Transdermal Drug Delivery Systems Quiz

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Questions and Answers

What is the primary benefit of Transdermal Drug Delivery Systems (TDDDs) compared to traditional methods?

  • Reduced drug metabolism by the liver (correct)
  • Improved absorption in the gastrointestinal tract
  • Higher doses required for effective treatment
  • Increased side effects due to direct blood exposure

What is a primary characteristic of drug molecules suitable for transdermal delivery using chemical enhancers?

  • Molecular weight greater than 1 kDa
  • Affinity solely for lipophilic phases
  • Low molecular weight less than 1 kDa (correct)
  • High viscosity at skin temperature

Which therapeutic areas have significantly benefited from the use of TDDDs?

  • Dermatological treatments primarily
  • Antibiotic therapies exclusively
  • Pain management and hormonal therapy (correct)
  • Respiratory diseases only

Which of the following is NOT a type of vesicle used in transdermal drug delivery?

<p>Microsomes (C)</p> Signup and view all the answers

What role does the stratum corneum play in the function of TDDDs?

<p>Blocks external substances from entering the body (B)</p> Signup and view all the answers

How do thermal ablation techniques primarily achieve enhanced skin absorption?

<p>By increasing the temperature which alters skin diffusivity (B)</p> Signup and view all the answers

Which component is most commonly found in liposomes that aids in their structure and function?

<p>Phospholipids (D)</p> Signup and view all the answers

Why are TDDDs considered a noninvasive administration method?

<p>They involve minimal pain during drug application (C)</p> Signup and view all the answers

What is a significant limitation of TDDDs in their current use?

<p>The innate skin barrier preventing optimal delivery (A)</p> Signup and view all the answers

What key factor does NOT influence drug penetration through the skin?

<p>The color of the drug formulation (A)</p> Signup and view all the answers

Which layer of the skin is primarily responsible for protecting the body from external hazards?

<p>Epidermis (B)</p> Signup and view all the answers

In what way do TDDDs ensure a sustained therapeutic effect?

<p>By controlling drug release according to usage restrictions (D)</p> Signup and view all the answers

What is the main challenge posed by the barrier effect in transdermal drug delivery systems (TDDS)?

<p>The limited ability to deliver drugs to the target tissue (D)</p> Signup and view all the answers

Which pathway is primarily utilized for delivering substances with small molecular weights in TDDS?

<p>Intracellular pathway (B)</p> Signup and view all the answers

What type of therapeutic agents does iontophoresis utilize when applying positive voltage?

<p>Cationic therapeutic agents (D)</p> Signup and view all the answers

What is the effect of external stimuli on skin permeability in active transdermal delivery systems?

<p>They enhance the permeability of drugs and biomolecules (C)</p> Signup and view all the answers

What is a significant limitation for drug delivery through the stratum corneum in TDDS?

<p>The thickness of the epidermal layer (D)</p> Signup and view all the answers

What role does iontophoresis play in drug delivery?

<p>It enhances transdermal delivery using applied electrical current (B)</p> Signup and view all the answers

Which characteristic of the stratum corneum complicates transdermal drug delivery?

<p>It contains both hydrophilic and hydrophobic substances irregularly (B)</p> Signup and view all the answers

Which mode of TDDS is specifically designed to increase the rate and efficacy of drug delivery?

<p>Active transdermal delivery (C)</p> Signup and view all the answers

What current density is applied typically during iontophoresis to ensure effective drug delivery?

<p>0.5 mA/cm2 (C)</p> Signup and view all the answers

What characteristic of iontophoresis makes it less dependent on biological parameters compared to other drug delivery systems?

<p>Dependence on current (A)</p> Signup and view all the answers

Which ultrasound frequency range is most effective for enhancing transdermal drug delivery through sonophoresis?

<p>20 kHz to 16 MHz (C)</p> Signup and view all the answers

What is a common challenge associated with the use of sonophoresis for drug delivery?

<p>Device availability and optimization (B)</p> Signup and view all the answers

How does electroporation enhance drug delivery through the skin?

<p>By forming small pores in the stratum corneum (D)</p> Signup and view all the answers

Which of the following is crucial for effective drug transport via iontophoresis?

<p>Mobility of the drug molecule (A)</p> Signup and view all the answers

What type of drug is mentioned as being deliverable by sonophoresis, regardless of solubility?

<p>High molecular weight drugs such as insulin (C)</p> Signup and view all the answers

What is a physiological effect of ultrasonication in sonophoresis that aids drug penetration?

<p>Creation of thermal effects increasing skin temperature (A)</p> Signup and view all the answers

Which factor does NOT influence the efficacy of iontophoresis?

<p>Drug solubility (D)</p> Signup and view all the answers

What type of electric pulsing is typically used in electroporation?

<p>High voltage pulses ranging from 5 to 500 V (C)</p> Signup and view all the answers

What main effect do cavitation bubbles have during sonophoresis?

<p>They disturb skin layers, creating an aqueous path for the drug (A)</p> Signup and view all the answers

What is a primary disadvantage of electroporation in drug delivery?

<p>It can cause cell death and protein denaturation. (D)</p> Signup and view all the answers

How do dissolving microneedles facilitate drug delivery?

<p>They dissolve in the body, releasing drugs directly into the bloodstream. (C)</p> Signup and view all the answers

What temperature is required to effectively perform thermal ablation?

<p>Above 100 °C (D)</p> Signup and view all the answers

Which type of microneedles creates a physical pathway without releasing drugs?

<p>Solid microneedles (B)</p> Signup and view all the answers

What is the mechanism behind thermal ablation enhancing drug delivery?

<p>It generates microchannels through localized heating. (B)</p> Signup and view all the answers

What is one potential side effect associated with electroporation?

<p>Risk of infection at entry points (A)</p> Signup and view all the answers

Why is it important to control the thermal exposure during thermal ablation?

<p>To avoid damage to viable layers of skin. (C)</p> Signup and view all the answers

Which characteristic of microneedles helps avoid pain during drug delivery?

<p>Their small size and thin nature. (B)</p> Signup and view all the answers

What distinguishes drug-coated microneedles from solid microneedles?

<p>They release drugs as they enter the skin. (B)</p> Signup and view all the answers

What size are the micron-scale defects created by thermal ablation?

<p>About 50–100 μm in diameter (B)</p> Signup and view all the answers

Flashcards

Transdermal Drug Delivery System (TDDS)

A drug delivery system that uses the skin as a route of administration to deliver medication into the systemic circulation.

Transdermal Delivery

The process of delivering a drug through the intact skin to reach the systemic circulation for therapeutic effects.

Benefits of TDDS

TDDS offers a convenient and non-invasive way to administer medication, especially suitable for chronic conditions.

First-Pass Metabolism Bypass

TDDS bypasses the first-pass metabolism in the liver, leading to higher drug bioavailability.

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Controlled Drug Release

TDDS allows for controlled drug release over time, ensuring consistent therapeutic levels and reducing dosing frequency.

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Stratum Corneum Barrier

The skin's outermost layer, the stratum corneum, acts as a barrier to external substances, which can hinder the penetration of drugs.

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Skin Barrier Limitation

The natural barrier properties of the skin present a challenge for efficient drug delivery through TDDS.

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Iontophoresis

A method that uses an electrochemical potential gradient to deliver drugs through the skin.

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Factors Influencing Iontophoresis Efficacy

The effectiveness of iontophoresis depends on the properties of the drug, the electrical current, and the formulation.

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Sonophoresis

Ultrasound waves create temporary pores in the skin, allowing drugs to penetrate deeper.

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Ultrasound Frequency in Sonophoresis

The frequency of ultrasound waves used in sonophoresis affects its effectiveness.

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Coupler in Sonophoresis

A gel or cream that transmits ultrasound waves to the skin.

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Drug Versatility in Sonophoresis

Sonophoresis can deliver various drugs regardless of their properties, even large molecules.

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Electroporation

Short, high-voltage electric pulses create temporary pores in the skin for drug penetration.

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Electroporation Electrode Placement

Electroporation uses closely positioned electrodes to safely and painlessly deliver electric pulses.

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Sonophoresis Mechanism

The exact mechanism of sonophoresis is still under investigation.

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Sonophoresis Challenges

Sonophoresis has some limitations, including device availability and potential side effects.

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Barrier Effect in Transdermal Drug Delivery

The barrier effect is the difficulty of substances, especially those with large molecular weights, to penetrate the skin's outermost layer (stratum corneum). This barrier effect is mainly due to the complex structure and composition of the stratum corneum, which acts as a protective shield.

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What are Transdermal Drug Delivery Systems (TDDS)?

Transdermal drug delivery systems (TDDS) aim to deliver drugs through the skin to reach the bloodstream, bypassing the first-pass metabolism in the liver. This allows for controlled drug release and potentially higher bioavailability.

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Intracellular vs. Intercellular Pathway in TDDS

The intracellular pathway involves drug molecules entering the skin cells and moving through them. Conversely, the intercellular pathway involves molecules moving between skin cells, utilizing the spaces between them.

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Active Transdermal Delivery

Active transdermal delivery refers to using external stimuli like electrical, mechanical, or physical forces to enhance the penetration of drugs through the skin. This approach has been shown to improve delivery speed and effectiveness.

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What is Iontophoresis?

Iontophoresis is a method that uses a low voltage and low current to drive charged drug molecules into the skin, overcoming the skin barrier resistance and improving drug absorption.

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How does Iontophoresis work?

Iontophoresis works by creating a repulsive force between the charged drug molecules and the electrode, propelling them into the skin. This method has been found to enhance the penetration and absorption of several drugs, especially those with poor absorption profiles.

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Advantages of Active Transdermal Delivery

Unlike passive drug delivery, active methods like iontophoresis can increase the penetration of drugs through the skin, enhancing delivery speed and effectiveness. These methods offer targeted drug delivery with improved therapeutic benefits.

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Major Challenge in Transdermal Drug Delivery

The biggest challenge in developing transdermal drug delivery systems is overcoming the barrier effect posed by the stratum corneum. This barrier prevents effective penetration of drugs and limits the amount of drug reaching the target tissues.

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Why is the Stratum Corneum a Barrier?

The lipid-containing cells within the stratum corneum have a complex structure and composition that contributes to the barrier effect. This complexity, alongside the presence of both hydrophilic (water-loving) and hydrophobic (water-fearing) substances, makes for a tightly packed structure that hinders drug penetration.

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What is Thermal Ablation?

Thermal ablation is a technique that uses heat to remove tissue. It can be done with lasers or radiofrequency energy.

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How does Laser Thermal Ablation work?

Laser thermal ablation works by using laser light to create small holes and heat up the skin. This process causes water to vaporize and creates a more permeable skin surface.

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What is TDDS?

TDDS stands for Transdermal Drug Delivery System. This method uses your skin to deliver medications into your bloodstream. It's like a patch that sticks to your skin.

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What are Vesicles?

Vesicles are tiny sacs filled with water. These sacs can transport drugs across your skin, allowing them to enter your body.

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What are Liposomes?

Liposomes are a type of vesicle used for drug delivery. They are made of phospholipids, which are like tiny fatty molecules that create a sphere surrounding the drug.

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What is electroporation for drug delivery?

Electroporation is a technique that uses electric pulses to create temporary pores in cell membranes, allowing molecules to enter. It can deliver drugs to the skin, but it can also harm cells and has limited delivery capacity.

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What are microneedles used for?

Microneedles are tiny needles that puncture the skin, allowing drugs to be delivered directly into the bloodstream. They are a popular method for transdermal drug delivery because they avoid pain and are minimally invasive.

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What are solid microneedles?

A type of microneedle that acts like a physical channel, allowing drugs to be absorbed directly. Think of it like a mini-tunnel for drugs to get through the skin.

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What are drug-coated microneedles?

Microneedles can be coated with drugs, and they release the medication as they penetrate the skin. Think of it like a tiny pill that dissolves as it goes into the skin.

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What are dissolving microneedles?

These microneedles are made of drug formulations that dissolve in the body. Think of it like a tiny capsule that releases medication as it dissolves.

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What are microneedle patches?

Microneedle patches combine microneedles with a patch to create a more comprehensive drug delivery system. Imagine it like a patch with tiny needles, delivering medication to the body.

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What is thermal ablation in drug delivery?

Thermal ablation is a technique that uses heat to disrupt the stratum corneum layer of the skin. Think of it like using heat to create tiny channels for drugs to pass through.

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How is thermal ablation used for drug delivery?

Thermal ablation requires high heat to create channels in the skin, but only for a very short time to avoid harming the skin. Imagine using a laser to create tiny holes in the skin for a few seconds.

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What are the benefits of thermal ablation?

Thermal ablation creates small, localized defects in the skin, which are invisible to the naked eye and don't cause pain, bleeding, or infection. Think of it like creating microscopic holes that heal quickly.

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How does thermal ablation affect the skin?

Thermal ablation creates channels in the skin because the heat causes vaporization of keratin. Think of it like using a hairdryer to evaporate water on your skin, only on a much smaller scale.

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Study Notes

Transdermal Drug Delivery Systems (TDDDs)

  • TDDDs deliver drugs through intact skin to systemic circulation, beneficial post therapeutic dose.
  • Ideal for chronic treatment types.
  • Anti-diabetic agents are an example of drugs investigated for transdermal delivery.
  • Conventional DDS methods are compared to novel DDS approaches.

Drug Delivery Systems (DDS)

  • DDS is a general term for any physicochemical technology.
  • It involves controlling the delivery and release of pharmacologically active compounds to tissues or cells to achieve optimal effects.

Iontophoresis

  • One of the physical methods for drug delivery.
  • Cationic or neutral therapeutic agents are placed under an anode or anionic agents under a cathode.
  • A low voltage and low current density is applied for electro-repulsion to drive ions into and through the skin.
  • Iontophoresis promotes the transport of ions through the membrane.
  • An externally applied potential difference (less than 0.5 mA/cm²) is used.
  • Efficacy depends on the polarity, valency, and mobility of the drug, formulation, and the applied electrical cycle.
  • Drug absorption by iontophoresis is less-dependent on biological parameters.

Sonophoresis

  • Ultrasound frequencies improve transdermal drug delivery.
  • Low-frequency ultrasound is more effective, facilitating drug movement by creating aqueous pathways through cavitation.
  • The drug is mixed with a coupler (gel or cream) which transmits ultrasonic waves to the skin and disturbs the layers to create a path for the drug.
  • It increases drug penetration through passages created from the application of ultrasonic waves.
  • This increases the local temperature of the skin area.
  • The method is effective for various drugs irrespective of their solubility, dissociation, ionization constants and electrical properties.

Electroporation

  • Uses high-voltage electric pulses to create temporary pores in the stratum corneum (SC) of skin.
  • This improves permeability and aids drug diffusion.
  • Employing closely positioned electrodes avoids pain and is safe.
  • Effective for low and high molecular weight drugs, including antiangiogenic peptides, oligonucleotides and heparin.
  • Drawbacks include small delivery loads, cell death, heating-induced damage, and denaturation of proteins.

Microneedles

  • Micron-sized needles pierce superficial skin layer for drug diffusion.
  • Short and thin needles deliver drugs directly to blood capillaries for rapid absorption with minimal pain.
  • Solid microneedles create a physical path for drug absorption.
  • Drug-coated microneedles deliver drugs coated on needle surfaces.
  • Dissolvable microneedles are made of drug formulations for in-body dissolving.
  • Microneedle patches combine microneedles with patch designs.

Thermal Ablation (Thermophoresis)

  • Selectively disrupts stratum corneum by localized heat.
  • Creates micro-channels for enhanced drug delivery.
  • Requires high temperatures (above 100°C) for heating and vaporizing keratin.
  • Micron-scale defects (50-100 µm) are created for pain-free drug delivery.
  • Techniques include laser and radiofrequency methods depending on heat source.

TDDS Using Chemical Enhancers (Passive Delivery)

  • Drugs with low molecular weight (<1 kDa) and affinity for lipophilic/hydrophilic phases, short half-life and low skin irritation are ideal.
  • Many factors hinder drug penetration, including species, skin age/site, temperature, skin state, area/duration of application, pretreatment methods, and penetrant's physical characteristics.
  • Recent studies focus on innovative approaches (e.g chemical enhancers, super-strong formulations, microemulsions, and vesicles) to enhance skin penetration and solubility.

Vesicles

  • Colloidal particles filled with water consisting of amphiphilic molecules (bilayer arrangement).
  • Can carry water-soluble or fat-soluble drugs for transdermal absorption.
  • Under conditions of excess water, such amphiphilic molecules form concentric bilayers.
  • Types include liposomes, transfersomes and ethosomes, depending on the properties of the constituent substance.

Liposomes

  • Circular soft vesicles formed by one or more bi-layer membranes.
  • Consist of phospholipids (with or without cholesterol).
  • Phospholipid structure includes polar head groups and hydrophobic hydrocarbon chains.
  • Polar groups can be either positively or negatively charged.

Transfersomes

  • Deformable or highly flexible liposomes with added single-chain surfactants.
  • Enhanced elasticity and fluidity, enabling penetration of skin pores.
  • Can deliver drugs with high molecular weight (up to 1000 kDa).

Ethosomes

  • Composed of phospholipids, alcohols, and water.
  • Higher alcohol concentrations compared to liposomes.
  • Flexibility and fluidity increase as water molecules are replaced by alcohol near the lipid headgroup.
  • Stable structure, high capture efficiency to delay drug release.
  • Deeper penetration compared to typical liposomes.

Polymeric Nanoparticles

  • Nanocarriers ranging from 1-1000 nm.
  • Tailored to deliver drugs in targeted, controlled release, extended blood residence time.
  • Improves drug bioavailability and reduces toxicity with various types like nanospheres, nanocapsules, and polymer micelles.
  • Polylactic acid, poly(D,L-lactide-co-glycolide) (PLGA) are common examples.

Nanoemulsions

  • Class of emulsions with droplet sizes between 20 and 500 nm.
  • Exhibit excellent stability, tunable rheology, and exceptional properties.
  • Used in pharmaceutical formulations (topical, ocular, intravenous).

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