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DRUG (Drug Types (Partial Agonist, Competitive Antagonist, Full Agonist,…

- - - - the inhibitory concentration for 50% inhibition
    - - the lethal dose that kills 50% of the sample population
    - - the effective concentration of agonist for 50% response
- - - - polymer particle
      - hydrogel particle
      - dendrimer
      - protein-drug conjugate
      - metal particle
      - liposome
      - Carbon nanotube
      - solid-lipid hybrid particle
    - - sphere
      - star
      - plate
      - rod
      - cube
    - - Surface functional group
      - surface charge
      - PEGylation or other coatings
      - targeting ligand (antibody, peptide, aptarmer)
- - - - Formulation, stability scale-up synthesis, chronic safety in animals
      - company files investigational new drug (IND) application with FDA
      - Chemicals tested for efficacy and safety in tubes and animals. Results used to choose drug candidate
      - Novel chemicals synthesized
      - Research team formed and objectives set
    - - Phase II
        
        Testing of drug on patients to assess efficacy and side effects in small scale
      - Phase I:
        
        Testing of drug on healthy volunteers for safety, involves testing multiple doses
      - Phase III
        
        Testing of drug on patients to assess efficacy, effectiveness and safety in large scale
      - Phase IV
        
        Market Approval. This phase is the most significant one due to the population effect.
- - - - Multidrug Resistance (MDR)
        
        Increased drug efflux
        
        Drug modification
        
        Decreased drug influx
        
        Target Modification
        
        DNA repair and blocked programmed cell death
        
        Mutational response and selection
- - - - Route of administration
        
        Sublingual delivery
        
        Oral delivery
        
        Buccal delivery
        
        Intravenous delivery
        
        Ocular deliver
        
        intramuscular delivery
        
        Subcutaneous delivery
        
        Transdermal deliver
        
        Pulmonary/Nasal delivery
        
        Vaginal/rectal deliver
  - - - Connective
        
        Extracellular Matrix: Abundant amount
        
        Main Functions: Support and protection of tissues/organs
        
        Cells: Several types of fixed and wandering cells
        
        Muscle
        
        Extracellular Matrix: Moderate amount
        
        Main Functions: Strong contraction; body movements
        
        Cells: Elongated contractile cells
        
        Epithelial
        
        Extracellular Matrix: Small Amount
        
        Main Functions: Lining of surface or body cavities; glandular secretion
        
        Cells: Aggregated polyhedral cells
        
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        Nervous
        
        Extracellular Matrix: Very small amount
        
        Main Functions: Transmission of nerve impulses
        
        Cells: Elongated cells with extremely fine processes
  - - - Diffusion
      - Transport barriers
      - Extracellular Matrix
- - - - Connective
      - Epithelia:
      - Muscle
      - Nervous
  - - - Depending on the target tissue and receptor, each of the 11 organ systems possess unique challenges
      - Dependent on the route of administration
  - - - Directly responsible for the absorption phase in PK ADME
      - Associated with the route of administration
  - - - Cell and Molecular Level
        
        Diffusion Barriers
        
        Transport Barriers
        
        Extracellular Matrix Barriers
- - - - BBB supporting systems
        
        endothelial cells
        
        extracellular base membrane
        
        brain capillary
        
        adjoining pericytes
        
        astrocytes
        
        microglia
- - - - efflux pumps
      - receptor-mediated transcytosis (RMT)
      - transport proteins
      - Adsorptive transcytosis (AMT)
      - transcellular lipophilic pathway: small lipid soluble substances
      - Cell mediated transcytosis
      - Paracellular aqueous pathway: small water-soluble molecules