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POLYSACCHARIDES AS
BUILDING BLOCKS FOR
NANOTHERAPEUTICS
Tony Francis
Department of Chemistry
St. Mary’s college
Manarkadu
Introduction
 Over the past two decades nanoparticles (NPs)-
based therapeutics have been introduced for the
treatment of cancer, diabetes, allergy, infections
and inflammation.
 Of the available NP systems polysaccharides are
the most outstanding one because of there virtues
such as biocompatibility, biodegradability, low
toxicity, low cost and there ease of chemical
modification
Classification Carbohydrates
 Monosaccharides- A Carbohydrate that cannot be
hydrolysed further to give simple units of
polyhydroxy aldehyde or ketone.
 Oligosaccharides- Carbohydrate that can yield
two to ten monosaccharide unit on hydrolysis.
 Polysaccharides- Polymers of monosaccharides
joined together by glycosidic linkage.
Polysaccharides classification
based on there origin
 Plant origin – Cellulose, Pectin and guar gum
 Animal origin – Chitosan, Heparin and Hyaluronan
 Algal origin – Alginate and Carrageenan
 Microbial origin- Dextran and Xanthan gum
 Marine origin- Agar and Agarose
Classification based on the
monomer groups
 Homopolysaccharides or Homoglycans- They
are polysaccharides which consists of only a
single type of monosaccharide unit.
Ex.- cellulose, starch etc.
 Heteropolysaccharides or Heteroglycans -
They are polysaccharides built up of two or
more different monomeric units.
Ex.- Chitosan, Hyaluronan etc.
Starch
 It is a glucose polymer
 Made up of a mixture of amylose (15-20%) and
amylopectin (80-85%)
 They can be hydrolysed by enzyme called
amylase
•Potato, rice, wheat and maize are the
major sources of starch in human food.
Cellulose
•It is the most abundant polysaccharide.
•It is found in all plants as the major structural
component of the cell wall.
•It is the β-isomer of amylose consisting of β-
(1,4)-linked glucose residues.
Glycogen
 It is energy reserve for animals
 It is the chief form of carbohydrates stored in
animal body
 It is insoluble in water. It turns red when mixed
with iodine.
 It is composed of branched chain of glucose
residues.
 It is stored in liver and skeletal muscles.
Chitin
 Chitin is considered the most abundant
biopolymer in nature after cellulose
 Chitin is the principal structural component of
the exoskeleton of invertebrates
 There are serious difficulties in modification
reactions to prepare well-defined derivatives of
chitin since it is insoluble in common solvents
Chitosan
 Chitosan is produced from the deacetylation of
chitin
 It is a hemostatic material from which blood
anticoagulants and antithrombogenic agents
have been formed
 It is positively charged and therefore can
interact with negatively charged molecules
such as negatively charged polysaccharides,
polyanions, nucleic acid and negatively
•It is obtained commercially from shrimp or crab
shell chitin
•Chitosan is relatively inexpensive, non-toxic
• They possesses reactive amino groups and has
the capability to accelerate the healing of wound
in human
•It confers considerable antibacterial activity
against a broad spectrum of bacteria
•Chitosan has broad applications in the
biomedical field ,paper production, heavy metal
chelating agents and waste removal
CS based delivery systems have been described
for nasal, ocular, oral, parenteral and transdermal
drug delivery
Pullulan
 It is neutral, homopolysaccharide consisting of
a–(1,6)-linked maltotriose residues
 Its unique linkage pattern contributes to
exceptional physiochemical properties such as
adhesiveness, water solubility and relatively
low viscosity upon dissolving in water
 Pullulan and its derivatives have been used
industrially in foods and pharmaceuticals.
Heparin
 Due to high content of sulfo and carboxyl groups,
heparin has the highest negative charge density of
any known biological molecule
 It is extracted mainly from mucosal tissues of
porcine and bovine
 Heparin has been used as an anticoagulant since
the 1930s
 Beyond its anticoagulant activity, it shows antiviral
activity and regulate angiogenesis
Hyaluronic Acid
 Also called hyaluronan or hyaluronate or HA
 It is a linear polysaccharide consisting of
alternating units of N-acetyl-D-glucosamine
and glucuronic acid, being found in virtually
every tissue of invertebrates
 HA can form three-dimensional structures in
solution with extensive intramolecular
hydrogen bonding
 It has the ability to promote angiogenesis, to
modulate wound site inflammation by acting as
a free radical scavenger
•HA is water-soluble and forms highly
viscous solutions with unique
viscoelastic properties
Dextran
 Dextran is a water-soluble polysaccharide
which consists mainly of α-(1, 6) linked D-
glucopyranose residues with a low percentage
of α-1,2, α-1,3 and α-1,4 linked side chains
 Dextran is used as a blood plasma substitute
due to its non-toxicity
 Dextran has wide applications in novel drug
delivery systems as a polymeric carrier
•Dextran is also a suitable polymer to be used for
the preparation of hydrogels, which are becoming
increasingly important in the biomedical,
pharmaceutical, biotechnological and
environmental fields.
Cyclodextrins
 They are natural cyclic oligomers of a-
(1,4)linked-glucopyranosyl that are produced
from starch by enzymatic conversion.
 CDs have a hydrophilic exterior and a
hydrophobic cavity that enables them to act as
hosts to hydrophobic molecules
 There are three main members of the CD
family, composed of six, seven and eight
glucose units and known as α-, β- and ɤ-CD,
respectively.
•The shielding ability of CDs helps in
stabilize biomolecules from adverse
effects of non-specific interactions, which
in turn make CDs suitable for drug
delivery systems
Pectins
 Pectins are polysaccharides occurring in all
plants primarily in their cell wall
 They act as intracellular cementing material
that gives body to fruits and helps them keep
their shape
 They are composed of D–galactopyranosyl
uronic acid units, which are a–(1,4)–linkage
contain methyl esters and acetyl groups
The main mechanisms of
nanoparticle
preparation from polysaccharides
1. Covalent cross-linking
2. Ionic cross-linking
3. Polyelectrolyte complexes
(PEC)
4. Self-assembly
5.
Polysaccharide
–drug conjugate
Why is Drug Delivery important?
By using DD the ability to engineer controlled
localized delivery of drugs might contribute to
the :-
1) Efficiency of the treatment and
2) Reduces the side effects.
Enhanced permeability and
retention (EPR) effect & Drug
Delivery
It is the property by which certain sizes of
molecules tend to accumulate in tumor tissue
much more than they do in normal tissues.
This is because the tumors can induce blood
vessel growth (angiogenesis) by secreting
various growth factors which helps in tumor
expansion
REQUIREMENTS FOR AN
EFFICIENT DRUG DELIVERY
VEHICLE
THEY SHOULD BE :-
1. NON-TOXIC
2. BIOCOMPATIBLE
3. HIGH DRUG LOADING CAPACITY
4. CONTROL RELEASE AND AVIOD THE “BURST
EFFECT”
5. CONTROL MATRIX DEGRADATION AND
ENGINEER ITS SURFACE
6. BE DETECTABLE BY VARIOUS IMAGING
TECHNIQUES
IMPORTANT DD SYSTEMS
 POLYMERIC NANOPARTICLES
 QUANTUM DOTS
 METALLIC NANOPARTICLES
 POLYSACCHARIDES
 LIPOSOMES
 CERAMIC NANOPARTICLES
 CARBON NANOPARTICLES
 DENDRIMERS
All these systems can be
divided
ORGANIC
 POLYMERIC NPS
 LIPOSOMES
 POLYSACCHARIDE
S
 DENDRIMERS
 CARBON NPS
INORGANIC
 QUANTUM DOTS
 METALLIC NPS
 CERAMIC NPS
Conclusion
So we can say that of all the available drug
delivery systems the polysaccharide NP DD
systems are the most efficient because of there
outstanding virtues, such as biocompatibility,
biodegradability, low toxicity low cost and ease of
chemical modification
Polysaccharides as building blocks for nanotherapeutics

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Polysaccharides as building blocks for nanotherapeutics

  • 1. POLYSACCHARIDES AS BUILDING BLOCKS FOR NANOTHERAPEUTICS Tony Francis Department of Chemistry St. Mary’s college Manarkadu
  • 2. Introduction  Over the past two decades nanoparticles (NPs)- based therapeutics have been introduced for the treatment of cancer, diabetes, allergy, infections and inflammation.  Of the available NP systems polysaccharides are the most outstanding one because of there virtues such as biocompatibility, biodegradability, low toxicity, low cost and there ease of chemical modification
  • 3. Classification Carbohydrates  Monosaccharides- A Carbohydrate that cannot be hydrolysed further to give simple units of polyhydroxy aldehyde or ketone.  Oligosaccharides- Carbohydrate that can yield two to ten monosaccharide unit on hydrolysis.  Polysaccharides- Polymers of monosaccharides joined together by glycosidic linkage.
  • 4. Polysaccharides classification based on there origin  Plant origin – Cellulose, Pectin and guar gum  Animal origin – Chitosan, Heparin and Hyaluronan  Algal origin – Alginate and Carrageenan  Microbial origin- Dextran and Xanthan gum  Marine origin- Agar and Agarose
  • 5. Classification based on the monomer groups  Homopolysaccharides or Homoglycans- They are polysaccharides which consists of only a single type of monosaccharide unit. Ex.- cellulose, starch etc.  Heteropolysaccharides or Heteroglycans - They are polysaccharides built up of two or more different monomeric units. Ex.- Chitosan, Hyaluronan etc.
  • 6. Starch  It is a glucose polymer  Made up of a mixture of amylose (15-20%) and amylopectin (80-85%)  They can be hydrolysed by enzyme called amylase
  • 7. •Potato, rice, wheat and maize are the major sources of starch in human food.
  • 8. Cellulose •It is the most abundant polysaccharide. •It is found in all plants as the major structural component of the cell wall. •It is the β-isomer of amylose consisting of β- (1,4)-linked glucose residues.
  • 9. Glycogen  It is energy reserve for animals  It is the chief form of carbohydrates stored in animal body  It is insoluble in water. It turns red when mixed with iodine.  It is composed of branched chain of glucose residues.  It is stored in liver and skeletal muscles.
  • 10. Chitin  Chitin is considered the most abundant biopolymer in nature after cellulose  Chitin is the principal structural component of the exoskeleton of invertebrates  There are serious difficulties in modification reactions to prepare well-defined derivatives of chitin since it is insoluble in common solvents
  • 11. Chitosan  Chitosan is produced from the deacetylation of chitin  It is a hemostatic material from which blood anticoagulants and antithrombogenic agents have been formed  It is positively charged and therefore can interact with negatively charged molecules such as negatively charged polysaccharides, polyanions, nucleic acid and negatively
  • 12. •It is obtained commercially from shrimp or crab shell chitin •Chitosan is relatively inexpensive, non-toxic • They possesses reactive amino groups and has the capability to accelerate the healing of wound in human •It confers considerable antibacterial activity against a broad spectrum of bacteria •Chitosan has broad applications in the biomedical field ,paper production, heavy metal chelating agents and waste removal CS based delivery systems have been described for nasal, ocular, oral, parenteral and transdermal drug delivery
  • 13. Pullulan  It is neutral, homopolysaccharide consisting of a–(1,6)-linked maltotriose residues  Its unique linkage pattern contributes to exceptional physiochemical properties such as adhesiveness, water solubility and relatively low viscosity upon dissolving in water  Pullulan and its derivatives have been used industrially in foods and pharmaceuticals.
  • 14. Heparin  Due to high content of sulfo and carboxyl groups, heparin has the highest negative charge density of any known biological molecule  It is extracted mainly from mucosal tissues of porcine and bovine  Heparin has been used as an anticoagulant since the 1930s  Beyond its anticoagulant activity, it shows antiviral activity and regulate angiogenesis
  • 15. Hyaluronic Acid  Also called hyaluronan or hyaluronate or HA  It is a linear polysaccharide consisting of alternating units of N-acetyl-D-glucosamine and glucuronic acid, being found in virtually every tissue of invertebrates  HA can form three-dimensional structures in solution with extensive intramolecular hydrogen bonding  It has the ability to promote angiogenesis, to modulate wound site inflammation by acting as a free radical scavenger
  • 16. •HA is water-soluble and forms highly viscous solutions with unique viscoelastic properties
  • 17. Dextran  Dextran is a water-soluble polysaccharide which consists mainly of α-(1, 6) linked D- glucopyranose residues with a low percentage of α-1,2, α-1,3 and α-1,4 linked side chains  Dextran is used as a blood plasma substitute due to its non-toxicity  Dextran has wide applications in novel drug delivery systems as a polymeric carrier
  • 18. •Dextran is also a suitable polymer to be used for the preparation of hydrogels, which are becoming increasingly important in the biomedical, pharmaceutical, biotechnological and environmental fields.
  • 19. Cyclodextrins  They are natural cyclic oligomers of a- (1,4)linked-glucopyranosyl that are produced from starch by enzymatic conversion.  CDs have a hydrophilic exterior and a hydrophobic cavity that enables them to act as hosts to hydrophobic molecules  There are three main members of the CD family, composed of six, seven and eight glucose units and known as α-, β- and ɤ-CD, respectively.
  • 20. •The shielding ability of CDs helps in stabilize biomolecules from adverse effects of non-specific interactions, which in turn make CDs suitable for drug delivery systems
  • 21. Pectins  Pectins are polysaccharides occurring in all plants primarily in their cell wall  They act as intracellular cementing material that gives body to fruits and helps them keep their shape  They are composed of D–galactopyranosyl uronic acid units, which are a–(1,4)–linkage contain methyl esters and acetyl groups
  • 22. The main mechanisms of nanoparticle preparation from polysaccharides 1. Covalent cross-linking 2. Ionic cross-linking
  • 23. 3. Polyelectrolyte complexes (PEC) 4. Self-assembly 5. Polysaccharide –drug conjugate
  • 24. Why is Drug Delivery important? By using DD the ability to engineer controlled localized delivery of drugs might contribute to the :- 1) Efficiency of the treatment and 2) Reduces the side effects.
  • 25. Enhanced permeability and retention (EPR) effect & Drug Delivery It is the property by which certain sizes of molecules tend to accumulate in tumor tissue much more than they do in normal tissues. This is because the tumors can induce blood vessel growth (angiogenesis) by secreting various growth factors which helps in tumor expansion
  • 26.
  • 27. REQUIREMENTS FOR AN EFFICIENT DRUG DELIVERY VEHICLE THEY SHOULD BE :- 1. NON-TOXIC 2. BIOCOMPATIBLE 3. HIGH DRUG LOADING CAPACITY 4. CONTROL RELEASE AND AVIOD THE “BURST EFFECT” 5. CONTROL MATRIX DEGRADATION AND ENGINEER ITS SURFACE 6. BE DETECTABLE BY VARIOUS IMAGING TECHNIQUES
  • 28. IMPORTANT DD SYSTEMS  POLYMERIC NANOPARTICLES  QUANTUM DOTS  METALLIC NANOPARTICLES  POLYSACCHARIDES  LIPOSOMES  CERAMIC NANOPARTICLES  CARBON NANOPARTICLES  DENDRIMERS
  • 29. All these systems can be divided ORGANIC  POLYMERIC NPS  LIPOSOMES  POLYSACCHARIDE S  DENDRIMERS  CARBON NPS INORGANIC  QUANTUM DOTS  METALLIC NPS  CERAMIC NPS
  • 30. Conclusion So we can say that of all the available drug delivery systems the polysaccharide NP DD systems are the most efficient because of there outstanding virtues, such as biocompatibility, biodegradability, low toxicity low cost and ease of chemical modification