Drug targeting to particular organs
Download
1 / 50

Drug Targeting to Particular Organs - PowerPoint PPT Presentation


  • 83 Views
  • Uploaded on

Drug Targeting to Particular Organs. Prof. Dr. Basavaraj K. Nanjwade M. Pharm., Ph. D Department of Pharmaceutics KLE University College of Pharmacy, BELGAUM-590010, Karnataka, India. Cell No.: 0091-9742431000 E-mail: [email protected] CONTENT. Drug Delivery to respiratory system.

loader
I am the owner, or an agent authorized to act on behalf of the owner, of the copyrighted work described.
capcha
Download Presentation

PowerPoint Slideshow about ' Drug Targeting to Particular Organs' - daryl-wilcox


An Image/Link below is provided (as is) to download presentation

Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author.While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server.


- - - - - - - - - - - - - - - - - - - - - - - - - - E N D - - - - - - - - - - - - - - - - - - - - - - - - - -
Presentation Transcript
Drug targeting to particular organs

Drug Targeting to Particular Organs

Prof. Dr. Basavaraj K. NanjwadeM. Pharm., Ph. D

Department of Pharmaceutics

KLE University College of Pharmacy,

BELGAUM-590010, Karnataka, India.

Cell No.: 0091-9742431000

E-mail: [email protected]

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Content
CONTENT

  • Drug Delivery to respiratory system.

  • Problems of drug delivery to the brain and targeting to brain.

  • Drug delivery to Eye.

  • Drug targeting in Neoplastic diseases.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Targeting all respiratory system
Targeting all respiratory system

  • Dosing to the complete respiratory system has previously only been possible by special nebulizer.

  • Dosing to the complete respiratory system has only been regarded as an option for a very narrow range of therapeutics.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Pulmonary dose nasal dose
Pulmonary dose + Nasal dose

  • Delivery to both nasal and pulmonary airways, it will be possible to target the complete airway system.

  • Two separate formulation technologies for reaching nasal airways and for the pulmonary airways.

  • Nasal delivery and pulmonary delivery places each their requirements on the powder formulation characteristics.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Targeting lung regions
Targeting Lung Regions

  • Extrathoracic and alveolar regions can effectively be targeted with mono- and polydisperse aerosols respired steadily.

  • Effective targeting of the bronchial region can only be achieved with bolus inhalations.

  • When particles are suspended in a gas heavier than air, targeting the alveolar region can be enhanced.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Targeting lung regions1
Targeting Lung Regions

  • Optimization Particle and Breathing Parameters

  • Bolus Inhalation

  • Gas Composition

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Optimization particle and breathing parameters
Optimization Particle and Breathing Parameters

  • Targeting extrathoracic, upper bronchial, lower bronchial, and alveolar region for steady state breathing of aerosols.

  • The targeting efficiency can be increased for mono-as well as polydisperse aerosols to more than 90% by combining extrathoracic and upper bronchial regions and lower bronchial and alveolar regions.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Monodisperse particles
Monodisperse particles

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Mono and polydisperse particles
Mono and Polydisperse particles

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Targeting combined regions
Targeting Combined regions

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Bolus inhalation
Bolus Inhalation

  • Boluses are very suitable for targeting as long as the particle sizes and breathing patterns are used.

  • Particles 1 μm in size are ideal for this purpose because of their very low deposition on their way to the targeted region and their large deposition in the small peripheral lung structures during breath-holding.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Hydrophobic 1 m particles
Hydrophobic 1µm particles

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Gas composition
Gas Composition

  • The particle-loaded inhaled gas is heavier (lighter) than air, particles penetrate deeper (less deep) into the lungs.

  • Deposition occurs deeper in the lungs when particle-loaded sulphox rather than particle loaded heliox is inhaled.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Gas composition1
Gas composition

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Emerging carriers for respiratory drug delivery
Emerging Carriers for Respiratory Drug Delivery

  • Nanoparticle Formulations for Inhalation

  • Vaccine delivery

  • Gene therapy

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Targeted delivery to the respiratory system
Targeted delivery to the Respiratory System

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Liposomes as drug delivery systems to alveolar macrophage
Liposomes as drug delivery systems to alveolar macrophage

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Protein and peptide drugs to the respiratory system
Protein and Peptide Drugs to the Respiratory System

  • Improving the transport of the drug to its site of action

  • Improving the stability of the drug in vivo

  • Prolonging the residence time of the drug at its site of action by reducing clearance

  • Decreasing the nonspecific delivery of the drug to non-target tissues

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Protein and peptide drugs to the respiratory system1
Protein and Peptide Drugs to the Respiratory System

  • Decreasing irritation caused by the drug

  • Decreasing toxicity due to high initial doses of the drug

  • Altering the immunogenicity of the protein

  • Improving taste of the product

  • Improving shelf life of the product

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug targeting
Drug Targeting

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Avoiding injections
Avoiding injections

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Different types of targeting
Different Types of Targeting

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug delivery to brain
Drug Delivery to Brain

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Problems of drug delivery to the brain
Problems of Drug Delivery to the Brain

  • The relative impermeability of the BBB results from tight junctions between capillary endothelial cells which are formed by cell adhesion molecules.

  • Approximately 98% of the small molecules and nearly all large molecules (mwN1 kD, kilodaltons), such as recombinant proteins or gene-based medicines do not cross the BBB.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Blood brain barrier
Blood Brain Barrier

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug targeting to brain
Drug Targeting to Brain

  • To bypass the BBB and to deliver therapeutics into the brain, three different approaches are currently used.

  • Invasive approach

  • Pharmacological approach

  • Physiological approach

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug targeting in the brain areas
Drug Targeting in the Brain Areas

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Pharmacological approach
Pharmacological approach

  • Pharmacological approach consists of modifying, through medicinal chemistry, a molecule that is known to be active against a CNS target to enable it to penetrate the BBB.

  • Modification of drugs through a reduction in the relative number of polar groups increases the transfer of a drug across the BBB.

  • Lipid carriers have been used for transport.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Transport of molecules across the bbb
Transport of molecules across the BBB

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Pharmacological approach1
Pharmacological approach

  • Formulation of drugs facilitates brain delivery by increasing the drug solubility and stability in plasma

  • Limitations: The modifications necessary to cross the BBB often result in loss of the desired CNS activity. Increasing the lipophilicity of a molecule to improve transport can also result in making it a substrate for the efflux pump P-glycoprotein (P-gp).

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Physiological approach
Physiological approach

  • Physiological approach is recognized by the scientific community as the onewith the most likely chance of success.

  • Transporter-mediated delivery

  • Receptor-mediated transcytosis

  • Receptors at the blood–brain barrier

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Physiological approach1
Physiological approach

  • Transferrin receptor (TR)

  • Insulin receptor

  • Liposomes coated with targeting molecules such as antibodies, Trojan Horses Liposomes (THL)

  • Nanoparticles coated with transferrin or transferrin receptor antibodies

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Motivation
Motivation

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Blood brain barrier transport mechanism
Blood Brain Barrier Transport Mechanism

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug delivery to eye
Drug Delivery to Eye

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Anatomy of the eye
Anatomy of the Eye

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug delivery to eye1
Drug Delivery to Eye

  • Ophthalmic preparation

    • Applied topically to the cornea, or instilled in the space between the eyeball and lower eyelid

    • Solution

      • Dilutes with tear and wash away through lachrymal apparatus

      • Administer at frequent intervals

    • Suspension

      • Longer contact time

      • Irritation potential due to the particle size of drug

    • Ointment

      • Longer contact time and greater storage stability

      • Producing film over the eye and blurring vision

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug delivery to eye2
Drug Delivery to Eye

  • Emulsions

    • Prolonged release of drug from vehicle but blurred vision, patient non compliance and oil entrapment are the drawbacks.

  • Gels

    • Comfortable, less blurred vision but the drawbacks are matted eyelids and no rate control on diffusion.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Controlled delivery system

Release at a constant rate for a long time

Enhanced corneal absorption

Drug with not serious side effect or tolerate by the patient

Drug Delivery to Eye

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Advantages
Advantages

  • Increase ocular residence, hence, improving bioavailability.

  • Possibility of providing a prolonged drug release and thus a better efficacy.

  • Lower incidence of visual and systemic side effects.

  • Increased shelf life with respect to aqueous solutions.

  • Exclusion of preservatives, thus reducing the risk of sensitivity reactions

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Advantges
Advantges

  • Possibility of targeting internal ocular tissue through non-corneal routes

  • Reduction of systemic side effects and thus reduced adverse effects.

  • Reduction of the number of administration and thus better patient compliance.

  • Administration of an accurate dose in the eye, which is fully retained at the administration site, thus a better therapy.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Classification
Classification

  • Mucoadhesive dosage forms

  • Ocular inserts

  • Collagen shield

  • Drug presoaked hydrogel type contact lens

  • Ocular iontophoresis

  • Polymeric solutions

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Classification1
Classification

  • Ocular penetration enhancers

  • Phase transition systems

  • Particulate system like, microspheres and nanoparticles

  • Vesicular systems like liposomes, niosomes, phamacosomes and discosomes

  • Chemical delivery system for ocular drug targeting

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug delivery to eye3
Drug Delivery to Eye

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Drug targeting to neoplastic diseases
Drug targeting to Neoplastic Diseases

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Targeted delivery to tumors
Targeted Delivery to Tumors

  • Goal is to inject treatment far from tumor and have large accumulation in tumor and minimal accumulation in normal cells/organs.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Cancer treatments
Cancer Treatments

  • Tumor penetration is a key issue for successful chemotherapy

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Nanoparticle use in cancer treatments
Nanoparticle use in Cancer Treatments

  • Because of their small size, nanoparticles can pass through interstitial spaces between necrotic and quiescent cells.

  • Tumor cells typically have larger interstitial spaces than healthy cells

  • Particles collect in center bringing therapeutics to kill the tumor from inside out.

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Nanoparticle targeting and accumulation
Nanoparticle Targeting and Accumulation

  • To maximize their effectiveness, the microenvironment of the tumor must be quantified and vectors developed to specifically target the tumor.

Necrotic

Quiescent

Proliferating

Therapeutic

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


Thank You

E-mail: [email protected]

Cell No: 00919742431000

DDSEC, Prince of Songkla University, Hat Yai, Thailand.


ad