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Use of Natural Polymers in novel Drug Delivery Systems using
Nanotechnology
by Group C:
Mehrab Tahir, Esha-tur-Razia, Ateeq-ur-Rehman, Tayyaba Khan, Aiman Imran, Shiza Batool, Shanza
Mir, Iqra Bibi, Sahar Alvi and Ramiza Rashid.
Introduction
●
Polymers are large molecules obtained from
conjugation reactions of repeating subunits
called monomers.
●
Natural polymers used in pharmaceutical
industry mainly include carbohydrates and
proteins from animal, plant or microbial
sources.
●
Nanoparticles of natural polymers and their
modified derivatives are very promising
candidates for the mucosal, colonic and
different targeted protein/peptide,
gene/vaccine, and anticancer drug
delivery. This technology can be employed
to make stimuli-responsive and controlled-
release novel Drug delivery systems.
We will further discuss a few important polymers and their derivatives that are most commonly used in novel drug
delivery systems using nanotechnology.
A simple classification of natural polymers could be as follows:
Biocompatible
Renewable
Non-
mutagenic
Non-
immunogenic
Low cost
General
properties
of Natural
polymers
Chemically
modifiable
Low cost
Non-toxic
Thiomers
or Thiolated
polymers i.e.
basically thiol
group conjugated
polymers have
enhanced
mucoadhesive,
enzyme
inhibiting, efflux-
pump inhibiting and permeation-
enhancing properties can prove to be
useful tools for the delivery of various
types of challenging drugs.
Pullulan
●
An Exopolysaccharide (a surface carbohydrate present outside bacterial and
fungal cells) of homopolysaccharide nature produced by yeast-like fungus
Aureobasidium pullulans.
●
It’s neutral, amorphous, hydrophillic and water-soluble in nature but its main
derivatives are modified to attain hydrophobic characteristics. It has low
viscosity in solution.
i. Peptide/ protein drug
delivery with increased
bioavailibility &
stability.
ii. Nanogels interactive
with β-amyloid
proteins in Alzheimer’s
Disease.
v. targeted liver disease
treatment/ MRI
diagnosis
vi. DNA/ protein delivery
to brain
vii.ionic strength sensitive
delivery of
radioisotopes to
tumour cells
iii.pH-sensitive and
thermo-sensitive drug
release systems for
targeted anticancer
and anti-ischemic
effects.
iv. Gene silencing by
siRNA delivery.
Use of Pullulan Nanoparticles
i. Hydrogels as wound
healing dressing
materials.
iv. Targeted drug delivery
of hydrophobic anti-
cancer cells in breast
cancer and colorectal
adenocarcinoma.
ii. Sun protection through
absorption of UV
radiations
iii.pH sensitive hydrogels
and nanocapsules for
controlled release of
hydrophobic drugs.
Use of Lignin Nanoparticles
Lignin
●
A by-product from the pulp and paper industry. This homopolysaccharide is extracted from various sources
of biomass (wood biomass, trees, wheat straw, corn stover etc) following kraft, sulfite, soda, and
organosolvation processing methods.
●
It is highly branched, amorphous, polyphenolic and aromatic in nature. It shows better miscibility with
other polymers, and improved antioxidant activity.
i. Carriers in drug
delivery for water
soluble antibiotics e.g.
tetracycline and
duoxorubicin etc.
iv. diagnosis and
biosensing. e.g. for
detection of human
nutrophil elastase
enzyme at site of
infection.
ii. colon-specific drug
delivery
iii.targeted delivery of
chemotherapeutic,
antiviral and
antibacterial agents.
Use of Cellulose Nanoparticles
Cellulose
●
One of the most abundant naturally occuring homopolysaccharide. Due to its
multiple reactive hydroxyl groups, it can be chemically modified into multiple
derivatives with enhanced as well as variable characteristics.
●
Cellulose itself is water-insoluble. Cellulose nanomaterials have higher
crystallinity, water-solubility and overall electrostatic stability & dispersibility.
i. Oral delivery systems
of Low solubility
medications (BCS
Classes II and IV).
Drastically enhances
solution concentration
by lowering the
crystallinity of drug,
stabilizing amorphous
drug after dissolving,
and preventing
recrystallization.
ii. Used in anti-cancer
oral delivery for
colon cancer.
iii. Used in control-
release transdermal
and transmucosal
delivery.of
hydrophobic drugs.
Use of CMC Nanoparticles
Carboxy Methyl Cellulose
●
A cellulose derivative and an anionic water-soluble
biopolymer. CMC is frequently utilised in drug
delivery and other biomedical studies because of its
hydrophilicity, bioadhesiveness, pH sensitivity and
gel forming characteristics.
●
It is highly branched, amorphous, polyphenolic and
aromatic in nature. It shows better miscibility with
other polymers, and improved antioxidant activity.
i. carrier for
antimicrobial agents as
well as scaffold in
wound dressing.
ii. FDA approved for
ocular use, and
relatively inexpensive.
Microcrystalline Cellulose
●
A cellulose derivative obtained by acid hydrolysis, mechanical, oxidative and enzymatic treatments of
cellulose fibers. Modified MCC can be used in tissue engineering, inorganic reaction template and drug
delivery.
●
MCC compared to cellulose fibers, has more advantages, such as nanoscale dimension, high surface area,
high specific strength and modulus and unique optical characteristics.
Use of MCC Nanoparticles
Chitosan
●
Obtained by the
alkaline deacetylation
of chitin, belonging to
heteropolysaccharide
class composed of two
repeating monomers;
glucosamine and N-
acetylglucosamine.
●
Polycationic in nature,
has antioxidant &
radical scavenging
activity.
●
Drug release
mechanisms include:

Diffusion

Swelling

Erosion.
i. Nasal drug delivery
systems with increased
bioavailibility.
ii. Oral peptide/protein
drug delivery system
with increased
permeation, stability
and bioavailibility.
iii.Modified Oral drug
delivery i.e.
mucoadhesive,
prolonged release etc.
vii.Enhanced transnasal
brain drug delivery to
treat CNS disorders.
viii.In gene therapy for
gene silencing using
siRNA.
iv. Enhanced anticancer
effect in colon and liver
cancer.
v. Ocular drug delivery
with better
mucoadhesion, more
stability and more
effectiveness using
thiomer.
vi. pH-sensitive antibiotic
delivery.
Use of Chitosan Nanoparticles
i. Binding agent
ii. Sustained release drug
delivery to increase oral
drug bioavailibility
iii.Anti-TB drug carrier
iv. Sustained release ocular
drug delivery system
Alginate
●
Obtained by extraction of brown seaweed by alkaline solution to solubilize alginic acid , then transforming it
into it’s salt form.
●
It has high cell affinity, good gelling properties and favorable mechanical strength.
Use of Alginate Nanoparticles
Hyaluronic Acid
●
Containing 2 repeating monomers of glucuronic acid and N -acetylglucosamine.
●
Obtained from animal origin or by fermentation of genetically modified bacteria.
●
Anti-inflammatory,analgesic and bacteriostatic effect.
●
CD4 receptor targeting intrinsic ability.
i. Anti-neoplastic drug
delivery system.
ii. Ocular surgery
iii.Wound Dressing.
iv. HA-based drug
delivery system.
v. HA-based nanogels in
cancer therapy.
vi. HA-based nanogels in
ocular drug delivery
system.
vii.Modified HA-based
nanogels role in
bacterial infections.
Use of Hyaluronic acid
Nanoparticles
●
Ocular drug delivery
system
●
Ulcerative colitis
treatment.
●
Cancer therapy.
●
Treatment of TB.
●
CNS delivery of drug.
●
Macrophages therapy
Gelatin
●
Obtained by hydrolysis of collagen.
●
Has cationic and anionic groups.
●
Triplet helical structure composed of repeating triplets of alanine,proline, and glycine.
●
Biphasic in nature, based upon interaction with gelatin-NPs , weakly bound drug release immediately
followed by release of tightly bound drug in a slow manner for sustained release effect.
Use of Gelatin Nanoparticles
Albumin
●
Protein in nature is found in eggs, milk and in blood serum made by liver.
●
Thiolated Albumin has enhanced mucoadhesive,stabilizing, and mechanical
properties
●
High drug loading capacity and hydrophillic in nature.
i. Targeted anticancer
therapy in pancreatic
cancer.
ii. Drug delivery against
AIDS.
iii. CNS drug delivery.
iv. Sustained release of
drugs.
Use of Albumin
Nanoparticles
i. Carriers for sustained
release and more efficient
drug delivery.
ii. Treatment of pancreatic
cancer by Chinese
medicine.
iii. Particle tracking via
coupling with fluorescent
marker.
Fibroin
●
Is a dominant silk protein possessing ideal characteristics for fibroin nanoparticle formulation.
●
It’s highly water-soluble and possesses preparation flexibility.
●
It’s characteristic of being amphoteric in nature allows it to strengthen itself by making cross-links with itself
and other positively charged polymers.
Use of Fibroin
Nanoparticles
iv. Targeted ocular drug
delivery system for
treatment of fungal
keratitis.
v. Orthopedic
administration.
Legumin
●
Major storage protein of soybean.
●
Six sub-units pairs linked via a disulfide bond.
●
Bioadhesive, large surface area , low antigenicity, ease of particle size control.
●
Numerous biomedical applications.
i. As drug carriers in
anticancer therapy
against non-small lung
tumor
ii. Targeted gene delivery.
Use of Legumin Nanoparticles

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natural polymers in pharmatechnology.pdf

  • 1. Use of Natural Polymers in novel Drug Delivery Systems using Nanotechnology by Group C: Mehrab Tahir, Esha-tur-Razia, Ateeq-ur-Rehman, Tayyaba Khan, Aiman Imran, Shiza Batool, Shanza Mir, Iqra Bibi, Sahar Alvi and Ramiza Rashid.
  • 2. Introduction ● Polymers are large molecules obtained from conjugation reactions of repeating subunits called monomers. ● Natural polymers used in pharmaceutical industry mainly include carbohydrates and proteins from animal, plant or microbial sources. ● Nanoparticles of natural polymers and their modified derivatives are very promising candidates for the mucosal, colonic and different targeted protein/peptide, gene/vaccine, and anticancer drug delivery. This technology can be employed to make stimuli-responsive and controlled- release novel Drug delivery systems. We will further discuss a few important polymers and their derivatives that are most commonly used in novel drug delivery systems using nanotechnology. A simple classification of natural polymers could be as follows:
  • 3. Biocompatible Renewable Non- mutagenic Non- immunogenic Low cost General properties of Natural polymers Chemically modifiable Low cost Non-toxic Thiomers or Thiolated polymers i.e. basically thiol group conjugated polymers have enhanced mucoadhesive, enzyme inhibiting, efflux- pump inhibiting and permeation- enhancing properties can prove to be useful tools for the delivery of various types of challenging drugs.
  • 4. Pullulan ● An Exopolysaccharide (a surface carbohydrate present outside bacterial and fungal cells) of homopolysaccharide nature produced by yeast-like fungus Aureobasidium pullulans. ● It’s neutral, amorphous, hydrophillic and water-soluble in nature but its main derivatives are modified to attain hydrophobic characteristics. It has low viscosity in solution. i. Peptide/ protein drug delivery with increased bioavailibility & stability. ii. Nanogels interactive with β-amyloid proteins in Alzheimer’s Disease. v. targeted liver disease treatment/ MRI diagnosis vi. DNA/ protein delivery to brain vii.ionic strength sensitive delivery of radioisotopes to tumour cells iii.pH-sensitive and thermo-sensitive drug release systems for targeted anticancer and anti-ischemic effects. iv. Gene silencing by siRNA delivery. Use of Pullulan Nanoparticles
  • 5. i. Hydrogels as wound healing dressing materials. iv. Targeted drug delivery of hydrophobic anti- cancer cells in breast cancer and colorectal adenocarcinoma. ii. Sun protection through absorption of UV radiations iii.pH sensitive hydrogels and nanocapsules for controlled release of hydrophobic drugs. Use of Lignin Nanoparticles Lignin ● A by-product from the pulp and paper industry. This homopolysaccharide is extracted from various sources of biomass (wood biomass, trees, wheat straw, corn stover etc) following kraft, sulfite, soda, and organosolvation processing methods. ● It is highly branched, amorphous, polyphenolic and aromatic in nature. It shows better miscibility with other polymers, and improved antioxidant activity.
  • 6. i. Carriers in drug delivery for water soluble antibiotics e.g. tetracycline and duoxorubicin etc. iv. diagnosis and biosensing. e.g. for detection of human nutrophil elastase enzyme at site of infection. ii. colon-specific drug delivery iii.targeted delivery of chemotherapeutic, antiviral and antibacterial agents. Use of Cellulose Nanoparticles Cellulose ● One of the most abundant naturally occuring homopolysaccharide. Due to its multiple reactive hydroxyl groups, it can be chemically modified into multiple derivatives with enhanced as well as variable characteristics. ● Cellulose itself is water-insoluble. Cellulose nanomaterials have higher crystallinity, water-solubility and overall electrostatic stability & dispersibility.
  • 7. i. Oral delivery systems of Low solubility medications (BCS Classes II and IV). Drastically enhances solution concentration by lowering the crystallinity of drug, stabilizing amorphous drug after dissolving, and preventing recrystallization. ii. Used in anti-cancer oral delivery for colon cancer. iii. Used in control- release transdermal and transmucosal delivery.of hydrophobic drugs. Use of CMC Nanoparticles Carboxy Methyl Cellulose ● A cellulose derivative and an anionic water-soluble biopolymer. CMC is frequently utilised in drug delivery and other biomedical studies because of its hydrophilicity, bioadhesiveness, pH sensitivity and gel forming characteristics. ● It is highly branched, amorphous, polyphenolic and aromatic in nature. It shows better miscibility with other polymers, and improved antioxidant activity.
  • 8. i. carrier for antimicrobial agents as well as scaffold in wound dressing. ii. FDA approved for ocular use, and relatively inexpensive. Microcrystalline Cellulose ● A cellulose derivative obtained by acid hydrolysis, mechanical, oxidative and enzymatic treatments of cellulose fibers. Modified MCC can be used in tissue engineering, inorganic reaction template and drug delivery. ● MCC compared to cellulose fibers, has more advantages, such as nanoscale dimension, high surface area, high specific strength and modulus and unique optical characteristics. Use of MCC Nanoparticles
  • 9. Chitosan ● Obtained by the alkaline deacetylation of chitin, belonging to heteropolysaccharide class composed of two repeating monomers; glucosamine and N- acetylglucosamine. ● Polycationic in nature, has antioxidant & radical scavenging activity. ● Drug release mechanisms include:  Diffusion  Swelling  Erosion.
  • 10. i. Nasal drug delivery systems with increased bioavailibility. ii. Oral peptide/protein drug delivery system with increased permeation, stability and bioavailibility. iii.Modified Oral drug delivery i.e. mucoadhesive, prolonged release etc. vii.Enhanced transnasal brain drug delivery to treat CNS disorders. viii.In gene therapy for gene silencing using siRNA. iv. Enhanced anticancer effect in colon and liver cancer. v. Ocular drug delivery with better mucoadhesion, more stability and more effectiveness using thiomer. vi. pH-sensitive antibiotic delivery. Use of Chitosan Nanoparticles
  • 11. i. Binding agent ii. Sustained release drug delivery to increase oral drug bioavailibility iii.Anti-TB drug carrier iv. Sustained release ocular drug delivery system Alginate ● Obtained by extraction of brown seaweed by alkaline solution to solubilize alginic acid , then transforming it into it’s salt form. ● It has high cell affinity, good gelling properties and favorable mechanical strength. Use of Alginate Nanoparticles
  • 12. Hyaluronic Acid ● Containing 2 repeating monomers of glucuronic acid and N -acetylglucosamine. ● Obtained from animal origin or by fermentation of genetically modified bacteria. ● Anti-inflammatory,analgesic and bacteriostatic effect. ● CD4 receptor targeting intrinsic ability. i. Anti-neoplastic drug delivery system. ii. Ocular surgery iii.Wound Dressing. iv. HA-based drug delivery system. v. HA-based nanogels in cancer therapy. vi. HA-based nanogels in ocular drug delivery system. vii.Modified HA-based nanogels role in bacterial infections. Use of Hyaluronic acid Nanoparticles
  • 13. ● Ocular drug delivery system ● Ulcerative colitis treatment. ● Cancer therapy. ● Treatment of TB. ● CNS delivery of drug. ● Macrophages therapy Gelatin ● Obtained by hydrolysis of collagen. ● Has cationic and anionic groups. ● Triplet helical structure composed of repeating triplets of alanine,proline, and glycine. ● Biphasic in nature, based upon interaction with gelatin-NPs , weakly bound drug release immediately followed by release of tightly bound drug in a slow manner for sustained release effect. Use of Gelatin Nanoparticles
  • 14. Albumin ● Protein in nature is found in eggs, milk and in blood serum made by liver. ● Thiolated Albumin has enhanced mucoadhesive,stabilizing, and mechanical properties ● High drug loading capacity and hydrophillic in nature. i. Targeted anticancer therapy in pancreatic cancer. ii. Drug delivery against AIDS. iii. CNS drug delivery. iv. Sustained release of drugs. Use of Albumin Nanoparticles
  • 15. i. Carriers for sustained release and more efficient drug delivery. ii. Treatment of pancreatic cancer by Chinese medicine. iii. Particle tracking via coupling with fluorescent marker. Fibroin ● Is a dominant silk protein possessing ideal characteristics for fibroin nanoparticle formulation. ● It’s highly water-soluble and possesses preparation flexibility. ● It’s characteristic of being amphoteric in nature allows it to strengthen itself by making cross-links with itself and other positively charged polymers. Use of Fibroin Nanoparticles iv. Targeted ocular drug delivery system for treatment of fungal keratitis. v. Orthopedic administration.
  • 16. Legumin ● Major storage protein of soybean. ● Six sub-units pairs linked via a disulfide bond. ● Bioadhesive, large surface area , low antigenicity, ease of particle size control. ● Numerous biomedical applications. i. As drug carriers in anticancer therapy against non-small lung tumor ii. Targeted gene delivery. Use of Legumin Nanoparticles