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Liposomas 3
Liposomas 3
Liposomas 3
Hydrophobic
Cell Membrane
Uses of Liposomes
Chelation therapy for treatment of heavy metal
poisoning
Enzyme replacement
Diagnostic imaging of tumors
Cosmetics
Study of membranes
Drug Delivery
Why Use Liposomes in Drug
Delivery?
Drug Targeting
Inactive: Unmodified liposomes gather in specific tissue
reticuloendothelial system
Active: alter liposome surface with ligand (antibodies,
enzymes, protein A, sugars)
Physical: temperature or pH sensitive liposomes
Directly to site
Why Use Liposomes in
Drug Delivery?
Pharmokinetics - efficacy and toxicity
Changes the absorbance and biodistribution
Deliver drug in desired form
Multidrug resistance
Protection
Decrease harmful side effects
Change where drug accumulates in the body
Protects drug
Why Use Liposomes in
Drug Delivery?
Release
Affect the time in which the drug is released
Immuno Cationic
Liposomes Help Improve
Therapeutic index
Rapid metabolism
Unfavorable pharmokinetics
Low solubility
Lack of stability
Irritation
Custom design
Lipid content
Size
Surface charge
Method of preparation
Current liposomal drug
preparations
Type of Agents Examples
Anticancer Drugs Duanorubicin, Doxorubicin*, Epirubicin
Methotrexate, Cisplatin*, Cytarabin
Anti bacterial Triclosan, Clindamycin hydrochloride,
Ampicillin, peperacillin, rifamicin
Antiviral AZT
DNA material cDNA - CFTR*
Enzymes Hexosaminidase A
Glucocerebrosidase, Peroxidase
Radionuclide In-111*, Tc-99m
Fungicides Amphotericin B*
Vaccines Malaria merozoite, Malaria sporozoite
Hepatitis B antigen, Rabies virus glycoprotein
*Currently in Clinical Trials or Approved for Clinical Use
CFTR
Gene Therapy
Deliver cDNA of Cystic Fibrosis Transmembrane Conductance
Regulator (CFTR) to epithelial tissue of respiratory system
Cationic liposome
Fuse to cell membrane and
incorporate cDNA into cell
Clinical trials - no significant
change in symptoms
Systemic fungal
infections in immune compromised patients
Lipid
Garrett, R. and Grisham C. Biochemistry, 2nd ed. Saunders Colleges Publishing. New York (1999). 264.