TataKelola dan KamSiber Kecerdasan Buatan v022.pdf
Nanotechnology based drug delivery
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Nanotechnology Based Drug DeliveryNanotechnology Based Drug Delivery
Presented by:
Chinchole Pravin Sonu
(M.PHARM 2nd
SEM)
DEPARTMENT OF PHARMACEUTICS & QUALITY
ASSURANCE
R. C. Patel Institute of Pharmaceutical Education
and Research, shirpur.
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Nanoparticles for Drug DeliveryNanoparticles for Drug Delivery
Metal-based nanoparticlesMetal-based nanoparticles
Lipid-based nanoparticlesLipid-based nanoparticles
Polymer-based nanoparticlesPolymer-based nanoparticles
Biological nanoparticlesBiological nanoparticles
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NanobiopharmaceuticalsNanobiopharmaceuticals
In biopharmaceuticals, in addition to theIn biopharmaceuticals, in addition to the
main technologies covered-liposomal,main technologies covered-liposomal,
monoclonal antibody-based, and polymer-monoclonal antibody-based, and polymer-
based technologies host of newerbased technologies host of newer
technologies such as nanoparticlestechnologies such as nanoparticles
including various nanodimensional entitiesincluding various nanodimensional entities
such as molecular imprinted polymers,such as molecular imprinted polymers,
metallofullerenes, prodrug delivery, oral,metallofullerenes, prodrug delivery, oral,
injectable and implantable, pulmonary, andinjectable and implantable, pulmonary, and
transdermal and transmucosal deliverytransdermal and transmucosal delivery
have come up.have come up.
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Drug Delivery Technology Important toDrug Delivery Technology Important to
Pharma IndustryPharma Industry
Drug delivery formulations involve low costDrug delivery formulations involve low cost
research compared that for discovery ofresearch compared that for discovery of
new molecule,new molecule,
Minimizing the drug use would significantlyMinimizing the drug use would significantly
reduce the effective cost of drug whichreduce the effective cost of drug which
would give financial relief to the patients,would give financial relief to the patients,
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Delivery systems increase commercialDelivery systems increase commercial
opportunity by distinguishing a drug fromopportunity by distinguishing a drug from
competitive threats posed by “me too”competitive threats posed by “me too”
drugs anddrugs and
Novel means of delivery particularly usingNovel means of delivery particularly using
nano-carriers, can allow branded drugs tonano-carriers, can allow branded drugs to
be rescued from abyss of genericbe rescued from abyss of generic
competition (may be called “resurrection ofcompetition (may be called “resurrection of
drug”).drug”).
Drug Delivery Technology Important toDrug Delivery Technology Important to
Pharma IndustryPharma Industry
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SOME SIGNIFICANT ACHIEVEMENTS OFSOME SIGNIFICANT ACHIEVEMENTS OF
NANODEVICESNANODEVICES
Development of one dose a day ciprofloxacin usingDevelopment of one dose a day ciprofloxacin using
nanotechnologynanotechnology
Tumor targeted taxol delivery using nanoparticles inTumor targeted taxol delivery using nanoparticles in
Phase 2 clinical trial stagePhase 2 clinical trial stage
Improved ophthalmic delivery formulation usingImproved ophthalmic delivery formulation using
smart hydrogel nanoparticlessmart hydrogel nanoparticles
Oral insulin formulation using nanoparticles carriers.Oral insulin formulation using nanoparticles carriers.
Liposomal based Amphotericin B formulationLiposomal based Amphotericin B formulation
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CHALLENGESCHALLENGES
Prevention of drug from biological degradationPrevention of drug from biological degradation
Effective TargetingEffective Targeting
Patient CompliancePatient Compliance
Cost effectivenessCost effectiveness
Product life extensionProduct life extension
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PRIORITY AREASPRIORITY AREAS
Cancer NanotechnologyCancer Nanotechnology
(i)(i) Diagnosis using QuantumDiagnosis using Quantum
DotsDots
(ii) Tumor Targeted Delivery(ii) Tumor Targeted Delivery
(iii)(iii) ImagingImaging
(iv) Cancer Gene Therapy(iv) Cancer Gene Therapy
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PRIORITY AREASPRIORITY AREAS
DNA Vaccines for parasitic, bacterial andDNA Vaccines for parasitic, bacterial and
viral diseasesviral diseases
Oral and pulmonary routes for systemicOral and pulmonary routes for systemic
delivery of proteins and peptidesdelivery of proteins and peptides
Nanotechnology in Tissue EngineeringNanotechnology in Tissue Engineering
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Liposome'sLiposome's
Their exterior lipid bilayer is very chemically reactive, thereby providing aTheir exterior lipid bilayer is very chemically reactive, thereby providing a
means to conveniently couple “tags” on a covalent basis.means to conveniently couple “tags” on a covalent basis.
Such “tags” can be antibodies, antigens, cell receptors, nucleic acidSuch “tags” can be antibodies, antigens, cell receptors, nucleic acid
probes, etc.probes, etc.
This provides significant versatility in assay formats (i.e., immunoassay,This provides significant versatility in assay formats (i.e., immunoassay,
receptor-based, nucleic acid probe, etc.) possible.receptor-based, nucleic acid probe, etc.) possible.
With diameters ranging in size from approximately 50 nm to 800 nm,With diameters ranging in size from approximately 50 nm to 800 nm,
their aqueous core encapsulates up to millions of molecules of signaltheir aqueous core encapsulates up to millions of molecules of signal
generating “markers” that can be detected in a variety of different way.generating “markers” that can be detected in a variety of different way.
A variety of different encapsulants are possible including visuallyA variety of different encapsulants are possible including visually
detectable dyes (since the lipid bilayer is transparent), optically anddetectable dyes (since the lipid bilayer is transparent), optically and
fluorometrically detectable dyes, enzymes, and electroactive compounds.fluorometrically detectable dyes, enzymes, and electroactive compounds.
This provides significant versatility in the detection schemes possible.This provides significant versatility in the detection schemes possible.
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NiosomesNiosomes
Niosomes, non-ionic surfactant vesicles, are widely studied as anNiosomes, non-ionic surfactant vesicles, are widely studied as an
alternative to liposomesalternative to liposomes
These vesicles appear to be similar to liposomes in terms of theirThese vesicles appear to be similar to liposomes in terms of their
physical propertiesphysical properties
They are also prepared in the same way and under a variety ofThey are also prepared in the same way and under a variety of
conditions, from unilamellar or multilamellar structures.conditions, from unilamellar or multilamellar structures.
Niosomes alleviate the disadvantages associated with liposomes,Niosomes alleviate the disadvantages associated with liposomes,
such as chemical instability, variable purity of phospholipids andsuch as chemical instability, variable purity of phospholipids and
high cost.high cost.
They have the potential for controlled and targated drug deliveryThey have the potential for controlled and targated drug delivery
Niosomes enhanced the penetration of drugsNiosomes enhanced the penetration of drugs
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NanopowderNanopowder
Nanopowders are powders composed ofNanopowders are powders composed of
nanoparticles, that is particles having an averagenanoparticles, that is particles having an average
diameter below 50 nanometers (nm).diameter below 50 nanometers (nm).
A jar of a true nanopowder when emptied fromA jar of a true nanopowder when emptied from
chest height to toward the floor will disperse intochest height to toward the floor will disperse into
the air before reaching the floor.the air before reaching the floor.
Most manufacturers of “nanopowders” produceMost manufacturers of “nanopowders” produce
micropowder assemblies of nanoparticles but themicropowder assemblies of nanoparticles but the
powder itself is rarely a nanopowder.powder itself is rarely a nanopowder.
Such compounds have two or more differentSuch compounds have two or more different
cations (positively charged elements) in theircations (positively charged elements) in their
chemical formula. An example of a complexchemical formula. An example of a complex
compound is calcium titanate (CaTiO3).compound is calcium titanate (CaTiO3).
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NanoclusterNanocluster
One of the central themes in nanoscienceOne of the central themes in nanoscience
research is to synthesize high qualityresearch is to synthesize high quality
nanoparticles with precise control overnanoparticles with precise control over
particle size, shape, structure, andparticle size, shape, structure, and
composition.composition.
For inorganic nanoparticles (e.g. metalFor inorganic nanoparticles (e.g. metal
and semiconductor), two regimes are ofand semiconductor), two regimes are of
particular interest, that is, nanoclusters inparticular interest, that is, nanoclusters in
a size range from subnanometer to ~2 nma size range from subnanometer to ~2 nm
and nanocrystals (typically 2-100 nm).and nanocrystals (typically 2-100 nm).
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NanocrystalsNanocrystals
When the size of the material is reduced to less than 100When the size of the material is reduced to less than 100
nanometers, the realm of quantum physics takes over andnanometers, the realm of quantum physics takes over and
materials begin to demonstrate entirely new properties.materials begin to demonstrate entirely new properties.
Nano-design of drugs by various techniques like milling,Nano-design of drugs by various techniques like milling,
high pressure homogenization, controlled precipitation etc.,high pressure homogenization, controlled precipitation etc.,
are explored to produce, drug nanocrystals, nanoparticles,are explored to produce, drug nanocrystals, nanoparticles,
nanoprecipitates, nanosuspensions (which for ease ofnanoprecipitates, nanosuspensions (which for ease of
understanding commonly mentioned as nanocrystals).understanding commonly mentioned as nanocrystals).
As decreased size will increase the solubility of drugsAs decreased size will increase the solubility of drugs
hence, this technology is explored to increase oralhence, this technology is explored to increase oral
bioavailability of sparingly water soluble drugs.bioavailability of sparingly water soluble drugs.
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MicelleMicelle
Micelle is an aggregate of amphipathic molecules in water, with theMicelle is an aggregate of amphipathic molecules in water, with the
nonpolar portions in the interior and the polar portions at the exteriornonpolar portions in the interior and the polar portions at the exterior
surface, exposed to water.surface, exposed to water.
Amphiphilic molecules form micelle above a particular concentration whichAmphiphilic molecules form micelle above a particular concentration which
is called as critical micellar concentration (CMC).is called as critical micellar concentration (CMC).
Micelles are known to have an anisotropic water distribution within theirMicelles are known to have an anisotropic water distribution within their
structure, means water concentration decreases from the surface towardsstructure, means water concentration decreases from the surface towards
the core of the micelle, with a completely hydrophobic (water-excluded)the core of the micelle, with a completely hydrophobic (water-excluded)
core.core.
Hydrophobic drugs can be encapsulated/solubalized, into inner core.Hydrophobic drugs can be encapsulated/solubalized, into inner core.
The spatial position of a solubilized drug in a micelle will depend on itsThe spatial position of a solubilized drug in a micelle will depend on its
polarity, nonpolar molecules will be solubilized in the micellar core, andpolarity, nonpolar molecules will be solubilized in the micellar core, and
substances with intermediate polarity will be distributed along thesubstances with intermediate polarity will be distributed along the
surfactant molecules in certain intermediatesurfactant molecules in certain intermediate
positions.positions.
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DendrimersDendrimers
These branched macromolecules are constructed around aThese branched macromolecules are constructed around a
simple core unit.simple core unit.
Dendrimers have a high degree of molecular uniformity,Dendrimers have a high degree of molecular uniformity,
narrow molecular weight distribution, specific size andnarrow molecular weight distribution, specific size and
shape characteristics, and a highly- functionalizedshape characteristics, and a highly- functionalized
terminal surface.terminal surface.
The manufacturing process is a series of repetitive stepsThe manufacturing process is a series of repetitive steps
starting with a central initiator core. Each subsequentstarting with a central initiator core. Each subsequent
growth step represents a new "generation" of polymer withgrowth step represents a new "generation" of polymer with
a larger molecular diameter, twice the number of reactivea larger molecular diameter, twice the number of reactive
surface sites, and approximately double the molecularsurface sites, and approximately double the molecular
weight of the preceding generation.weight of the preceding generation.
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Polymeric NanoparticlesPolymeric Nanoparticles
In recent years, biodegradable polymericIn recent years, biodegradable polymeric
nanoparticles have attracted considerablenanoparticles have attracted considerable
attention as potential drug deliveryattention as potential drug delivery
devices in view of their applications indevices in view of their applications in
drug targeting to particulardrug targeting to particular
organs/tissues, as carriers of DNAorgans/tissues, as carriers of DNA
in gene therapy, and in their ability toin gene therapy, and in their ability to
deliver proteins, peptides and genesdeliver proteins, peptides and genes
through a per oral route of administration.through a per oral route of administration.
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Carbon 60Carbon 60
C60 are spherical molecules about 1nm inC60 are spherical molecules about 1nm in
diameter, comprising 60 carbon atomsdiameter, comprising 60 carbon atoms
arranged as 20 hexagons and 12 pentagons: thearranged as 20 hexagons and 12 pentagons: the
configuration of a football.configuration of a football.
Hence they find application asHence they find application as
NanoPharmaceuticals with large drug payload inNanoPharmaceuticals with large drug payload in
their cage like structure.their cage like structure.
On the other hand with development of variousOn the other hand with development of various
chemical substitutes for C60, it is possible tochemical substitutes for C60, it is possible to
develop functionalized C60 with better drugdevelop functionalized C60 with better drug
targeting propertiestargeting properties
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Carbon NanotubeCarbon Nanotube
Carbon nanotubes are adept at entering theCarbon nanotubes are adept at entering the
nuclei of cells and may one day be used tonuclei of cells and may one day be used to
deliver drugs and vaccines.deliver drugs and vaccines.
The modified nanotubes have so far only beenThe modified nanotubes have so far only been
used to ferry a small peptide into the nuclei ofused to ferry a small peptide into the nuclei of
fibroblast cells.fibroblast cells.
But the researchers are hopeful that theBut the researchers are hopeful that the
technique may one day form the basis for newtechnique may one day form the basis for new
anti-cancer treatments, gene therapies andanti-cancer treatments, gene therapies and
vaccines.vaccines.
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Equipments for NanoparticlesEquipments for Nanoparticles
1.Homogenizer
2.Ultra Sonicator
3.Mills
4.Spray Milling
5.Supercritical Fluid Technology
6.Electrospray
7.Ultracentrifugation
8.Nanofiltration