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PM4B - Antonio > Advanced Drug Delivery > Flashcards

Advanced Drug Delivery Flashcards

1
Q

What does drug delivery/ targeting mean?

A

Delivery of a drug to its precise site of action at the right concentration for the right time

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2
Q

What are conventional dosage forms?

A

Drug release/ drug plasma levels depend on the physicochemical properties of the active ingredient

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3
Q

What are non-conventional dosage forms?

A

Drug release/ drug plasma levels are determined by the technological characteristics of the formulation (e.g. modified release)

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4
Q

What type of dosage form is ‘modified-release’?

A

Non-conventional

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5
Q

Can dopamine cross the blood brain barrier?

A

No

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6
Q

In what terms can a drug be ‘modified’?

A

(1) Rate
(2) Time
(3) Space

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7
Q

Why can L-DOPA cross the blood brain barrier where dopamine cannot?

A

Carboxylic acid group has been added

Is an amino acid

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8
Q

What are some ways in which ‘rate’ of a drug release can be changed?

A

(1) Very fast release

(2) Sustained release

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9
Q

How many ‘time’ of a drug release be changed?

A

When release starts after a certain time following administration

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10
Q

How may ‘space’ of a drug release be changed?

A

Occurs in specific areas/ tissues

Targeting

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11
Q

Who is Paul Ehrlich?

A

Nobel prize winner for medicine in 1908

Worked in field of immunity

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12
Q

What is the objective of drug targeting?

A

Localise and concentrate drugs to the desired therapeutic site, avoiding all other tissues in the body

i.e. pharmacological response without the side-effects

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13
Q

What is first order drug targeting?

A

Organ/ tissue specificity

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14
Q

What is second order drug targeting?

A

Certain type of cell specificity

e.g. tumour cells

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15
Q

What is third order drug targetting?

A

Intracellular compartment specificity

e.g. lysosomes

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16
Q

What are three approaches to drug targeting?

A

(1) Magic bullet
(2) Prodrug
(3) Macromolecular carrier

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17
Q

What is the ‘magic bullet’ approach to drug targeting?

A

API is potent + selective

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18
Q

What is the ‘prodrug’ approach to drug targeting?

A

Inactive prodrug

Activated to drug in site of action

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19
Q

What is the ‘macromolecular carrier’ approach to drug targeting?

A

Carrier transports the drug to desired site of action

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20
Q

What drug targeting approach do monoclonal antibodies largely align with?

A

(1) Magic bullet

(2) Macromolecular carrier

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21
Q

When were monoclonal antibodies first introduced?

A

1975

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22
Q

What types of monoclonal antibody are commercially available?

A

(1) Diagnostic agents

(2) Therapeutic agents

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23
Q

Why is drug targeting of bacterial cells easier than that of cancer cells?

A

Bacterial cells have many differences to human cells

Cancer cells are very similar

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24
Q

Who coined the phrase ‘magic bullet’?

A

Paul Ehrlich

Medicine nobel prize winner

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25
Q

What is the difference between a polyclonal antibody and a monoclonal antibody?

A

Polyclonal: Multiple antigen targets

Monoclonal: Single antigen target

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26
Q

What was the first monoclonal antibody to reach the market?

A

OKT3

Anti-CD3 antibody

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27
Q

What is OKT3 used for?

A

Prevent rejection of kidney transplants

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28
Q

What is abciximab?

A

Monoclonal antibody

Used for prevention of cardiac ishaemic complications

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29
Q

What is trastuzumab?

A

Monoclonal antibody

HER-2 positive breast carcinoma

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30
Q

What is Herceptin?

A

Trastuzumab monoclonal antibody

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31
Q

What is ReoPro?

A

Abciximab monoclonal antibody

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32
Q

What is the principle of monoclonal antibodies as imaging agents?

A

mABs against tumour-associated antigens have been developed

mABs are conjugated with a diagnostic imaging agent

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33
Q

What are some available commercial products of monoclonal antibodies as imaging agents?

A

(1) Oncoscint
(2) Prostascint
(3) Myoscint

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34
Q

What is oncoscint?

A

Monoclonal antibody

For imaging of colon and ovarian cancer

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35
Q

What is prostascint?

A

Monoclonal antibody

For imaging of prostate cancer

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36
Q

What is myoscint?

A

Monoclonal antibody

Cardiac imaging

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37
Q

What is an antibody?

A

Protein

Produced by the body

As a result of exposure to an antigen

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38
Q

What is a prodrug?

A

Chemically/ pharmacologically inactive derivative of the drug

Undergo action at the target site

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39
Q

How many chains are there in an antibody?

A

4 chains

2 light

2 heavy

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40
Q

How are the chains of an antibody connected?

A

Disulfide bonds

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41
Q

What happens to a prodrug when it reaches the target site?

A
  • Chemically activated
  • Physically activated
  • Enzymatically activated
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42
Q

Why are prodrugs used?

A

(1) Improve permeability through biological membranes
(2) Site-specific administration
(3) Increase duration of drug action
(4) Decrease toxicity and side-effects
(5) Improve the formulation

(6) Improve organoleptic properties
- Effects on organs

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43
Q

What does ‘organoleptic’ mean?

A

Action/ effects on organs

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44
Q

What are macromolecular carriers?

A

Biologically inert macromolecules

Used to deliver the drug to the site of action

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45
Q

What are macromolecular carriers generally composed of?

A

Polymers

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46
Q

What types of macromolecular carrier are there?

A

(1) Particulate carrier system

(2) Soluble macromolecular carrier

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47
Q

How can a drug be in a macromolecular carrier?

A

(1) Entrapped in the carrier via physical bonds

(2) Covalently conjugated via covalent bonds

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48
Q

In a macromolecular carrier, what does the distribution of the drug depend on?

A

The characteristics of the carrier

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49
Q

What are the types of targeting in macromolecular carriers?

A

(1) Active targeting
(2) Passive targeting

(3) Physical targeting
- Apply physical stimulus to promote API release in a certain area

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50
Q

How does ‘passive targeting’ work in macromolecular carriers?

A

Exploits the natural (passive) distribution pattern of a drug carrier

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51
Q

What type(s) of drug targeting technologies are associated with monoclonal antibodies?

A

(1) Magic bullet

(2) Macromolecular carriers

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52
Q

What type(s) of drug targeting technologies are associated with liposomes?

A

Macromolecular carriers

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53
Q

What type(s) of drug targeting technologies are associated with microparticles?

A

Macromolecular carriers

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54
Q

What type(s) of drug targeting technologies are associated with nanoparticles?

A

Macromolecular carriers

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55
Q

What type(s) of drug targeting technologies are associated with micelles?

A

Macromolecular carriers

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56
Q

What type(s) of drug targeting technologies are associated with polymer therapeutics?

A

Macromolecular carriers

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57
Q

From smallest to largest, list the sizes of general drug delivery systems and carriers.

A

(1) Monoclonal antibodies
(2) Nanoparticles
(3) Microparticles

(4) Macrodevices
- e.g. implantable devices

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58
Q

What is needed for a drug to have a therapeutic effect?

A

(1) Pharmacologically active

(2) To arrive at the right place at the right time

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59
Q

What is levodopa?

A

Modified dopamine, can cross BBB

Prodrug

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60
Q

How can drug release be modified?

A

(1) Rate
- very fast/ sustained release

(2) Time
- when release starts after a certain time following administration

(3) Space
- specific tissues (targeting)

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61
Q

What is 1st order targeting?

A

Organ/ tissue

e.g. liver

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62
Q

What is 2nd order targeting?

A

Certain type of cell

e.g. tumour cells

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63
Q

What is 3rd order targeting?

A

Intracellular compartment

e.g. lysosomes

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64
Q

What are some different targeting approaches?

A

(1) Magic bullet
(2) Prodrug
(3) Macromolecular carrier

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65
Q

What is magic bullet?

A

Targeting approach

Active ingredient is active and selective

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66
Q

What is prodrug targeting?

A

Targeting approach

Inactive prodrug - activated at site of action

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67
Q

What is macromolecular targeting?

A

Targeting approach

Carrier transports drug to site of action

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68
Q

What type(s) of activation can prodrugs undergo at the target site?

A

Chemical/ physical/ enzymatic activation

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69
Q

Why do we use prodrugs?

A

(1) Improve permeability through membranes
(2) Site-specific administration
(3) Increase duration of drug action
(4) Decrease toxicity + side effects
(5) Improve formulation
(7) Improve organoleptic properties

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70
Q

Define organoleptic properties.

A

Taste/ sight/ smell/ touch of drug

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71
Q

What are macromolecular carriers generally composed of?

A

Polymer

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72
Q

What are the two mechanisms by which a macromolecular carrier can deliver a drug?

A

(1) Entrapped in the carrier
- physical bonds

(2) Covalently conjugated
- covalent bonds

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73
Q

Which targeting approach is monoclonal antibodies and antibody-drug conjugates?

A

Magic bullet/ macromolecular carrier

74
Q

Which targeting approach are liposomes?

A

Macromolecular carrier

75
Q

Which targeting approach is micro/ nanoparticles?

A

Macromolecular carrier

76
Q

Which targeting approach do micelles implement?

A

Macromolecular carrier

77
Q

Which targeting approach are polymer therapeutics?

A

Macromolecular carrier

78
Q

What are liposomes?

A

Microparticulated/ colloidal drug carriers

79
Q

When were liposomes discovered and by whom?

A

1965

Bangham

80
Q

Describe the structure of a liposome.

A

Vesicular structures

≥1 lipid bilayers
- normally phospholipids

Aqueous core

81
Q

Describe structure of glycerol.

A

3 carbons

3 chains coming off each oxygen on each carbon

Fatty acid chains

82
Q

Describe the structure of cholesterol.

A

Lipophilic (hydrophobic) region of rings

Hydrophilic hydroxyl group

83
Q

What effect does cholesterol have on the phospholipid bilayer?

A

Tm = main transition temperature

Condensing effect (if above Tm)

Fluidising effect (if below Tm)

84
Q

What is Tm?

A

Main transition temperature

Temperature above which are move fluid

85
Q

When does addition of cholesterol into the phospholipid bilayer have a condensing effect?

A

If above Tm

86
Q

When does addition of cholesterol into the phospholipid bilayer have a fluidising effect?

A

If below Tm

87
Q

What type of lipid tends to form micelles?

A

Lisaphospholipids

88
Q

What type of lipid tends to form bilayer vesicles?

A

Double chain phospholipids

Large head groups

89
Q

What type of lipid tends to form planar bilayers?

A

Double chain phospholipids

Small head groups

90
Q

What type of lipid tends to form inverted micelles?

A

Unsatured phosphadylethanol amine

91
Q

What is an SUV?

A

Small unilamellar vesicles

92
Q

What is an LUV?

A

Large unilamellar vesicles

93
Q

What is an MLV?

A

Multilamellar vesicles

94
Q

What is an MVV?

A

Multivesicular vesicles

95
Q

How large are SUVs?

A

0.02-02 micrometres

96
Q

How large are LUV?

A

0.2-10 micrometres

97
Q

Where will a lipophilic drug reside in a liposome?

A

Inserted in the tails

98
Q

Where will a hydrophilic drug reside in a liposome?

A

Inserted in aqueous core

99
Q

How do you prepare liposomes?

A

Form spontaneously after addition of water to phospholipids

(1) Lipid hydration
(2) Selection of liposomes based on size
(3) Remove non-encapsulated drug

100
Q

What is Thin Layer Evaporation?

A

(1) Phospholipids dissolved in organic solvent
(2) Phospholipid film
(3) Film hydration under stirring
(4) Sonication (ultrasound bath) OR extrusion (application of pressure through filters)

101
Q

How are liposomes characterised?

A
  • Lipid:drug ratio
  • Encapsulation efficiency
  • Size
  • Lamellarity
102
Q

What are the administration routes for liposomes?

A
  • PARENTERALLY
  • topically
  • pulmonary
  • orally
103
Q

What are some issues with liposome stability, before administration?

A
  • oxidation of lipophilic chains

- hydrolysis + formation of lysophospholipids

104
Q

What are some issues with liposome stability, after administration?

A

Can be captured by macrophages + carried to the liver

- no longer bioavailable

105
Q

What is STEALTH?

A

Sterically stabilised liposomes

Masks liposomes from macrophages

106
Q

What are the different types of liposomes?

A
  • conventional liposomes
  • sterically stabilised (stealth) liposomes
  • immunoliposomes (antibody targeted)
  • cationic liposomes (gene delivery)
107
Q

What is amphotericin B?

A

Antifungal

108
Q

What are polymer-drug conjugates and polymer-protein conjugates, generally?

A

Systems with covalent conjugation between polymer and API

109
Q

What are polymer-drug conjugates?

A

Many drugs

1 polymer

110
Q

What is a polymer-protein conjugate?

A

Many polymers

1 protein

111
Q

What does the term ‘conjugation’ indicate?

A

Covalent conjugation/ bonding

112
Q

What are the following:

  • asparaginase
  • methioninase
  • arginine deaminase
  • uricase
A

Therapeutic enzymes

Proteins used for therapeutic applications

113
Q

What are 3 types of protein used for therapeutic application?

A

(1) Therapeutic enzymes
(2) Signalling proteins
(3) Antibodies/ protein fragments/ peptides

114
Q

What are some problems with proteins as therapeutic agents?

A 
- rapid renal excretion
  ø smaller than 40KDa
- proteolytic degradation
  ø enzymes
- immunogenicity
- aggregation
- solubility
- difficulty in formulation
115
Q

What size of protein will be excreted renally?

A

<40KDa

116
Q

What effect does addition of polymers to a protein have, regarding renal excretion?

A

Increases hydrodynamic volume

Reduces renal clearance

Makes it too large

117
Q

What effect does addition of polymers to a protein have, regarding aggregation?

A

Prevents/ reduces aggregation

HOWEVER, can reduce interaction with receptor

118
Q

What relationship does PKa have on pH, with regard to a dynamic equilibrium?

A

PKa = pH when 2 components are at same concentration

119
Q

What is PEG?

A

Best polymer for protein conjugation

Only has one potentially reactive group

120
Q

What is an example of a PEGylated protein for cancer.

A

Oncaspar (Pegaspargase)

For acute lymphoblastic leukaemia

121
Q

What effect does PEGylation have on half-life?

A

Increases half-life dramatically

122
Q

Why did DIVEMA fail as an anticancer agent?

A

Toxicity

123
Q

What is Copaxone used for?

A

SC administration in multiple sclerosis

Mimics myelin

124
Q

Which are generally more cytotoxic, polycations or poylanions?

A

Polycations

125
Q

How can polymeric drugs be broken down in the body?

A

(1) Biodegradable?

(2) Is it > or < than 40KDa

126
Q

What is a polymer-drug conjugate?

A

Drug delivery technology in which low MW drug molecules are covalently attached to a polymeric carrier

127
Q

What is the Ringsdorf’s model of polymer-drug conjugates?

A
  • hydrophilic polymeric backbone
  • biodegradable linker
  • targeting group (binds to receptor)
128
Q

What is HPMA?

A

First synthetic polymer-drug conjugate to undergo clinical evaluation

129
Q

How does an angiogenic tumour vessel that is <1-2mm get nutrients?

A

Diffusion

No induction blood supply

130
Q

How does an angiogenic tumour vessel that is >1-2mm get nutrients?

A

Induction of angiogenesis

131
Q

How does an angiogenic tumour vessel that is >200mm^3 get nutrients?

A

Hypoxia + necrosis in ~20% of tumour

132
Q

What is the enhanced permeability and retention (EPR) effect?

A

Polymeric therapeutic agents are retained better in tumour tissues than normal tissues, when compared with low MW drugs

133
Q

How does a free drug (low MW) enter a cell, compared to polymer-drug conjugates?

A

Passive diffusion

134
Q

How does a polymer-drug conjugate enter a cell, compared to a free (low MW) drug?

A

Endocytic capture

Endosome -> Lysosome -> Released intracellularly

135
Q

What are some advantages/ rationale for polymer-drug conjugates?

A
  • passive tumour targeting (EPR effect)
  • decreased toxicity
  • active tumour targeting (if targeting moiety present)
  • solubilisation of active ingredient
  • prolonged circulation time
    ø extending half-life
  • overcome some drug resistance mechanisms (MDR)
136
Q

What are the requirements for polymer-drug conjugates?

A

(1) Drug
- potent, in relation to polymer carrying capacity

(2) Linker
- stable during transport
- degradable within target environment

(3) Polymer
- non-toxic + non-immunogenic
- suitable for industrial-scale manufacture
- biodegradable/ <40KDa

(4) Targeting group
- specific for a target

137
Q

What is the only polymer-drug conjugate on the market?

A

Movantik

Carries naloxone

138
Q

What is Movantik?

A

The only polymer-drug conjugate on the market

PEGylated naloxone

139
Q

What is the polymer-drug conjugate carrying naloxone?

A

Movantik

140
Q

What does Movantik deliver?

A

Naloxone

141
Q

Where does naloxone initiate its effect?

A

Binds to mu-opioid receptors in GIT

142
Q

What are the types of microparticles?

A

(1) Microcapsules

(2) Microspheres

143
Q

What is a microcapsule?

A

Type of microparticle

Outer shell + inner core (2 distinct regions)

144
Q

What is a microsphere?

A

Type of microparticle

1 distinct region

Matrix style

145
Q

How can the core of a microcapsule be referred to?

A

Nuclei OR core

146
Q

How are microparticles administered?

A

(1) IV

(2) Directly to body compartment
- e.g. inhaled/ local injection/ SC injection

147
Q

What are the requirements of the materials used for microparticles?

A
  • chemically inert
  • non-toxic
  • biocompatible
  • biodegradable
  • easy to sterilise
148
Q

What are some applications of microparticles?

A
  • modified-release
  • conversion of liquids into pseudo-solids
  • protection from external environment
  • mask flavour + odour
  • reduce gastric irritation
149
Q

What is a pseudo-solid?

A

Transferring a liquid into somewhat of a solid via binding

Solid, but act like liquid

150
Q

What is a pseudo-solid?

A

Transferring a liquid into somewhat of a solid via binding

Solid, but act like liquid

151
Q

How can microparticles be prepared?

A

(1) Dispersion of drug in polymer solution

(2) Coacervation (phase separation)
- changing temp of polymer solution
- salting out (add charged species)
- adding a non-solvent
- inducing a polymer-polymer reaction

(3) Hardening of coating

152
Q

What is interfacial polymerisation?

A

Method of microparticle manufacture

(1) Aqueous phase + API
(2) Organic phase

153
Q

What is coacervation?

A

Phase separation of a solvent and solute

154
Q

State 2 methods for preparation of microspheres.

A

(1) Heat denaturation

(2) Chemical denaturation

155
Q

Describe the heat-denaturation method for preparation of microspheres.

A

(1) Oil + aqueous solution of protein + API
(2) Emulsion forms
(3) Heat at 100-170ºC
(4) Microspheres thermally stabilise

156
Q

Describe the chemical-denaturation method for preparation of microspheres.

A

(1) Oil + aqueous solution of protein + API
(2) Emulsion forms

(3) Addition of glutharaldehyde/ butadiene
- cross-linking agents

(4) Microspheres chemically stabilise

157
Q

What are some advantages of spray drying?

A
  • quick + reproducible
  • control on particle size
  • low cost
  • good yield
  • applicable to heat sensitive materials
158
Q

What are some disadvantages of spray drying?

A
  • need polymers that make low-viscosity solutions
  • need small droplets
  • water-soluble compounds have poor encapsulation
159
Q

How are drugs released from microspheres?

A

(1) Erosion
(2) Disintegration of microsphere

(3) Swelling
- API diffuses out

(4) Desorption + diffusion
(5) Ionic exchange

160
Q

Which polymers are often used for nanoparticles?

A
  • PLA
  • PLGA

Esters with ester bonds

161
Q

How can nanoparticles be prepared via solvent evaporation?

A

(1) Add aqueous solvent (polymer+drug) to water+emulsifying agent
(2) Forms droplets of solvent (in water phase) into water+emulsifying agent
(3) Evaporate solvent
(4) Nanoparticles containing API remain

162
Q

What can cause longer term toxicity in nano/microparticles?

A

(1) Lack of biodegradation

(2) Lack of bioerosion

163
Q

What does toxicity of nano and microparticles depend on?

A

Size + number of particles injected

164
Q

What is a problem with IV injections of nanoparticles?

A

Can be endocytose by macrophages

Causes problems to reach other tissues

BUT good for targeting liver/ spleen

165
Q

How can endocytosis of nanoparticles by macrophages be prevented/ reduced?

A

PEGylation of nanoparticles

166
Q

What is Abraxane?

A

PEGylated nanoparticle

Used in cancer therapy

167
Q

What is an example of a PEGylated nanoparticle?

A

Abraxane

168
Q

Define antibody-drug conjugates.

A

Monoclonal antibodies conjugated to cytotoxic agents

169
Q

How can the anti-cancer activity of monoclonal antibodies be increased?

A

Conjugating them with effector molecules

Drug can be attached via a ‘linker’ molecule

170
Q

What is a ‘linker’, with regard to advanced delivery methods?

A

Attaches the drug/ API to carrier (polymer/ antibody etc)

171
Q

What is Neulasta?

A

PEGylated protein

Pegfilgrastim

172
Q

What is Neulasta used for?

A

Reduction in duration of neutropenia + incidence of febrile neutropenia

In cytotoxic chemotherapy for malignancy

173
Q

What is the rationale for using Neulasta?

A

42hr half-life compared to 3.5-3.8hrs

Due to MW being 39KDa vs 18.8KDa of Nupogen

174
Q

How does the frequency of administration of Neulasta (Pegfilgrastim) compare to that of Neupogen (filgrastim)?

A

1 SC Neulasta 1x/cycle = OD SC Neupogen (filgrastim)

175
Q

What is branded filgrastim called?

A

Neupogen

176
Q

What is Neupogen?

A

Filgrastim branded

177
Q

What is the administration route of Neulasta?

A

SC - 45º

178
Q

What are some potential side effects of Neulasta use?

A
  • spleen rupture
  • Acute Respiratory Distress Syndrome
  • anaphylaxis
179
Q

What is Acute Respiratory Distress Syndrome?

A
  • fever
  • SOB
  • trouble breathing
  • fast breathing rate
180
Q

What is the therapeutic application of Caelyx?

A
  • metastatic breast cancer

- advanced ovarian cancer when platinum drug has been tried already

181
Q

What is the administration route of Caelyx?

A

IV infusion

PM4B - Antonio (28 decks)

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