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31 Cards in this Set

  • Front
  • Back
Advanced Drug Delivery: A therapeutic Systems approach to optimize the timing (temporal control) and location (spatial control) of drug delivery.

(Statement, not a question)
Statement, not a question
Rationale and Incentives for ADR, what are the three?
1) Benefits to the patient
2) Convenience
3) Compliance
Rationale and Incentives for ADR: What are the benifits to the patient?
1) Safety and Efficacy
2) Convenience
3) Compliance
Temporal control of drug delivery. What is it?
Optimizing the TIMING of drug delivery.
In reference to Temporal Control of Drug Delivery, what ar the three objectives?
1) To achieve constant blood levels. I.E. to minimize peaks and troughs in the blood.

2) To accommodate Periodic Changes in the Body--where drug delivery is timed to maximize effects or minimize side effects.

3) To Achieve Bioresponsive Drug Delivery. Where the drug is delivered automatically in response to a biological need.
What is Chronotherapeutics?
Therapeutics based on biological rhythms.

There are several types of rhythms that operate in bodily processes.
Give some examples of bodily processes that are periodic in nature?
1) Endocrine Function
2) Cardiovascular Function
3) Immune Function
4) Cytokinetics
Self-Regulated Systems (Glucose-responsive insulin delivery) is best used in the "To achieve bioresponsive drug delivery"

(statement, not a question)
Statement, not a question.
What is Targeting?
Where the goal of the therapeutic system is to deliver the drug only to where it is needed.
What are some potential target sites?
1) Tissue Site
2) The Cell
3) Intracellular
Descirbe the Ideal Drug Delivery System.
1) Gives proper timing of drug delivery over the period of treatment.

2) Delivers the drug only to the site of action
Descirbe the Available and Experimental Theraperutic Systems.
1) Polymeric and Mechanical Devices: Intravenous, Oral, Transdermal, Subdermal, Intrauterine, Ophthalmic.

2) Carriers: A) Particles (Liposomes and microspheres) and B) Soluble Macromolecules (antibodies and other proteins).
Why are polymers for therapeutic systems important?
They are critical for most of advanced drug delivery:

1) They control the rate of drug release from the system (drug travels through pores in the polymer)

2) They are currently used in most routes of administration
Mass Transfer Across Polymers. Describe the rate of passage (flux) of the drug through a polymer.
Flux = (area/length) x (permeability) x (concentration deifference)

Permeability = (partition coefficient) x (diffusivity)
Flux = rate of transport through the polymer
Area = area in contact with the environment
Length = polymer thickness
Permeability = a function of drug/polymer interaction
Concentration difference = concentration gradient across the polymer
Partition Coefficient = solubility in external medium/solubility in polymer
Diffusivity = how well the drug can diffuse through the polymer

(this is not a question)
(not a question)
What are the three main mathematical models that apply to drug release from polymer systems?
1) Zero-Order Release
2) First-Order Release
3) Square-root-of-time release
Descirbe Zero-Order Release.
Release rate remains constant until the device is exhausted of active agent.
Describe First-Order Release.
Release rate is proportional to the mass of active agent contained within the device. Generally not important for controlled release.
Describe Square-root-of-time release.
Release rate is linear with the square roote of time and remains finite as the system approached exhaustion. Very important for controlled release.
Know the equations and the graph, page 3-4 of the notes.
Know the equations and the graph, page 3-4 of the notes.
Which plot depict steady, prolonged drug release rates?
t^1/2 (square-root-of-time)
What is a diffusion device?
Diffusion through polymer determines release.
Diffusion Device: Describe the resevoir.
Where diffusion from a saturated resevoir is controlled by polymer membrane.

A) Initial high release from membrane
B) Constant release when depot concentration is constant
C) Release rapidly decline as device rapidly approaches exhaustion
Diffusion Device: Describe the Matrix.
Unifromly dispersed drug diffuses thorugh a polymer matrix.

Fluid enters and dissolves the drug in the outer areas. The dissovled drug leaves, creating a ghost (empty) matrix, which continously expands (i.e. path length increases) over time. Square root of time release.
Describe solvent-controlled osmotic release.
Osmotic pressure governs the release.
What type of osmotic release device are focusing on?
Ones with Flexible Compartment.
Describe the mechanics of the Flexible Compartment.
Water is drawn in by osmosis, because an osmotic agent (NaCl) is inside.

Drug is forced through a laser-drilled hole and is released in a precisely controlled fashion.

Note: dry release is nearly zeri-order.
Note: the "flexible membrane" may look totally different from the above picture

(not a question)
Statement, not a question.
Describe the Solvent-controlled Swelling type of release.
The drug is uniformly dispersed in a polymer matrix. Release is governed by the swelling of the matrix in biological fluids.

As matrix swells, pore size increase, as does flux.
Describe the Solvent-controlled chemical controlled release.
Bioerodible polymers. The drug is uniformly dispersed in a polymer matrix. The matrix degrades in biological fluids, usually by hydrolysis of the polymer.
Different factors can control the drug release. Such as...?
Boerodible: drug can be released as matrix degrades AND by diffusion through intact matrix.