Drug Carrier System
Drug Carrier System
Drug Carrier System
Presenter:Javaria Asghar
06331513019
Introduction
Drug;
Medicine or other substance which has a physiological effect when introduced or ingested into the
body.
Drug carriers:
• Any substrate used in the process of drug delivery.
• Functions:
1. Selectivity
2. Effectiveness
3. Safety
4. Primarily used to control the release of a drug into systemic circulation.
5. Improve pharmacokinetic properties
6. Improve bioavailability
• Drug delivery is the method or process of administering
a pharmaceutical compound to achieve a therapeutic effect in
humans or animals.
• The carriers can be made slowly degradable, stimuli-reactive
(e.g., pH- or temperature-sensitive)
• They can even be targeted (e.g., by conjugating them with
specific antibodies against certain characteristic components
of the area of interest).
Pharmaceutical carriers
• Liquid crystal:May flow like a liquid, but its molecules may be oriented in
a crystal-like way.
• Micelles: These are aggregates of surfactant molecules dispersed in a liquid
colloid.
• Dendritic polymers:Highly branched polymers with controllable structures,
which possess a large population of terminal functional groups, low solution or
melt viscosity, and good solubility. Their size, degree of branching and
functionality can be adjusted and controlled through the synthetic procedures.
• Nanoparticles:particulate dispersions or solid particles of size 10-1000nm.drug
can be dissolved,entraped encapsulated or attached to a nanoparticle matrix.
• Nanocapsules:They are vesicular systems made of a polymeric
membrane which encapsulates an inner liquid core at the nanoscale
• Nanospheres: Nanospheres are typically solid polymers with drugs
embedded in the polymer matrix.
Methods:
1. Encapsulation
2. Conjugation
• Drugs can be encapsulated in erythrocyte or bound to cell
membranes when erythrocyte is used as carriers.
• Drugs are mainly encapsulated in carriers, if nanoparticles or platelets
are used as drug delivery carriers
Various drug carriers that are envisaged in advanced delivery systems are :
• Soluble polymers.(CMC, hydrogels, PVC)
• Inorganic nanoparticles(silver(bactericides), gold in cancer treatment).
• Magnetic nanoparticles.(Cobalt, platinum)
• Biodegradable microsphere polymers (synthetic and natural).
• Neutrophils
• Fibroblasts.
• Artificial cells.
• Lipoproteins.
• Liposomes
• Micelles and immune micelle(to boost immune system by targeting lymph nodes).
Importance, Applications
and limitations
Mahnoor Nadeem
06331513037
Importance:
• Can target different organs to produce desired action without causing
harm to other healthy organs.
• Enhances the bioavailabilty of the drug administered orally by
avoiding first pass effect.
• Enhances drug absorption.
• Enhances solubility of poorly soluble drugs.
• Improve stability of drugs.
• Large molecule weight like protein can be administered.
• Scale up feasibility.
• Controlled and sustained release drugs.
• Three to five fold increase in drug plasma peaks.
• Good potential as vaccines adjuvant.
• Lower cytotoxicity.
• Specific accumulation in kpuffer cells for targeted liver delivery
diseases.
Applications:
• As the current chemotherapy is aimed at destroying all the rapidly
dividing cells, it can also damage the rapidly proliferating cells such as
hair follicles and intestinal epithelium. Cancer treatment with
nanoparticles is presented as a new option. In the treatment
performed with nanoparticles, other tissues and organs other than
the diseased area are not affected.
• In recent years, nanoparticles are topically used in wound healing.
The slower release of the nanoparticles than the gel increases the
retention time on the skin.
• Jaramillo-Ruiz et al., showed for the first time that carboxylan
dendrimers can be used in the prevention of infections developing as
a result of HIV and the suppression of T-cells.
• New researches have been conducted for Hepatitis B virus (HBV) by
using nanotechnology.
• In diabetic patients, . Decreased glucose level in interstitial fluid is
determined through polyethylene nanosensors coated with
fluorescent molecules subcutaneously placed in order to monitor
glucose levels.
• Also, artificial pancreas is considered as a permanent method for
diabetic patients. Silicone box with a diameter of 20 nm is coated with
nanopores. It is aimed to replace the healthy beta cells taken from the
animals with nonfunctional cells.
• Nanotechnological drugs provide treatment alternatives for
cardiovascular diseases at a cellular level. Chemoreceptors placed in the
carbon nanotechnological device can differentiate the plaques in the
arterial wall.
• In another study, bone regeneration is provided by administering
magnetic nanoparticles directly to the bone for osteoporosis treatment.
• It is reported that nanocalcium carbonate and nanocalcium citrate
applications have increased the bone mineral density in the rats
undergoing ovariectomy.
• Tricalcium phosphate nanoparticles containing zinc were injected to
the rats with osteoporosis and positive results are obtained as a result
of the jawbone mineral density measurements.
Limitations:
• The administration and implementation cost of Nano medicine is much
more expensive.
• Cytotoxicity of the nanoparticles also becomes a threat for future.
• Nano product facing greater problem due to their much higher cost and
complexicity.
• The limited availability and lower production rate of personalized
medicine & device is problematic for a large amount of user.
• Some innovative & noninvasive delivery improve the patient
acceptance by lowering the marketed price & production cost. I.e. Why
these results in the product degradation & quality issue.
• All type of drugs or medicine cannot be administered through the
nanoparticles, carriers or devices because they cannot be
incorporated in the polymer matric or they can be degraded.
• Novel drugs which are administered through the oral cavity should
possess the risk of undergoing acid or enzymatic degradation or
hydrolysis.
• Drug burst release by erosion.
• Lack of wide clinical studies.
• Low drug payload for hydrophilic drugs.
• Possibility of toxicity of the materials
• Harmful degradation products
• Necessity of surgical intervention either on
systems application or removal
• Patients discomfort with DDS device usage
• High cost of final product
Vesicular Drug Delivery
Systems
HADIQA ARSHAD
06331513008
• Deliver the drug at a rate directed by need of
body during the period of treatment, and
channel the active entity to the site of action
Definition • Various routes of administration, to achieve
targeted and controlled drug delivery .
• Improves the therapeutic efficacy and
reduces the side effects.
Types
• 20 nanometers to several micrometers in
size.
• Lipid bilayer structures.
• Enclosed by a membrane, composed of lipid
molecules :both hydrophilic and lipophilic
drugs can be successfully entrapped.; within
1. bilayer membrane.
Liposomes • Hydrophilic drugs get entrapped in the central
aqueous core of the vesicles.
• Attach to cellular membrane :fuse with them,
releasing their content into the cell.
• Drug trapped inside is released.
• Amphotericin B, Doxorubicin, Daunorubicin
• Lipid based drug delivery system .
• parenteral delivery of drugs having poor aqueous
solubility.
• Internal core is made up of fats and triglycerides,
stabilized : o/w emulsion, addition of high
2.Emulsome concentration of lecithin.
• Characteristics of both liposomes and emulsions.
s • Solidified or semi solidified internal oily core :
better opportunity to load lipophilic drugs in high
concentration.
• Enhanced drug delivery.
• Improved preclinical efficacy for oral route.
• Doxurubicin
• Proteins like enzymes :delivered through
several approaches. Like polymeric carriers;
aqueous space of lipid and bilayered vesicles.
• But delivery by attachment on surface of
liposomes has shown the prominent response
for the development of antibodies at the target
3. site.
Enzymosomes • Enzymes upon complexing with lipids :
enzymosomes.
• developed with long circulation time in the
blood.
• Accumulate at inflammed target sites.
• Maintaining enzymatic activity in its intact form
• Developed for delivering the drugs having low
penetration power through skin.
• Soft lipid vesicles : size range from tens of nanometers to
microns.
• containing phospholipids, alcohol : high concentration
and water.
• Better skin permeation ability.
4.Ethosomes • Surface negative net charge to ethosomes due to which
size of vesicles decreases.
• Used for delivery of various antifungal agents, antiviral
agents.
• Pharmacological efficacy in drug targeting : transdermal
and dermal sites for the treatment of various skin
diseases.
• Minoxidil, Acyclovir
• Liposomal derivative.
• More stable than other lipidic particles.
• composed mainly of charged
5.Cochleates phosphatidylserine.
• no internal aqueous space .
• Amphotericin B, F VIII, proteins, peptides &
DNA 17 .
Structure
Mode of
Action
VESICULAR DRUG
DELIVERY CARRIERS
ATTIYA NAJEEB ABBASI
(06331513040)
SPHINGOSOMES
• Sphingosomes can be defined as colloidal, concentric bilayered vesicles where
aqueous compartment is entirely enclosed by a bilayer membrane, mainly
composed of natural or synthetic sphingolipids
COMPOSITION
• Sphingosomes consist of sphingolipid (sphingomyelin) and cholesterol
• The major sphingolipids that have been used in the formulation of sphingosomes
include Sphinganines, Hexadecasphinganine, Lysosphingomyelins, and
lysoglycosphingolipids,Gangliosides,
ADVANTAGES OF • Toxicity of the encapsulated drug
SPHINGOSOMES is reduced.
• Sphingosomes have better drug DISADVANTAGES OF
retention characteristics SPHINGOSOMES
• Sphingosomes increase efficacy • Since sphingolipids are
and therapeutic index of the expensive, sphingosomes are not
encapsulated drug. economic.
• Stability is increased via • Sphingosomes have poor
encapsulation. entrapment efficiency.
IMPORTANCE
Sphingosomes is more stable than the phospholipid liposome because of the
following.
• Sphingolipid are built up by only amide and ether linkage. They are more resistant
to hydrolysis than ester linkage of lecithin.
• They also contain a smaller amount of double bonds then lecithin and thus less
subjected to rancidity.
TRANSFEROSOMES
• Transfersomes can be defined as ultra deformable, stress responsive, complex
vesicles possessing an aqueous core surrounded by complex bilayer of lipids.
• These artificial vesicles are composed of one natural amphiphilic lipid and are
supplemented by a bilayer softener, that is, biocompatible surfactant (e.g., sodium
cholate, span 80, and tween 80).
• Presence of amphiphilic surfactants allows transfersomes to modify their
membrane composition reversibly so as to penetrate through narrow skin pores
STRUCTURE
ADVANTAGES OF DISADVANTAGES OF
TRANSFERSOMES TRANSFERSOMES
• They are so deformable that they can • They are chemically unstable.
penetrate even through the narrow
pores of skin without measurable loss. • Purity of phospholipids is another
important criterion to be considered.
• Both low and high molecular weight
drugs can be entrapped efficiently. • They are expensive.
• They protect the encapsulated drug
from enzymatic, metabolic
degradation.
• They can act as a depot formulation to
release the contained drug in controlled
manner.
PHARMACOSOMES
• Pharmacosomes are novel vesicular drug delivery systems having unique advantages over
other drug delivery systems .
• Provides maximum entrapment efficiency.
• The three main components for the preparation of pharmacosomes are : drug, solvent
and lipid.
• Drug should contain active hydrogen atom , esterified with lipid and form amphiphilic
complexes, which facilitate membrane transfer.
• Pharmacosomes provide an efficient method for delivery of drug directly to the site of
infection, leading to reduction of drug toxicity with no adverse effects.
• Also reduces the cost of therapy by improved bioavailability of medication, especially in
case of poorly soluble drugs
• Pharmacosomes are suitable for incorporating both hydrophilic and lipophilic drugs.
STRUCTURE
VIROSOMES
• Reconstituted viral envelopes .
• Lipid bilayer , inserted viral glycoproteins.
• Different enveloped viruses.
• Liposomes with influenza virus hemagglutinin (HA) and
neuraminidase (NA) spikes on their surface.
• Retain the cell entry and membrane fusion.
Use:
• vaccination for the efficient induction of antibody responses against
the virus they are derived from .
STRUCTURE
CUBOSOMES
• Cubosomes are bicontinuous cubic phase liquid crystals have many
properties that make them appealing as a universal vehicle for drug
delivery.
• Cubosomes are nanoparticles, more accurately nanostructure particles,
or self-assembled liquid crystalline particles with a solid-like rheology.
• Bicontinuous cubic liquid crystalline phase is an optically clear, very
viscous material that has a unique structure at the nanometer scale.
IMPORTANCE
• Cubosomes are capable of loading lipophilic, hydrophilic, and
amphiphilic drugs.
• Because of the three-dimensional nanostructure with hydrophobic and
hydrophilic domains, cubic liquid crystalline phases have been applied
in pharmaceutical drug delivery.
• The large interfacial area can provide a complex diffusion pathway for
sustained release of entrapped drug molecules, whereas lipid
constituents are biocompatible, bio adhesive, and digestible.
Released Erythrocytes,Dendrimers and Non-
Lipid Bio carrier for Site Specific Targeting
Definition
Such drug-loaded carrier erythrocytes are prepared simply by collecting blood samples from the
organism of interest, separating erythrocytes from plasma, entrapping drug in the erythrocytes,
and resealing the resultant cellular carriers. Hence, these carriers are called resealed erythrocytes.
Properties of Resealed Erythrocyte as Novel Drug Delivery Carriers
1. The drug should be released at target site in a controlled manner.
2. It should be biocompatible and should have minimum toxic effect.
3. It should possess specific physicochemical properties by which desired target size could be
recognized.
4. The degradation product of the carriers system, after release of the drug at the selected site
should be biocompatible. It should be physico-chemically compatible with drug.
5. The carrier system should have an appreciable stability during storage.
Advantages
1) Bio-degradable, biocompatible, posses long circulation t1/2
2) Entrapment of drug does not require the chemical modification
3) Prolong the systemic activity of drug
4) Larger amount of drug can be encapsulated
Disadvantage
1) Limited as carrier to non-phagocyte target tissue
2) Clumping of cells and dose dumping 36
7.Dendrimers
1.Niosomes
Niosomes are lamellar structures that are microscopic in size. They constitute of
non-ionic surfactant of the alkyl or dialkyl polyglycerol ether class and cholesterol
with subsequent hydration in aqueous media.
Advantages of Niosomes
1. Niosomes are osmotically active, chemically stable and have long storage time compared to liposomes.
2. Their surface formation and modification is very easy because of the functional groups on their
hydrophilic heads.
3. They have high compatibility with biological systems and low toxicity because of their non-ionic nature.
4. They are biodegradable and non-immunogenic.
5. They can entrap lipophilic drugs into vesicular bilayer membranes and hydrophilic drugs in aqueous
compartments.
6. They can improve the therapeutic performance of the drug molecules by protecting the drug from
biological environment, resulting in better availability and controlled drug delivery by restricting the
drug effects to target cells in targeted carriers and delaying clearance from the circulation in sustained
drug delivery.
7. Access to raw materials is convenient.
Method of Preparation of Noisome
2.Bilosomes
• Bilosomes are specialised delivery vehicles which protect vaccines from being broken down in the
stomach, thereby enabling the oral delivery of vaccines as an alternative to administering
treatment by injection.
• They consist of deoxycholic acid incorporated into the membrane of niosomes .
• Bile salts are commonly used as penetration enhancers by the pharmaceutical industry and
promote oral bio-availability.
Benefits
1. Bilosomes allow small quantities of antigen to be effective and also increase the efficacy
of antigen which are weak when injected.
2. Bilosomes do not require the use of live pathogens, making them a safe and effective
alternative to traditional vaccines.
3. This non-invasive system offers advantages in terms of user acceptance and compliance.
4. The conventional injection method suffers from high relative costs and requires trained
persons to administer the treatment.
5. Less toxicity envelope suitable for a wide range of therapeutic agents.
6. Immune response could be manipulated through control of the size of the carrying
vesicle.
3.Aquasomes
Nanoemulsions
CERAMIC NANOPARTICLES
• Ceramic nanoparticles are particles fabricated from
inorganic compounds with porous characteristics such as
silica, alumina and titania
• Their sizes are less than 100nm and are able to avoid
uptake by the reticulo-endothelial system as foreign bodies.
• Entrapped molecules such as drugs, proteins and enzymes
are protected from denaturation at physiological pH and
temperature as neither swelling nor change in porosity
occurs
• They are effective in delivering proteins and genes.
• However, these particles are not biodegradable and so
there is concern that they may accumulate in the body and
cause harmful effects
NANOTUBES
• Nanotubes are hollow cylinders made of carbon atoms. They can also be filled
and sealed, forming test tubes or potential drug delivery devices.
Carbon Nanotubes
• Circulates well within the body (covalent or non covalent bonding)
• Enter readily into the cells.
• To deliver prodrugs to cancer cells eg. Cisplatin
• No significant toxicity in body fluids
Carbon nanotubes’ unique properties including low cytotoxicity and good
biocompatibility attract their use as vector system in target delivery of drugs,
proteins and genes. However, toxicity of carbon nanotubes is of concern.
Carbon nanotubes may cause inflammatory and fibrotic reactions.
BUCKY BALLS (BUCKMINISTERFULLERENE)
“Buckyball” is the common name for a molecule called Buckminsterfullerene, which is made of 60 carbon atoms
formed in the shape of a hollow ball.
PROPERTIES:
• Extremely stable & withstand high temperature
• Unlike other molecules that have applications as cancer drug delivery vehicles, fullerenes don't break down in
the body and are excreted intact and hence useful for radioactive atoms inside.
USES:
• Drug delivery vehicles for cancer therapy
• Bucky ball- Antibody combination - delivers antitumor drugs.
• To fight allergy.
• As powerful antioxidants and also
• Inhibitor of HIV.
DEMERITS:
• Hurt Cells
• Have High Potential To Accumulate In Living Tissue
• Difficulty of targeting drug delivery to the location
ISSUES/DRAWBACKS
1) Potential toxicity – major concern (NPs can cross biological membranes)
2) Surface interactions -- become ineffective
3) Specific issues: In Cancer Rx,
NPs cannot extend upto core of tumor
↓
aggregates at periphery
↓
Does not fully eliminate tumor
4) Degradation by lysosomes
5) NPs cause platelet aggregation
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