Nanomedicine Overview
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Questions and Answers

What can lead to toxicity due to nanoparticles in biological systems?

  • Protection against liver metabolism
  • Limited penetration of nanoparticles into tissues
  • Increased renal elimination of serum proteins
  • High accumulation in unintended organs (correct)

    • What is a potential effect of chronic exposure to silver nanoparticles?

  • Significant accumulation of DNA damage (correct)
  • Enhanced immune response
  • Reduction in vascular inflammation
  • Improved antioxidant status

    • What characterizes liposomes as a type of nanoparticle-based drug delivery system?

  • They can encapsulate both hydrophilic and hydrophobic substances. (correct)
  • They are porous and allow for large molecule transport.
  • They are solid lipid particles with high toxicity.
  • They can only deliver hydrophilic drugs.

    • Which of the following statements about nanoparticle biodistribution is true?

    <p>Major organ uptake of nanoparticles can lead to their elimination.</p> Signup and view all the answers

    What negative health effect is associated with exposure to diesel exhaust nanoparticles?

    <p>Increased systolic blood pressure</p> Signup and view all the answers

    What is a characteristic feature of polymer micelles?

    <p>Hydrophobic drugs are encapsulated in the hydrophobic core.</p> Signup and view all the answers

    Which statement is true regarding the structure of polymer vesicles?

    <p>They mimic natural phospholipids with a bilayer membrane structure.</p> Signup and view all the answers

    What are the primary advantages of dendrimers?

    <p>Easy surface functionalization and multiple binding sites.</p> Signup and view all the answers

    How do lipid-polymer hybrid nanoparticles enhance their biocompatibility?

    <p>Through a multilayered structure combining lipid and polymeric layers.</p> Signup and view all the answers

    What distinguishes dendrimers from other polymeric particles?

    <p>The existence of a branched structure with a core and branches.</p> Signup and view all the answers

    Which biocompatible substance is NOT commonly involved in the preparation of Solid-Lipid Nanoparticles (SLNs)?

    <p>Polymers</p> Signup and view all the answers

    Which of the following is NOT an advantage of Solid-Lipid Nanoparticles (SLNs)?

    <p>Enhanced bioavailability</p> Signup and view all the answers

    Which type of nanoemulsion allows for the interdispersion of both oil and water phases?

    <p>Bi-continuous/multiple emulsion</p> Signup and view all the answers

    What characteristic is common to Nanostructured Lipid Carriers (NLCs)?

    <p>Solid matrix at room temperature</p> Signup and view all the answers

    Which of the following correctly describes the structure of a nanoemulsion?

    <p>Dispersed system with ≤ 100nm droplets</p> Signup and view all the answers

    Which component of Solid-Lipid Nanoparticles (SLNs) contributes to high lipid content and facilitates encapsulation of poorly soluble drugs?

    <p>Fatty acids</p> Signup and view all the answers

    What process allows for the encapsulation of drugs like Abraxane within nanoemulsions?

    <p>Enhanced Permeability and Retention (EPR)</p> Signup and view all the answers

    Which of the following represents a key benefit of using SLNs in pharmaceutical formulations?

    <p>Effective release of drug</p> Signup and view all the answers

    Which characteristic is NOT associated with liposomes?

    <p>Typically larger than 1μm in size</p> Signup and view all the answers

    What is a major application of theranostic nanoparticles (NPs)?

    <p>Targeted drug delivery systems</p> Signup and view all the answers

    Which disadvantage is specifically mentioned regarding liposomes?

    <p>Fast clearance from the bloodstream</p> Signup and view all the answers

    What is the primary function of cytarabine in Vyxeos therapy?

    <p>Inhibition of DNA synthesis</p> Signup and view all the answers

    Which generation of liposomes is designed to improve drug loading and release profiles?

    <p>Third generation</p> Signup and view all the answers

    Which of the following factors is NOT a consideration when choosing nanotechnology for drug delivery?

    <p>Therapeutic efficacy of the drug used</p> Signup and view all the answers

    What is the Enhanced Permeability and Retention (EPR) effect primarily responsible for?

    <p>Driving drug accumulation in tumor tissues</p> Signup and view all the answers

    What type of nanoparticles consist of solid lipids at room temperature dispersed in water?

    <p>Solid-lipid nanoparticles (SLNs)</p> Signup and view all the answers

    Which of the following is a challenge associated with the use of nanoparticles for drug delivery?

    <p>Lack of specific regulations</p> Signup and view all the answers

    What is a primary advantage of using liposomes as drug carriers?

    <p>Simple modification and targeting potential</p> Signup and view all the answers

    Which liposomal formulation is specifically noted for its use in treating hematological malignancies?

    <p>Marqibo</p> Signup and view all the answers

    What mechanism allows nanoparticles to effectively target tumor tissues?

    <p>Utilizing passive mechanisms of the EPR effect</p> Signup and view all the answers

    Which of the following nanoparticle types are mentioned as widely studied for drug delivery?

    <p>Liposomes, polymeric nanoparticles, and nanostructured lipid carriers</p> Signup and view all the answers

    How do liposomes facilitate drug delivery across the plasma membrane?

    <p>By mimicking the structure of human plasma membranes</p> Signup and view all the answers

    Which of the following is NOT a potential risk associated with the use of nanoparticles in drug delivery?

    <p>Increased drug potency</p> Signup and view all the answers

    What does the design process of nanoparticles for drug delivery typically involve?

    <p>Complex multi-step synthesis and standard purification methods</p> Signup and view all the answers

    What is a primary benefit of using nanoparticles in drug delivery?

    <p>They increase water solubility of poorly soluble drugs.</p> Signup and view all the answers

    What mechanism is utilized by nanoparticles for active targeting?

    <p>Attachment of target molecules.</p> Signup and view all the answers

    Which characteristic is NOT typical of nanoparticles?

    <p>Similar chemical properties to small-molecule drugs.</p> Signup and view all the answers

    What role do theranostic nanoparticles serve in medicine?

    <p>Combine treatment and monitoring of drug effects.</p> Signup and view all the answers

    What does the EPR effect in nanoparticle delivery refer to?

    <p>Enhanced permeability and retention in pathological tissues.</p> Signup and view all the answers

    How do nanoparticles assist in personalized medicine?

    <p>By distinguishing between pathological and normal tissues.</p> Signup and view all the answers

    What is a disadvantage associated with nanoparticle-based drug delivery systems?

    <p>They may have limited capacity for drug loading.</p> Signup and view all the answers

    Which factor is essential when choosing nanotechnology for drug delivery?

    <p>Physicochemical properties of the drugs and targets.</p> Signup and view all the answers

    In what way do NPs act as radiosensitizers?

    <p>By attenuating high-energy X-rays to enhance their effect.</p> Signup and view all the answers

    Which of the following is a typical characteristic of nanoparticle drug delivery systems?

    <p>Ability to incorporate multiple functions for therapy.</p> Signup and view all the answers

    Study Notes

    Nanomedicine Overview

    • Nanomedicine is a rapidly developing field focused on using nanoparticles for drug delivery, diagnosis, and therapy.
    • Nanomedicine has the potential to revolutionize personalized medicine and improve drug therapy.

    Learning Objectives

    • Understanding the basics of nanomedicine and its potential applications in drug delivery.
    • Describing the differences between different types of nanoparticle-based drug delivery systems.
    • Explaining the advantages and disadvantages of different types of nanoparticle-based drug delivery systems.
    • Understanding the factors to consider when choosing nanotechnology for drug delivery.
    • Discussing the potential of nanomedicine for personalized medicine and the future of drug.

    Medicinal Chemistry

    • Physicochemical properties of drugs (FG, acidity/basicity, salt and solubility, chirality) are crucial in drug design.
    • Drug target interactions (enzyme/receptor) are important factors in understanding drug mechanism.
    • Drug discovery development and optimization (SAR, bioisosterism, rigidification)

    Nanoparticle Characteristics

    • Nanoparticles are smaller than traditional drugs.
    • Nanoparticles have distinctive physical and chemical properties compared to small molecule drugs.
    • Examples of nanoparticles include micelles, liposomes, dendrimers, gold nanoshells, quantum dots, and polymers.

    Advantages of Nanoparticles

    • High surface area-to-volume ratio for loading multiple drugs.
    • Improved drug accumulation at pathological tissues using targeting molecules (active targeting).
    • Enhanced permeability and retention (EPR) effect for passive targeting mechanism.
    • Increased water solubility of poorly water-soluble drugs for enhanced biocompatibility.
    • Multifunctional features to differentiate pathological tissue from normal tissue.
    • Contribution to personalized medicine.

    Nanocarrier Size & Types

    • Nanocarriers vary in size, with different types of nanocarriers having specific size ranges.
    • Examples of nanocarriers, including liposomes, solid lipid nanoparticles, polymer vesicles, and polymer nanoparticles, are listed.

    Nanomedicine Applications

    • Using nanoparticles to improve solubility and stability of poorly water-soluble drugs.
    • Nanoparticles acting as radiosensitizers to attenuate high-energy X-rays, thereby destroying pathological tissues.
    • Utilizing nanoparticles to deliver drugs to specific cells or organs (nanocarriers).
    • Theranostic nanoparticles for combining treatment and monitoring of treatment effectiveness.

    Liposomes

    • Composed of phospholipid bilayers, similar to biological membranes.
    • Encapsulate hydrophobic and hydrophilic drugs.
    • Vary in size from 20nm to 1µm.
    • Good biocompatibility and promote drug diffusion across the plasma membrane.
    • Carry hydrophilic and hydrophobic drugs.
    • Advantages are easy modification and targeting potential, ability to carry hydrophobic or hydrophilic drugs, and cost-effectiveness.
    • Disadvantages include reduced bioavailability, limited high drug loading for hydrophobic drugs, and fast clearance from the blood stream.

    Different Types of Liposomes

    • Different generations of liposomes utilize varying technologies for enhanced functionality and drug loading.
    • Some liposomes have stimuli responsive components to activate the release of the drug in specific environments.

    Drug Loading on Liposomes

    • Drug loading can occur through various mechanisms, such as mixing drugs and lipids, performing the encapsulation during liposome formation.
    • Remote loading uses pH and electrical potential differences to control drug loading.

    Solid-Lipid Nanoparticles (SLNs)

    • Colloidal carriers consisting of solid lipids at room temperature, dispersed in water or aqueous solution, containing surfactants.
    • Biocompatible substances like triglycerides, fatty acids, and steroids, prepare SLN systems.
    • Can be oraly administered, and available in different dosage forms.
    • Advantages of high drug loading capacity, stability of pharmaceuticals, easy manufacturing, and long-term stability.
    • They can encapsulate antitumor drugs and enhance drug solubility.

    Nanostructured Lipid Carriers (NLCs)

    • Solid matrix at room temperature.
    • Enhanced bioavailability, superior formulation properties, and increased drug loading.

    Nanoemulsions

    • Dispersed system with droplets less than 100nm.
    • Unique properties of small-sized droplets with high surface areas.
    • Three types: O/W, W/O, and bi-continuous/multiple emulsion (W/O/W and O/W/O).

    Examples of Nanoemulsions

    • Commercially available nanoemulsions include Abraxane (paclitaxel) and Diprivan (propofol).

    Polymer Micelles

    • Nanoparticles belonging to the nano colloid class formed by self-assembly of amphiphilic block copolymers in aqueous solution.
    • Hydrophobic drugs are encapsulated in the hydrophobic core, and the hydrophilic shell maintains particle stability.

    Polymer Vesicles

    • Vesicle membranes composed of special amphiphilic block copolymers, similar to natural phospholipids.
    • Hydrophobic segments of copolymers reduce contact with water, while hydrophilic domains are projected outwards.
    • Hydrophilic groups are distributed on the outer side of the membrane, typical of a bi-layer structure.
    • Encapsulation of hydrophobic substances and sub-encapsulation of hydrophilic groups in the water based core.

    Dendrimers

    • Highly branched polymer molecules.
    • Consist of a core (unit) and branches connected around the core.
    • Size ranges from 5-20 nm.
    • Advantages include high stability, ease of size control, and ease of surface functionalization.
    • Multiple sites for binding multiple drugs or targeting multiple drugs or targets

    Lipid-Polymer Hybrid Nanoparticles (LPHNs)

    • Multilayered particles with lipid and polymeric layers.
    • Exhibit high biocompatibility, loading efficiency, and stability.
    • Inner layers weakly bound by van der Waals forces.

    Multitherapy Nanoparticles

    • Contain two or more therapeutics to effectively treat diseases.
    • Example is Vyxeos, containing cytarabine and daunorubicin.

    Factors to Consider When Choosing Nanotechnology for Drug Delivery

    • Macromolecule loading efficiency must be considered given any potential issues with protein instability.
    • Production conditions should be mild to prevent protein instability.
    • Final properties of the nanosystems must be considered.
    • Liposomes, polymeric NPs, and nanostructured lipid carriers are widely used due to their potential for specific targeting.

    Enhanced Permeability and Retention (EPR) Effect

    • The driving force for nanocarrier delivery to tumor tissues.
    • Utilizes the passive mechanisms of EPR, which is a parameter crucial in nanocarrier design.
    • Pore size in endothelial walls determines nanoparticle entry.

    Nanoparticles for Active Targeting

    • Active targeting involves using ligands to bind to specific receptors on tumor cells, for enhanced delivery to tumor cells.
    • Useful in precision medicine.

    Controlled Release of Drugs from Nanoparticles

    • Methods for controlled drug release from nanoparticles.
    • Including diffusion-controlled, solvent-controlled.
    • Polymer degradation, hydrolytic cleavage.
    • Stimuli-sensitive destruction of diffusion barrier.

    Challenges of Using Nanoparticles

    • Lack of specific regulations for multi-step synthesis and production.
    • Lack of standard purification methods.
    • Difficulty in large-scale production.
    • High cost of production.
    • Potential toxicity and immunogenicity.
    • More efforts to approve and regulate nano-formulations for FDA and EMA approval.
    • High product price.

    Safety, Biodistribution, and Stability of Nanocarriers

    • Concerns of toxic effects and DNA damage; penetration of viable epidermal cells.
    • Biodistribution in unintended organs leading to toxicity, issues with liver metabolism, and limitations to renal elimination.
    • Some nanocarriers are efficient and safe to use in food or medicine.

    Toxic Effects of Nanoparticles

    • Hypersensitivity reactions associated with Alzheimer's disease and high magnetite concentrations.
    • Exposure to diesel exhaust (NP) can increase systolic blood pressure, vasodilation, and oxidative stress.
    • Chronic exposure to silver causes severe DNA damage.

    Take Home Message

    • Nanoparticle-based drug delivery systems offer advantages over small-molecule drugs.
    • Different types of nanoparticles have different advantages and disadvantages including liposomes, solid-lipid nanoparticles, nanoemulsions, polymeric nanoparticles, dendrimers, lipid-polymer hybrid nanoparticles.
    • Multitherapy nanoparticles treat diseases by combining two or more therapeutics.

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    Nanomedicine Lecture 27 PDF

    Description

    Explore the emerging field of nanomedicine, focusing on nanoparticles for drug delivery and therapy. This quiz covers the basics of nanotechnology, its applications in personalized medicine, and various drug delivery systems. Understand the physicochemical properties crucial in drug design and their implications in the future of medicine.

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