrict the use of these nanostructure.
 These are overcome by surface engineering the dendrimer such as glyco
dendrimers, Polyester dendrimers etc.
 Bioactive agents can easily encapsulated into the interior of dendrimers.

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 Improved bioavailability
 Site specific Drug delivery
 Controlled drug release
 Better patient compliance
 Increased solubility, stability, and permeability of drugs
 Improved delivery efficiency
 The capability to deliver a variety of drugs
 Ability to maintain drug levels in a therapeutically desirable range
 Increased half-life
 Increased drug retention and providing extended therapeutic effects (e.g.
Ocular drug delivery)
 Reduced side effects by targeted delivery
 Low toxicity and low immunogenicity
 High uniformity and purity

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 Cytotoxicity increase along with generation and concentration
 Cationic dendrimers are more toxic than anionic and neutral dendrimers
 PAMAM dendrimers can activate the immune response. This is
considering that the positively charged dendrimers may be employed as
vaccine carriers, due to their ability to increase cytokine production.
Regarding PAMAM immunogenicity, the dendrimer was not
immunogenic by itself, as it didn't induce production against dendrimer-
specific antibodies. However the conjugation of dendrimer with a protein
carrier induced the formation of antibodies for dendrimer surface groups
such as amine and oxyamine. Therefore, these studies have indicated the
need to conjugate PAMAM dendrimers to a protein carrier for antigenic
effect.

17. CONTD...
17

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Solubility
enhancers
Cellular
delivery
Gene delivery
Nano drugs
Diagnostics
As coating
agents
Contrast
agents
Targeted and
controlled
release drug
delivery
Delivery of
anticancer
drugs

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 Dendrimers have been considered as potential candidates for the delivery of
drugs and genes. Many drugs have been successfully delivered using
dendrimers
 Although an appreciable progress is continuously being made in the area of
dendrimer-assisted drug or gene delivery, there are many issues yet to be
resolved
 Developing cost effective synthetic strategies and scale up technologies for
dendrimers is another challenge for scientists to aid successful
commercialization of dendrimer-based drug/gene delivery system

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 Kesharwani P, Jain K, Jain NK. Dendrimer as nanocarrier for drug
delivery. Progress in Polymer Science. 2014 Feb 1;39(2):268-307.
 Fréchet JM. Dendrimers and supramolecular chemistry. Proceedings of the
National Academy of Sciences. 2002 Apr 16;99(8):4782-7.
 Abbasi E, Aval SF, Akbarzadeh A, Milani M, Nasrabadi HT, Joo SW,
Hanifehpour Y, Nejati-Koshki K, Pashaei-Asl R. Dendrimers: synthesis,
applications, and properties. Nanoscale research letters. 2014 Dec
1;9(1):247.
 Gupta V, Nayak SK. Dendrimers: a review on synthetic approaches.
Journal of Applied Pharmaceutical Science. 2015 Mar;5(03):117-22.

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