Tumor-targeted drug delivery MCQs With Answer is designed to help M. Pharm students master key concepts in Molecular Pharmaceutics and Novel Drug Delivery Systems (MPH 201T). This quiz focuses on the principles and practice of directing therapeutics specifically to tumors, reducing systemic toxicity and improving efficacy. You will revisit the enhanced permeability and retention (EPR) effect, active versus passive targeting, ligand–receptor strategies, nanocarrier design, endosomal escape, and tumor microenvironment-responsive release. The questions also cover clinically translated systems like pegylated liposomes, albumin-bound nanoparticles, and antibody–drug conjugates (ADCs), along with barriers such as protein corona, high interstitial fluid pressure, and the binding-site barrier. Use this set to test understanding and refine exam readiness.
Q1. Which statement best describes the Enhanced Permeability and Retention (EPR) effect in solid tumors?
- Preferential uptake of small-molecule drugs by active transporters in tumor cells
- Accumulation of nanosized carriers due to leaky vasculature and poor lymphatic drainage
- Enhanced efflux of nanoparticles from tumors via functional lymphatics
- Selective receptor-mediated endocytosis of all nanoparticles by cancer cells
Correct Answer: Accumulation of nanosized carriers due to leaky vasculature and poor lymphatic drainage
Q2. What hydrodynamic size range most commonly balances tumor extravasation via EPR with avoidance of rapid renal clearance?
- 1-5 nm
- 30-150 nm
- 300-800 nm
- Greater than 1 micron
Correct Answer: 30-150 nm
Q3. What is the primary purpose of PEGylation on nanocarriers intended for tumor targeting?
- Enhance drug solubility within the tumor interstitium
- Impart a stealth effect to reduce opsonization and prolong circulation
- Increase endosomal escape via the proton sponge effect
- Target integrins for receptor-mediated uptake
Correct Answer: Impart a stealth effect to reduce opsonization and prolong circulation
Q4. Which statement is most accurate regarding active (ligand-mediated) tumor targeting?
- It primarily enhances specific cellular uptake after extravasation rather than dramatically increasing total tumor accumulation
- It guarantees substantially higher tumor accumulation in all in vivo models
- It eliminates clearance by the mononuclear phagocyte system
- It prevents off-target toxicity completely
Correct Answer: It primarily enhances specific cellular uptake after extravasation rather than dramatically increasing total tumor accumulation
Q5. Which is a clinically approved example of a tumor-targeted nanomedicine?
- Conventional amphotericin B deoxycholate
- Doxil (pegylated liposomal doxorubicin)
- Paracetamol oral solution
- Regular insulin injection
Correct Answer: Doxil (pegylated liposomal doxorubicin)
Q6. Which is an endogenous tumor-associated stimulus commonly used to trigger drug release from smart nanocarriers?
- Near-infrared light
- Ultrasound
- Acidic extracellular pH
- External magnetic field
Correct Answer: Acidic extracellular pH
Q7. Which ligand–receptor pair is correctly matched for active tumor targeting?
- Folate receptor alpha — folic acid
- Epidermal growth factor receptor — dextran
- Nucleolin — trastuzumab
- Prostate-specific membrane antigen (PSMA) — albumin
Correct Answer: Folate receptor alpha — folic acid
Q8. In antibody–drug conjugates (ADCs), which component most critically governs payload release inside tumor cells?
- PEG molecular weight
- Zeta potential of the antibody
- Linker chemistry (e.g., enzyme- or pH-cleavable)
- Surfactant used during formulation
Correct Answer: Linker chemistry (e.g., enzyme- or pH-cleavable)
Q9. The enhanced endosomal escape often observed with branched polyethyleneimine (PEI) is attributed to which mechanism?
- EPR effect
- Proton sponge effect
- Bystander effect
- Accelerated blood clearance phenomenon
Correct Answer: Proton sponge effect
Q10. Elevated interstitial fluid pressure (IFP) in tumors most commonly leads to which outcome for nanocarrier delivery?
- Enhanced convective transport deep into the tumor
- Increased lymphatic drainage from the tumor core
- Limited convective transport from blood vessels and poor deep penetration
- Reduced hypoxia and improved perfusion
Correct Answer: Limited convective transport from blood vessels and poor deep penetration
Q11. How can the formation of a protein corona on nanoparticles affect tumor targeting?
- It universally enhances the specificity of all targeting ligands
- It may mask ligands and alter biodistribution, redirecting cellular uptake
- It eliminates complement activation-related reactions
- It guarantees improved tumor penetration
Correct Answer: It may mask ligands and alter biodistribution, redirecting cellular uptake
Q12. Which surface charge is generally associated with reduced nonspecific protein adsorption and prolonged circulation in vivo?
- Highly cationic (around +30 mV)
- Slightly negative to near-neutral (about -10 to 0 mV)
- Highly negative (around -40 mV)
- Strongly cationic but without PEGylation
Correct Answer: Slightly negative to near-neutral (about -10 to 0 mV)
Q13. Which value best approximates the extracellular pH in many solid tumor microenvironments?
- 7.4
- 6.6
- 5.0
- 8.0
Correct Answer: 6.6
Q14. The Accelerated Blood Clearance (ABC) phenomenon observed with some PEGylated liposomes is best described as:
- Prolonged circulation upon repeated dosing due to immune tolerance
- Accelerated clearance after repeated dosing due to anti-PEG immune response
- Enhanced tumor uptake with each subsequent dose
- Complete prevention of opsonization after the first dose
Correct Answer: Accelerated clearance after repeated dosing due to anti-PEG immune response
Q15. Which strategy can enhance deep penetration of nanocarriers within tumor tissue?
- Conjugation of the tumor-penetrating peptide iRGD
- Increasing particle size to 500 nm
- Designing a systemic zeta potential of +50 mV
- Adding a radiolabel to increase molecular weight
Correct Answer: Conjugation of the tumor-penetrating peptide iRGD
Q16. In magnetic targeting of tumors, which statement is correct?
- An external magnetic field can localize magnetically responsive nanoparticles to a target region
- Magnetic nanoparticles intrinsically bind to all tumor receptors
- Magnetic hyperthermia requires only optical excitation
- Magnetic targeting eliminates the need for vascular extravasation
Correct Answer: An external magnetic field can localize magnetically responsive nanoparticles to a target region
Q17. Which is a characteristic advantage of caveolae-mediated endocytosis for certain nanocarriers?
- It invariably routes cargo to lysosomes for rapid degradation
- It often avoids lysosomal degradation and traffics via caveosomes
- It is limited to particles smaller than 5 nm
- It requires high-density mannose ligands
Correct Answer: It often avoids lysosomal degradation and traffics via caveosomes
Q18. Which linker is widely used in ADCs for enzyme-triggered intracellular release in tumors?
- Valine–citrulline peptide linker (cathepsin-cleavable)
- PEG-DSPE conjugate
- Simple succinate ester without enzyme sensitivity
- Noncleavable thioether that cannot be degraded
Correct Answer: Valine–citrulline peptide linker (cathepsin-cleavable)
Q19. What best defines a theranostic nanocarrier in oncology?
- A carrier that releases drug only in the liver
- A system integrating imaging capability with targeted drug delivery
- A formulation designed solely for radiosensitization
- A prodrug that is activated by sunlight
Correct Answer: A system integrating imaging capability with targeted drug delivery
Q20. The binding-site barrier can restrict deep tumor penetration of high-affinity ligands. Which strategy can mitigate this problem?
- Use ultra-high-affinity ligands (Kd less than 10 pM)
- Use moderate-affinity ligands to allow dissociation and re-binding deeper in tissue
- Increase particle size to limit diffusion
- Eliminate PEGylation to increase sticking at the vessel wall
Correct Answer: Use moderate-affinity ligands to allow dissociation and re-binding deeper in tissue

I am a Registered Pharmacist under the Pharmacy Act, 1948, and the founder of PharmacyFreak.com. I hold a Bachelor of Pharmacy degree from Rungta College of Pharmaceutical Science and Research. With a strong academic foundation and practical knowledge, I am committed to providing accurate, easy-to-understand content to support pharmacy students and professionals. My aim is to make complex pharmaceutical concepts accessible and useful for real-world application.
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