3.2: Topical Drug Delivery II

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Questions and Answers

What is a characteristic of hydrocarbon (oleaginous) bases in ointments?

  • They are primarily water-based.
  • They are greasy and insoluble in water. (correct)
  • They can easily absorb water.
  • They contain a high percentage of surfactants.

Which of the following statements accurately describes absorption bases?

  • They can absorb water due to surfactants. (correct)
  • They do not enhance drug delivery.
  • They are entirely water-soluble.
  • They form water-in-oil emulsions only in a dry environment.

What effect do hydrocarbon bases primarily have on skin contact?

  • They cause dehydration of the skin.
  • They provide a continuous, greasy, and water-repellent barrier. (correct)
  • They form a greasy but water-absorbent film.
  • They quickly evaporate, enhancing drug permeation.

Which of the following is considered an emulsion base in ointment formulations?

<p>Hydrous lanolin (A)</p> Signup and view all the answers

What is a common disadvantage of using ointments based on hydrocarbon bases?

<p>They tend to feel greasy and may stain clothing. (D)</p> Signup and view all the answers

Which of the following does NOT describe a property of absorption bases?

<p>Greasiness is absent. (C)</p> Signup and view all the answers

What distinguishes water-in-oil emulsions from other ointment bases?

<p>They contain oil as the external phase. (B)</p> Signup and view all the answers

What therapeutic effect do ointments generally provide when applied to the skin?

<p>They enhance drug permeation. (A)</p> Signup and view all the answers

What is the primary characteristic of lotions compared to other topical dosage forms?

<p>They have a continuous aqueous phase. (C)</p> Signup and view all the answers

What therapeutic effect do lotions provide upon application?

<p>They leave a thin film that cools and soothes the skin. (C)</p> Signup and view all the answers

What type of instability can lotions experience?

<p>Chemical, physical, and microbiological instability. (C)</p> Signup and view all the answers

In what form are active drugs typically found in gels?

<p>Suspended or dissolved in the liquid phase. (A)</p> Signup and view all the answers

What is a common property of gels in topical applications?

<p>They consist of a liquid phase trapped in a solid structure. (D)</p> Signup and view all the answers

Which of the following is NOT typically an example of a lotion?

<p>Iodine tincture. (C)</p> Signup and view all the answers

What type of vehicle do topical solutions typically use?

<p>Aqueous vehicles, sometimes with alcohol. (D)</p> Signup and view all the answers

Which statement about patient acceptance of lotions is accurate?

<p>Lotions are highly acceptable due to their ease of application. (B)</p> Signup and view all the answers

Which of the following polymers is used in gels but is not a polysaccharide?

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

What characteristic does a gel possess that aids in drug delivery?

<p>Porous matrix film (B)</p> Signup and view all the answers

Which of the following gels is designed specifically for joint pain relief?

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

What is a key advantage of using ethanol in gel formulations?

<p>It enhances drug penetration into the skin. (A)</p> Signup and view all the answers

Which of the following is a common application of collagen-based gels?

<p>Sealing small wounds (D)</p> Signup and view all the answers

Benzoyl peroxide gel is primarily used for which of the following conditions?

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

Which property is NOT typically associated with gelling polymers?

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

What is a notable difference between gels like hand sanitizer and gels used for acne treatment?

<p>Acne treatment gels contain antibiotics. (A)</p> Signup and view all the answers

What is a primary characteristic of Eucerin compared to anhydrous absorption bases?

<p>Moderately good emollient properties (C)</p> Signup and view all the answers

How do oil-in-water emulsion bases differ from water-in-oil emulsion bases regarding transepidermal water loss?

<p>They do not block transepidermal water loss (C)</p> Signup and view all the answers

Which of the following statements is true about water-soluble bases?

<p>They can be irritating to wounds (D)</p> Signup and view all the answers

What is a common therapeutic property of pastes used in dermatological applications?

<p>They absorb fluid and have high protective value (C)</p> Signup and view all the answers

What is the primary reason hydrophilic ointment is often referred to as vanishing cream?

<p>It evaporates, leaving a thin transparent film (D)</p> Signup and view all the answers

Which ingredient is commonly used in ointments classified as pastes?

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

What distinguishes water-washable bases from other formulations?

<p>They allow easy removal with water (C)</p> Signup and view all the answers

How do the protective properties of anhydrous absorption bases compare to those of Eucerin?

<p>Anhydrous bases are more protective than Eucerin (D)</p> Signup and view all the answers

What is the primary function of castor oil when added to pyroxylin?

<p>To soften the pyroxylin and ensure it remains in place. (C)</p> Signup and view all the answers

Which topical dosage form is specifically designed to be cut to fit the treatment area?

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

What type of topical dosage form allows for non-rubbing application, particularly useful for irritated areas?

<p>Aerosols. (A)</p> Signup and view all the answers

Which of the following is NOT a benefit of wet dressings?

<p>Provide a protective barrier against pathogens. (C)</p> Signup and view all the answers

What characteristic do foams have that differentiates them from other topical forms?

<p>They are gas-propelled liquids or solids. (C)</p> Signup and view all the answers

Which of the following excipients is used to prevent rancidity in hydrocarbon formulations?

<p>Butylated hydroxytoluene (BHT). (A)</p> Signup and view all the answers

What is one drawback of foams as a topical dosage form?

<p>They tend to break down quickly. (B)</p> Signup and view all the answers

What type of antimicrobial preservative is commonly found in water-containing dosage forms?

<p>Benzalkonium chloride. (B)</p> Signup and view all the answers

Which type of moisturizer primarily inhibits transepidermal water loss?

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

What is a significant drawback of using humectants in low humidity environments?

<p>They may draw water from the skin. (C)</p> Signup and view all the answers

What does the fingertip unit measurement represent?

<p>The quantity from fingertip to the index finger's first crease. (D)</p> Signup and view all the answers

Which of the following is a characteristic of co-solvents?

<p>They enhance drug solubility and prevent precipitation. (B)</p> Signup and view all the answers

What is the recommended time frame for applying moisturizers after bathing?

<p>Within 3 minutes of bathing. (A)</p> Signup and view all the answers

Which ingredient is commonly used as a humectant?

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

Which of the following is NOT a property of occlusive agents?

<p>They enhance drug penetration. (C)</p> Signup and view all the answers

What is the purpose of using a thin film of moisturizer during application?

<p>To achieve effective hydration without excess product. (B)</p> Signup and view all the answers

Flashcards

Ointment base types

Ointment bases are categorized based on their interaction with water, including hydrocarbon, absorption, and emulsion bases.

Hydrocarbon ointment base

A greasy, water-insoluble ointment base, typically anhydrous, that forms a continuous film on the skin.

Absorption ointment base

A greasy, ointment base that can absorb water due to surfactants, typically forming water-in-oil emulsions.

Emulsion ointment base (water-in-oil)

An ointment base where water is the internal phase and oil is the external phase, often containing pre-mixed water.

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Occlusiveness

The ability of an ointment base to prevent water loss from the skin.

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Emollient effect

The ability of an ointment base to soften and soothe the skin.

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White Petrolatum

A common, highly refined hydrocarbon ointment base used in ointments; commonly known as Vaseline.

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Hydrophilic Petrolatum

A water-absorbing ointment base containing petrolatum and surfactants; known as Aquaphor.

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Eucerin

A skin moisturizer similar to Aquaphor, but with added water and preservatives. It's somewhat occlusive.

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Oil-in-water creams

Creams where water is the external phase. They absorb varying amounts of water and can be turned into lotions.

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Hydrophilic ointment

A type of cream where water evaporates after application, leaving a protective film. Good for drug delivery.

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Water-soluble bases

Bases made of polyethylene glycols (PEGs). They feel greasy but are water-soluble and non-occlusive.

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Pastes

Ointments with a high percentage (20-50%) of fine powder, usually petrolatum. Forms a protective film.

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Occlusive

Something that prevents or blocks the passage of something, often used for skin care products to retain moisture.

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Emollient

A substance that softens or smoothes skin.

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Transepidermal water loss

The natural loss of water from the skin.

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Gelling Polymers

Polymers that create gel-like consistency, often used as suspending agents in higher concentrations. Examples include carbomer, tragacanth, alginic acid, and cellulose derivatives.

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Gel Characteristics

Most gels are designed to be both water-soluble and water-absorbing. This allows for easy application and drug release.

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Gel Application

When applied, the solvent evaporates, leaving a porous matrix film that allows drug diffusion.

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Gel Drug Delivery

The porous matrix film efficiently releases the drug, making gels advantageous for drug delivery.

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Gel Penetration Enhancement

Solvents like ethanol can increase drug penetration into the skin.

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Gel Potency

Gels often have greater potency compared to other dosage forms with the same drug concentration due to efficient release and penetration enhancement.

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Collodion

A liquid preparation of pyroxylin dissolved in alcohol, ether, and acetone, with or without added drugs, that forms a film upon application.

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Collodion Application

The film formed by collodion can seal small wounds and protect surrounding tissue.

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What are lotions?

Lotions are liquid emulsions or suspensions applied topically. They predominantly have an aqueous continuous phase, meaning water is the main component.

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Mention lotion examples

Calamine lotion, Clotrimazole lotion, Selenium sulfide lotion, and Cetaphil (oil-in-water emulsion) are common examples of lotions.

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What is a lotion's therapeutic effect?

Lotions evaporate upon application, leaving a thin film. This cooling effect soothes the skin and their fluidity allows easy application to various areas.

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Describe the stability of lotions

Lotions, like oral suspensions and emulsions, can experience physical instability (separation, settling), chemical instability, and microbiological instability.

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What are topical solutions?

Topical solutions are generally aqueous vehicles that sometimes contain alcohol.

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Examples of topical solutions

Burrow's solution, Dakin's solution (diluted sodium hypochlorite), and tinctures are examples of topical solutions.

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What are gels?

Gels are semi-solid systems where a liquid phase is confined within an interconnected polymeric matrix, often made from natural or synthetic gums.

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What is the composition of a typical gel?

Gels typically have a water based liquid phase, but can contain co-solvents like alcohol. The drug is usually suspended or dissolved in this liquid phase.

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Aerosols

A delivery system for medicines in the form of a spray, typically using a blend of drug and propellant. Examples include: Anti-fungal powders, Sunburn products.

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Wet Dressings

Aqueous solutions soaked into dressings like gauze, linens used for cleansing and promoting wound healing. Often contain astringents or antiseptic agents.

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Foams

Gas-propelled liquids or solids administered as aerosols, similar in consistency to shaving cream. Used for gentle application and easier spreading without rubbing.

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Antioxidants

Substances added to topical dosage forms to prevent rancidity in hydrocarbon-containing formulations.

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Antimicrobial Preservatives

Substances added to water-containing dosage forms to prevent microbial growth.

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Castor Oil

A natural oil used as a plasticizer in topical dosage forms – it softens the pyroxylin and helps it stay in place.

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Occlusive Moisturizers

Moisturizers that form a barrier on the skin to prevent water loss. They create a seal, keeping moisture in.

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Humectants

Moisturizers that attract water to hydrate the skin. They can pull moisture from the air or from deeper layers of the skin.

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Co-solvents

Substances that help dissolve medications in moisturizers, preventing the medicine from separating out.

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Fingertip Unit

A way to measure the correct amount of moisturizer to apply, about the size from your fingertip to the first crease.

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Rule of Hand

Estimates the amount of moisturizer needed for both sides of one hand, about one fingertip unit.

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Apply Moisturizer after Bathing

The best time to apply moisturizer is right after bathing or showering, when your skin is still damp.

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Clean Hands Before & After

Always wash your hands before and after applying moisturizer to prevent spreading germs.

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Thin Film Application

Apply moisturizer in a thin layer, usually enough to cover the area without being too thick.

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Study Notes

Topical Drug Delivery - Semisolids

  • Semisolids include ointments, intended for skin or mucous membrane application.
  • Ointments contain a medicinal substance.
  • Classifications based on interaction with water:
    • Hydrocarbon (oleaginous) bases: greasy, insoluble in water, anhydrous, do not absorb water.
      • Examples: White Petrolatum USP (Vaseline), White Ointment USP (wax added for stiffness/smoothness).
      • Properties: form an adherent, continuous, greasy, water-repellent film, good occlusiveness (blocks water loss), emollient effect (softens skin), enhance drug permeation, prolonged contact time.
      • Patient aspects: greasy/unpleasant, not water washable, can stain.
    • Absorption bases: greasy, anhydrous, can absorb water due to surfactants, typically form water-in-oil emulsions with added water.
      • Examples: lanolin, hydrophilic petrolatum USP (Aquaphor).
      • Properties: somewhat occlusive, less greasy than hydrocarbon bases, readily absorbed.

Topical Drug Delivery - Liquids

  • Lotions are fluid emulsions or suspensions for external application.
  • Continuous phase is typically aqueous.
  • Examples: Calamine lotion, clotrimazole lotion, selenium sulfide lotion, Cetaphil (oil-in-water emulsion).
  • Properties: non-occlusive, evaporates, cools/soothes skin, suitable for large areas, non-greasy-highly acceptable.

Topical Drug Delivery - Pastes

  • Pastes are ointments with high percentages (20-50%) of fine powder.
  • Base is usually petrolatum.
  • Examples of powders: Zinc oxide, talc, starch, bentonite.
  • Properties: thick, protective film, less greasy than corresponding base without powder, absorptive, stiff.

Topical Drug Delivery - Aerosols

  • Aerosols are drug/propellant blends for spray application.
  • Useful for areas where rubbing is irritating (e.g., sunburns).
  • Examples: antifungal spray powders, sunburn products (e.g., Solarcaine).

Topical Drug Delivery - Plasters

  • Plasters are solid/semisolid adhesive masses spread on backing material for prolonged external application.
  • Similar to patches but can be shaped to the treatment area.
  • Example: Salicylic acid plaster (Mediplast).

Topical Drug Delivery - Wet Dressings

  • Aqueous solutions applied as a dressing (e.g., gauze, linens).
  • Solutions are typically astringents or antiseptics.
  • Benefits: cleanse wounds of exudates, help with wound healing, maintain drainage, remove exudates/secretions.
  • Example: Aluminum acetate.

Topical Drug Delivery - Foams

  • Foams are gas-propelled liquids/solids, resemble shaving cream consistency.

Topical Dosage Form Excipients

  • Antioxidants prevent rancidity (e.g., BHT, BHA, Vitamin E).
  • Antimicrobial preservatives prevent microbial growth (e.g., benzalkonium chloride, parabens, benzoic acid).
  • Waxes increase stiffness/reduce tackiness (e.g., beeswax, cetyl esters wax, cetyl alcohol).
  • Moisturizers hydrate skin:
    • Occlusive (inhibit water loss: petrolatum, Aquaphor).
    • Non-occlusive (e.g., dimethicone, other silicones).

Topical Drug Considerations

  • Thin films are sufficient for most applications but diaper rash pastes use thicker films.
  • Fingertip unit-measurement method estimates product dosage.
  • Cleanse/dry treatment area, apply shortly after bathing/showering.
  • Use gentle rubbing/massage motions for application.
  • Avoid excessive amounts (especially in children) due to increased drug penetration.
  • Exercise caution in thin-skinned areas and intertriginous areas (skin-on-skin contact) due to increased drug penetration.

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