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Drug Delivery 2 > Polymer Delivery > Flashcards

Polymer Delivery Flashcards

1
Q

Nanoparticles targeting cancer cells

A

Passive tissue targeting in blood to enter the cell
Active cellular targeting to bind cancer cells and release drug
Enhanced permeation and retention effect

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2
Q

Liposome targeting

A

Do I’ll
Myocytes
ThermoDox
AmBisome
RexinG

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3
Q

Polymeric nanoparticles

A

Genexol-PM
BIND-014

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4
Q

Polymer-drug conjugates

A

Oncaspar

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5
Q

Albumin-bound nanoparticles

A

Abraxane

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6
Q

Inorganic Nanoparticles

A

Aurimune
Auroshell

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7
Q

Doxil

A

First approved nano drug
Indications:
AIDS-related Kaposi’s sarcoma
Recurrent ovarian cancer
Metastatic breast cancer
Multiple myeloma in combination with bortezomib

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8
Q

Doxil structure

A

Doxorubicin encapsulated in the internal
compartment: up to 15,000 molecules are loaded per vesicle
Lipid bilayer membrane of Liposome composed of
HSPC, PEG-DSPE, and cholersterol
2K Da segments of PEG are grafted to the liposome surface: the stealth liposomes are nearly invisible to the RES system

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9
Q

Doxil performance

A

Extra long circulation time compared to free doxorubicin
Large decrease in cardiotoxicity
SE: mucositis and PPE due to long circulation time and tendency of liposomes to accumulate at skin

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10
Q

Myocet

A

Approved in Europe and Canada
Lacks PED functional inaction on the particle
—not invisible to RES
—Not associated with PPE
—lower incidence of mucositis
Similar efficacy to Doxil with lower cardio-toxicity
Non-PEGylated

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11
Q

ThermoDox

A

First heat activated form of liposomal doxorubicin
Changes structure when heated to a specific temp
IV infusion to be combined with hyperthermia treatments like RFA

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12
Q

ThermoDox ongoing trials

A

Primary hepatocellular carcinoma (Phase 3)
—57% improvement in overall survival
Refractory chest wall breast cancer (phase 2)
Colorectal liver metastases (Phase 2)

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13
Q

RF liver Ablation + ThermoDox

A

Expanding the treatment zone addresses RFA limitations
- infuse 15 min prior to RFA
- concentrates in the the thermal zone
Grain boundary structure (similar to a soccer ball)

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14
Q

ThermoDox targeting strategies

A
  1. Conventional passive targeting
  2. Heat-activated permeation and release
    —25x more doxorubicin than IV
    —5x more doxorubicin than standard liposomal formulations
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15
Q

AmBisome

A

FDA approved
Active ingredient amphotericin B
Mild nephrotoxicity (compared to moderate in other forms and high in free form
Diameter is much smaller than other formulations

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16
Q

Rexin-G

A

liposomal replication incompetent retro vector encoding an N-terminal deletion mutant of cyclin G1 gene
US Fast Track status
All primary and secondary Phase II trials done for pancreatic cancer, sarcoma, and osteosarcoma

17
Q

Rexin G characteristics

A

tumoricidal dominant negative cyclin G1 that blocks cell cycle in G1, causing apoptosis of cancer cells
Stealthy with low immunogenicity, enabling repeated IV infusions
liposome platform can target cancer collagen matrix

18
Q

Genexol-PM

A

polymeric micelle formulation of paclitaxel
Clinical studies in progress for several malignancies including phase II and IV studies in recurrent breast cancer

19
Q

Genexol-PM structure

A

amphiphilic block copolymer + hydrophobic drug
Forms a polymeric micelle (10-200 nm)

20
Q

BIND-014

A

polymeric nanoparticle containing docetaxel
targeted to prostate-specific membrane antigen (PSMA)
Currently in Phase II for squamous histology and urothelial carcinoma, cholangiocarcinoma, cervical cancer, and squamous cell carcinoma of the head and neck

21
Q

BIND-014 Formulation

A

Used combinatorial screening to identify the optimal formulation

22
Q

BIND-014 results

A

was anticipated to improve the clinical benefit of docetaxel by increasing its concentration and duration of exposure in tumors

23
Q

Oncaspar

A

Modified enzyme used as an antineoplastic agent
Used for treatment of ALL patients hypersensitive to the native L-asparaginase
Indicated for acute lymphoblastic leukemia

24
Q

Oncaspar results

A

PEGylated asparaginase
Increased drug hydrodynamic radius
–prolonged circulation and retention time
–lower proteolysis
–slower renal excretion
Decreased antigenicity
–lower chance to develop hypersensitivity
Reduced the number of injections to the patient by 7x

25
Q

Abraxane

A

First tumor targeted chemotherapy based on nab technology
Indications: breast cancer, non-small cell lung cancer, pancreatic cancer

26
Q

Abraxane mechanism

A

Abraxane binds to albumin receptor gp60 and is actively transported across endothelial cells and into the interstitial space (transcytosis)

27
Q

Abraxane results

A

Longer overall survival
Longer progression-free survival
But improvements are marginal

28
Q

Inorganic nanoparticles

A

SPIONs (Feridex, Resovist, Endorem)
Aurimune
Auroshell

29
Q

Aurimune

A

27 nm gold nanoparticle coated with thiolated PEG and and attached to recombinant human TNF-a
PEG bound nanoparticles prevent uptake by liver and spleen
Au NPs are detectable in post-treatment tumor biopsies but not healthy tissues
Phase II trial for non-small lung cancer patients

30
Q

Aurimune results

A

Levels last longer
More penetrate the tumor
Greater efficacy

31
Q

Auroshell

A

gold metal shell and a non-conducting, or dielectric, sillica core and is the exogenous absorber of near IR laser energy delivered by the fiber

32
Q

Aurolase therapy

A

NPs delivered IV
Accumulate in tumor by EPR effect
Tumor illuminated with NIR laser
Nanoparticles selectively absorb laser energy converting to heat
Heat destroys tumor and blood vessels
Surrounding healthy tissue not significantly damaged

33
Q

SPIONs

A

Usually composed of Fe3O4
intrinsic toxicity so must be modified through surface coatings for biocompatibility
Mostly used for imaging and diagnostics in liver/other cells of RES
Commercial production ceased due to lack of sales and poor performance

34
Q

SPIO future

A

could be the next generation of MRI agents

35
Q

FDA or EMA approved nanomedicines

A

Oncaspar
Doxil
AmBisome
Myocet
Abraxane
Genexol-PM

Drug Delivery 2 (8 decks)

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