The document discusses drug targeting and targeted drug delivery systems. It defines drug targeting as delivering a drug only to its site of action and not to non-target organs, tissues, or cells. It discusses various types, approaches, and levels of drug targeting. It also discusses factors that affect drug targeting and various targeted drug delivery systems including prodrugs, liposomes, niosomes, nanoparticles, and microparticles.
Brief description of targeted drug delivery system, along with its concept and strategies for drug targeting. Advantages and disadvantages of drug targeting
Need for drug targeting.
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
Liposomes-Classification, methods of preparation and application Vijay Hemmadi
liposome preparation and application
A liposome is a tiny bubble (vesicle), made out of the same material as a cell membrane. Liposomes can be filled with drugs, and used to deliver drugs for cancer and other diseases. Membranes are usually made of phospholipids, which are molecules that have a head group and a tail group
Brief description of targeted drug delivery system, along with its concept and strategies for drug targeting. Advantages and disadvantages of drug targeting
Need for drug targeting.
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
Liposomes-Classification, methods of preparation and application Vijay Hemmadi
liposome preparation and application
A liposome is a tiny bubble (vesicle), made out of the same material as a cell membrane. Liposomes can be filled with drugs, and used to deliver drugs for cancer and other diseases. Membranes are usually made of phospholipids, which are molecules that have a head group and a tail group
Introduction
Structure
Niosomes Vs. Liposome
Advantages & Disadvantages
Properties of Niosomes
Method of Manufacturing
Evaluation of Niosomes
Applications
Marketed products
“It is define has an substance or Pharmaceutical material is encapsulated over the surface of solid, droplet of liquid and dispersion of medium is known has Microencapsulation”
Various approaches to Targeted Drug Delivery Systems (TDDS) in its formuation and evaluation in a pharmaceutical industry and research is outlined in this presentation.
Easy & to the point Topics are clearly given in this presentation..
Thanks & Best Regard
(Anurag Pandey) B.Pharm
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail both)
This will provide you the introduction about the tumor, its Anatomy & Physiology,How they are monitored?, Classification and grades of tumor, Tumor Targeting Techniques, strategies and Principles. Also provide you some examples of Marketed products.
Liposomes, Structure of liposome, phospholipids, classification of liposomes, method of preparation of liposomes, mechanism of liposome formation, application of liposomes.
Introduction
Structure
Niosomes Vs. Liposome
Advantages & Disadvantages
Properties of Niosomes
Method of Manufacturing
Evaluation of Niosomes
Applications
Marketed products
“It is define has an substance or Pharmaceutical material is encapsulated over the surface of solid, droplet of liquid and dispersion of medium is known has Microencapsulation”
Various approaches to Targeted Drug Delivery Systems (TDDS) in its formuation and evaluation in a pharmaceutical industry and research is outlined in this presentation.
Easy & to the point Topics are clearly given in this presentation..
Thanks & Best Regard
(Anurag Pandey) B.Pharm
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail both)
This will provide you the introduction about the tumor, its Anatomy & Physiology,How they are monitored?, Classification and grades of tumor, Tumor Targeting Techniques, strategies and Principles. Also provide you some examples of Marketed products.
Liposomes, Structure of liposome, phospholipids, classification of liposomes, method of preparation of liposomes, mechanism of liposome formation, application of liposomes.
This presentation which highlights the various technology innovations and developments in targeted drug delivery as well as maps its applications in different therapeutic segments was presented at the Novel Drug Delivery Systems and Clinical Trial Management 2013 Conference at Shangai, China.
After the manufacturing of the drug, it is essential that these should be stored properly. The stability of drug during it’s storage depend on so many factor and proper packaging is one of them. The pharmaceutical products are in direct contact with the container and closures. So improper packaging and poor quality of container may lead to deterioration of the product.
Sustained release, are terms used to identify drug delivery system that are designed to achieve a prolonged therapeutic effect by continuously releasing medication over an extended period of time after administration of a single dose.
Sustained release dosage forms provide an
amount of drug initially made available to the body
to cause the desired therapeutic response, followed
by a constant release of medication for maintenance
of activity over a period of time
Chitosan (2-amino-2deoxy-(1→4)-β-D-glucopyranan), a polyaminosaccharide, normally obtained by alkaline deacetylation of chitin is the principal component of living organisms such as fungi and crustacea.
Adv. biopharm. APPLICATION OF PHARMACOKINETICS : TARGETED DRUG DELIVERY SYSTEMSAkankshaAshtankar
MIP 201T & MPH 202T
ADVANCED BIOPHARMACEUTICS & PHARMACOKINETICS : UNIT 5
APPLICATION OF PHARMACOKINETICS : TARGETED DRUG DELIVERY SYSTEMS By - AKANKSHA ASHTANKAR
Implants- B.Pharm SEM 7- Novel Drug Delivery Systemvedanshu malviya
Implantable drug delivery device classification is not a straightforward task as there are a number of complex implants that will fall into hybrid categories. Nevertheless, implantable drug delivery devices can be broadly classified in two main groups: passive implants and active implants. The first group includes two main types of implants: biodegradable and non-biodegradable implants. On the other hand, active systems rely on energy dependent methods that provide the driving force to control drug release. The second group includes devices such as osmotic pressure gradients and electromechanical drives.
it is the study of factors influencing the rate and amount of drug that reaches the systemic circulation and the use of this information to optimize the therapeutic efficacy of the drug product.
It is the science of preparing, using, and administering drugs to living organisms or tissues
Metabolism (biotransformation): irreversible transformation of parent compounds into daughter metabolites.
Elimination ( Excretion): removal of the drug from the body and terminate it action.
Drug deposition- together they k/w as distribution and elimination
this is on pster format. thanks to Dr. Bankim Chandra Nandy for helping me out to make this..this is based information collected ..reference is given . thank you.
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The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
MANAGEMENT OF ATRIOVENTRICULAR CONDUCTION BLOCK.pdfJim Jacob Roy
Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
Ocular injury ppt Upendra pal optometrist upums saifai etawah
Drug targating
1. 11
Drug Targeting
Mr. Sagar Kishor savaleMr. Sagar Kishor savale
[[Department of Pharmaceutics]Department of Pharmaceutics]
avengersagar16@gmail.comavengersagar16@gmail.com
2015-0162015-016
Department of Pharmacy (Pharmaceutics) | Sagar savale
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2. 22
CONTENTSCONTENTS
Problems with CDDSProblems with CDDS
Drug TargetingDrug Targeting
Types of Drug TargetingTypes of Drug Targeting
Approaches of Drug TargetingApproaches of Drug Targeting
Levels of Drug TargetingLevels of Drug Targeting
Factors affecting Drug TargetingFactors affecting Drug Targeting
Targeted Drug Delivery SystemTargeted Drug Delivery System
Problems with TDDSProblems with TDDS
ReferencesReferences
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Problems Associated With Conventional DrugProblems Associated With Conventional Drug
Delivery SystemDelivery System
Difficulty in assessing diseased site (RA, Diseases of CNS,Difficulty in assessing diseased site (RA, Diseases of CNS,
Cancer, Interact able bacterial, fungal & parasitic infection)Cancer, Interact able bacterial, fungal & parasitic infection)
High dose & frequent administration of drugs leads to toxicHigh dose & frequent administration of drugs leads to toxic
manifestationmanifestation
Inappropriate pharmacodepositionInappropriate pharmacodeposition
Inactivation or decomposition of drug by GIT pH, by enzymesInactivation or decomposition of drug by GIT pH, by enzymes
which digest food , metabolism by microbial florawhich digest food , metabolism by microbial flora
In parentral route deactivation & metabolism of drug, doseIn parentral route deactivation & metabolism of drug, dose
related toxicity frequently observed.related toxicity frequently observed.
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Ideal Characteristics of Targeted Drug Delivery SystemIdeal Characteristics of Targeted Drug Delivery System
It should beIt should be
Biochemically Inert ( Non-toxic)Biochemically Inert ( Non-toxic)
NonimmunogenicNonimmunogenic
Physically & Chemically stablePhysically & Chemically stable in-vivoin-vivo && in-vitro.in-vitro.
The carrier must be biodegradable or readily eliminated fromThe carrier must be biodegradable or readily eliminated from
body without problemsbody without problems
Preparation of the delivery system must be reproducible, cost-Preparation of the delivery system must be reproducible, cost-
effective & simpleeffective & simple
Drug Targeting
Drug targeting means to deliver the drug only to its
site of action & not to the non-target organs, tissues or cells.
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5. 55
Rational for Targeted Drug DeliveryRational for Targeted Drug Delivery
SystemSystem
To supply drug selectively to its site of action to provideTo supply drug selectively to its site of action to provide
maximum therapeutic activitymaximum therapeutic activity
Preventing degradation or inactivation of drugPreventing degradation or inactivation of drug
Prevention of inappropriate deposition of the drugPrevention of inappropriate deposition of the drug
For the drugs that have low therapeutic indexFor the drugs that have low therapeutic index
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Types of Drug TargetingTypes of Drug Targeting
First Order TargetingFirst Order Targeting
It involves the delivery of a drug to specific organ or a tissueIt involves the delivery of a drug to specific organ or a tissue
Second Order TargetingSecond Order Targeting
It involves targeting towards the specific cell type within theIt involves targeting towards the specific cell type within the
tissue or organ (e.g. Tumor cells Vs Normal cell)tissue or organ (e.g. Tumor cells Vs Normal cell)
Third Order TargetingThird Order Targeting
It involves a delivery to a specific intracellular compartment inIt involves a delivery to a specific intracellular compartment in
the target cell ( e.g. Lysosomes)the target cell ( e.g. Lysosomes)
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Approaches of Drug TargetingApproaches of Drug Targeting
First ApproachFirst Approach
It involves the use of biologically active agents that areIt involves the use of biologically active agents that are
both potent & selective to a particular site in the bodyboth potent & selective to a particular site in the body
((Magic Bullet Approach of EhrlichMagic Bullet Approach of Ehrlich))
Second ApproachSecond Approach
It involves the preparation of pharmacologically inertIt involves the preparation of pharmacologically inert
form of active drugs, which upon reaching the active sitesform of active drugs, which upon reaching the active sites
becomes activated by a chemical or enzymatic reactionbecomes activated by a chemical or enzymatic reaction
(( Prodrug ApproachProdrug Approach))
Third ApproachThird Approach
Biologically inert macromolecular carrier system thatBiologically inert macromolecular carrier system that
directs a drug to a specific site in the body where it isdirects a drug to a specific site in the body where it is
accumulated & shows its effect (accumulated & shows its effect ( Magic Gun or MissileMagic Gun or Missile
Approach)Approach)
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Levels of Drug TargetingLevels of Drug Targeting
Followings are the levels of drug targetingFollowings are the levels of drug targeting
Passive TargetingPassive Targeting
Inverse TargetingInverse Targeting
Active Targeting ( Ligand Mediated Targeting & PhysicalActive Targeting ( Ligand Mediated Targeting & Physical
Targeting )Targeting )
Dual TargetingDual Targeting
Double TargetingDouble Targeting
Combination TargetingCombination Targeting
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Passive Targeting
Means targeting occurs because of the body’s natural
response to the physicochemical characteristics of the drug or drug
carrier system
e.g.
The ability of some colloids to be taken up by the RES
specially in the liver & spleen
Inverse Targeting
These process involves the reversion of the biodistribution
trend of the carrier & hence the process is referred as inverse
targeting
e.g.
Suppression of the RES by the pre-injection of the large
amount of blank colloidal carriers which leads to impairment of the
host defense system.
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Active Targeting
The facilitation of the binding of the drug-carrier to target
cells through the use of ligands or engineered homing devices to
increase receptor mediated localization of the drug & target specific
delivery of drug is referred as active targeting.
.
Active Targeting
Ligand Mediated
Targeting
Physical
Targeting
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Ligand Mediated Targeting
Here the carrier for the drug is made specific for the certain cell
or group of cells by incorporating ligands such as antibody, polypeptide,
oligosaccharides etc. on the surface of the carrier.
e.g.
apoprotein coat serves as ligand for the LDL receptors
Physical Targeting
In this mode of targeting ,some characteristics of the
bioenvironment are used either to direct the carrier to particular
location or to cause selective release of its content.
e.g.
Application of the external magnetic stimuli has been
suggested for the localization of the magno-responsive liposomes and
microspheres within a preselective capillary bed.
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Dual Targeting
This classical approach of the drug targeting employs, carrier
molecules which have their own intrinsic anti-viral effect thus
synergies the anti-viral effect of the loaded active drug.
Double Targeting
In this mechanism spatial targeting is combined with temporal
control release .
Sustain release
Stimuli Responsive Release
Self-regulating Release
Active Targeting
Passive Targeting
Double
Targeting
Controlled
Release of Drug
Drug
Targeting
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13. 1313
e.g.
PEG coated liposomes (for selective release of drug in
low pH medium) attached with MAb (for targeting specific
target like tumor)
Combination Targeting
These targeting systems are equipped with carriers,
polymers & homing devices of molecular specificity that could
provide a direct approach to the target site.
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Factors affecting the Drug TargetingFactors affecting the Drug Targeting
Cellular Uptake & ProcessingCellular Uptake & Processing
OpsonizationOpsonization
Phagocytosis carried out specialized cells of mononuclearPhagocytosis carried out specialized cells of mononuclear
phagocyte system mediated by absorption of specific bloodphagocyte system mediated by absorption of specific blood
components (opsonins) is called as opsonization.components (opsonins) is called as opsonization.
Affected ByAffected By: Hydrophilic property of carrier system,: Hydrophilic property of carrier system,
Its molecular weight, size & conc. in extra-vascularIts molecular weight, size & conc. in extra-vascular
fluidfluid
Transport Across the Epithelial BarrierTransport Across the Epithelial Barrier
Affected ByAffected By: pH of the site, enzymes present, surface area of target,: pH of the site, enzymes present, surface area of target,
segment length, microbial flora, transit timesegment length, microbial flora, transit time
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Extravasation
In many diseases drugs have to egress from the central
circulation & interact with its extra vascular-extracellular or extra
vascular-intracellular targets .This process of transvascular exchange
is called as extravasation.
Affected By: permeability of the blood capillary walls, rate & flow of
blood supply, physiochemical factors of the compound,
presences of the anionic sites on the endothelium etc.
Lymphatic Uptake
Following extravasation, drug molecules either reabsorbed
into the blood circulation or into lymphatic system & then return with
lymph into blood circulation. This process is known as Lymphatic
Uptake.
Affected By: size & surface characteristics of the particles,
formulation medium, composition & pH of the
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16. 1616
Targeted Drug Delivery
System
Prodrugs Drug-Carrier Delivery
System
Liposomes
Niosomes
Nanoparticles
Microparticles
Erythrocytes
Neutrophills
Specialized Emulsions
Virosomes
ADPET
Polymeric Prodrugs
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ProdrugsProdrugs
ConceptConcept ::
Chemically modification of the drug, which followingChemically modification of the drug, which following
administration in side the body under go suitable changes yieldingadministration in side the body under go suitable changes yielding
active principles at the target site in the body compartmentactive principles at the target site in the body compartment
avoiding unnecessary exposure of drugs to the other parts of theavoiding unnecessary exposure of drugs to the other parts of the
body.body.
e.g.e.g.
Delivery of L-Dopa (precursor of dopamine) to brain, inDelivery of L-Dopa (precursor of dopamine) to brain, in
the corpus striatum converted to dopamine by an enzyme aromaticthe corpus striatum converted to dopamine by an enzyme aromatic
amino acid decarboxylaseamino acid decarboxylase
A prodrug is pharmacologically inertA prodrug is pharmacologically inert
form of an active drug that undergoform of an active drug that undergo
transformation to the parent compound intransformation to the parent compound in
vivo either by a chemical or an enzymaticvivo either by a chemical or an enzymatic
reaction to exert its therapeutic effects.reaction to exert its therapeutic effects.
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Drug-Carrier Delivery
Systems
Drug Carriers
Carrier is the one of the most important entities
essentially required for the successful transport of the
loaded drug(s). These are the drug vectors which
sequester, transport and retain drug en route, while elute or
delivery it within or in the vicinity of target.
Ideal Features of Drug Carrier
Must be specific & selective for target cells
Must maintain avidity & identity of the surface ligands.
It must be able to cross the anatomical barriers & in case
of tumor, tumor vasculature.
Should be stable in plasma, interstitial & other biofluids04/28/1604/28/16 Sagar SavaleSagar Savale
20. 2020
It should be non-toxic, non-immunogenic & biodegradable, & after
recognition, & internalization the carrier system should release the drug
moiety inside the target
The biomolecules used for carrier navigation & site recognition should
not be ubiquitous otherwise it may cross over the sites, defeating the
concept of targeting
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Liposomes are microscopic
vesicles composed of one or more lipid
bilayers, separated by water or
aqueous buffer compartments with a
diameter ranging from 80nm-10µm.
Liposomes
As a Carrier for Targeted Drug Delivery
Mainly used to target the organs like liver & spleen
prolonged circulating time & small size (easy for extravasation)
Magnetic liposomes
pH sensitive cationic liposomes & anionic liposomes
MAb can be easily incorporated on their surface
Ostearlylamylopectin coated liposomes specific for lung targeting
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Niosomes
Niosomes are essentially no n-ionic
surfactant based multi-lamellar or uni-
lamellar vesicles in which an aqueous
solution of solute is entirely enclosed by a
membrane resulted from the organization of
the surfactant molecules as a bilayers.
Niosomes are chemically more stable
compare to liposomes
As a Carrier for Targeted Drug Delivery System
carrier for drug delivery to the sites other than liver &
spleen.
e.g. Niosomes containing muramic acid
Like liposomes selectively taken up by liver & spleen
Immunoglobulin can be easily coated on the lipid surface
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Nanoparticles
As a Carrier for Targeted Drug Delivery System
polyoxyethylene coated nanoparticles
Polysorbate 80 coated nanoparticles for drug delivery to brain
transferrin coated gelatin nanoparticles
for targeting the lymph nodes
easily cross the vasculature of the tumor cells
Nanoparticles include the
colloidal particles ranging in size
from 10-1000nm.
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24. 2424
Microparticles
Microparticles
include particles larger than 1µm
but small enough not to sediment
when suspended in water & larger
enough to scatter the incoming
light.
As a Carrier for Targeted Drug Delivery System
For targeting inflammatory bowels
To target specific blood cells.
Magnetic microspheres for delivery of radiopharmaceuticals
MAb can be easily attached
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Virosomes
Virosomes are
reconstituted influenza virus
envelopes. The membrane of these
vesicles consists of a spherical,
unilamellar lipid bilayer. Purified
influenza envelope glycoproteins are
inserted into the lipid bilayer. The
mean diameter of the vesicles is in
the range of 120 - 180 nm.
As a Carrier for Targeted Drug Delivery System
Can be easily conjugated to the antibody against
the antigen present on the tumor cells.
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Specialized Emulsions
Emulsions are the dispersion of one liquid
inside the other liquid
As a Carrier for Targeted Drug Delivery System
For liver targeting
Polyoxyethylene as an emulsifier
Conjugating antibodies to the distal end of
polyoxyethylene
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27. 2727
Released RBCs
The membrane of
RBCs can be temporarily broken by
changing tonicity or applying current
to load drug inside them & this can
be repair to gate intact RBCs. These
RBCs can be used as targeted drug
delivery
As a Carrier for Targeted Drug Delivery System
In liver cancer tumors, in Gaucher’s disease, in case of
iron overload
Magnetic RBCs04/28/1604/28/16 Sagar SavaleSagar Savale
28. 2828
Neutrophills
Neutrophills are one of
the WBCs present inside the
blood.
As a Carrier for Targeted Drug Delivery System
Mainly in the pyrogenic diseases like acute arthritis,
ulcerative colitis
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Problems Associated With Targeted DrugProblems Associated With Targeted Drug
Delivery SystemDelivery System
Rapid clearance of targeted systemsRapid clearance of targeted systems
Immune reactions against i.v. administered carrier systemImmune reactions against i.v. administered carrier system
Target tissue heterogeneityTarget tissue heterogeneity
Problems of insufficient localization of targeted systems intoProblems of insufficient localization of targeted systems into
tumor cellstumor cells
Down regulation & slugging of surface epitopesDown regulation & slugging of surface epitopes
Diffusion & redistribution of released drug leading to non-Diffusion & redistribution of released drug leading to non-
specific accumulationspecific accumulation
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REFERENCESREFERENCES
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Kulkarni J S, Pawar A P, Shedbalkar V P, BiopharmaceuticsKulkarni J S, Pawar A P, Shedbalkar V P, Biopharmaceutics
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Vyas S P, Khar R K, Targeted & controlled Drug DeliveryVyas S P, Khar R K, Targeted & controlled Drug Delivery
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delivery-systemdelivery-system
www.pathology.unibe.ch/.../virosomes/drug_tg.htmwww.pathology.unibe.ch/.../virosomes/drug_tg.htm
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