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Liposomal
Delivery Systems
in Cancer
Therapy
Email: info@creative-biolabs.com
Web: www.creative-biolabs.com
CONTENT
2
7. Creative Biolabs’ Liposome Services
& Products
1. Background
2. Introduction of Liposomes
3. Functional Liposome
Development
4. Two Major Methods for
Liposome Drug Loading
5. Liposomal Drug Delivery
System for Cancer Therapy
6. Liposomal Formulations of Anticancer
Drugs in Clinical Trials
3
Background
Cancer is a life-threatening disease, causing approximately 3.4 million deaths
worldwide. The first-line treatment for cancer is the surgical removal of solid tumors,
radiotherapy and chemotherapy. However, these methods have many limitations that
need to be resolved.
• Surgical resection is not suitable for tumors that are invisible or uncertain.
• Radiotherapy effectively destroys cancer cells while also damaging non-cancer cells.
• Most APIs used in chemotherapy are highly cytotoxic to cancer cells and normal cells.
• Some anticancer agents are highly hydrophobic, resulting in low bioavailability.
Targeting the tumor vasculatures is essential for cancer treatment.
Encapsulating anticancer drugs in liposome systems provides a safe platform for
targeted drug delivery for cancer treatment.
4
Liposomes, first discovered by Alee Bangham in 1963, are the most
studied nanostructures for advanced drug delivery. Liposomes are
artificial spherical vesicles prepared from natural phospholipids, and
have one or more lipid bilayers with discrete aqueous spaces. Because
of their amphiphilic properties in aqueous media-unique hydrophilic
heads and hydrophobic tails, they are suitable for a range of
pharmaceutical and biomedical applications. For instance, hydrophobic
compounds enter the double membrane, while hydrophilic compounds
are encapsulated in the water core.
Introduction of Liposomes
Due to their biocompatibility and drug encapsulation ability, liposomes
are a promising nanocarrier for drug delivery.
Nutrient
Hydrophobic tail
nonpolar chains
Hydrophobic head
polar region
Functional
Liposome
Development
(Riaz, 2018)
5
6
Functional
Liposome
Development
Preparation of the
PEGylated DOTAP–DOPE liposomes
and lipoplexes
(Sara P, et al., 2021)
Two Major Methods for Liposome Drug Loading
(Griffin P , et al., 2021)
7
Liposomal Drug
Delivery System
for Cancer
Therapy
(Aleksandra B , et al., 2021)
8
The Advantages of Liposomal Drug Delivery System
• Minimizing targeted therapies and toxic side effects of drugs
• Enhancing the bioavailability of hydrophobic anti-cancer drugs
• Reducing the clearance of anti-tumor drugs by immunity
• Enhancing drug solubility
• Prolonging the systemic circulation time of delivered anti-tumor drugs
• Providing targeted drug delivery
• Improving multidrug-resistance
• Protecting drugs against their surrounding environment
9
Liposomes have a role
10
Product Name Encapsulated Drugs Type of Liposomes Indications Lipid Composition Particle Size (nm) Status
ATI-1123 Docetaxel
Protein stabilized
liposomes
NSCLC, gastric, pancreatic
cancer, and soft tissue
sarcoma
Phospholipids, cholesterol, human
serum albumin, and sucrose
60-80 Phase I
MCC-465 Doxorubicin
Antibody conjugated
PEGylated liposomes
Stomach cancer
DPPC, maleimidated DPPE, PEG,
GAH
143 Phase I
EndoTAG-1 Paclitaxel Cationic liposomes Solid tumors DOTAP, DOPC 180–200 Phase II
LEP-ETU Paclitaxel Anionic liposomes Metastatic breast cancer
DMPC, DOPC, DSPC, cholesterol,
and cardiolipin
100–160 Phase II
CPX-351
Cytarabine and
daunorubicin (5:1)
Bilamellar liposomes Acute myeloid leukemia DSPC, DSPG and cholesterol 100 Phase III
Lipoplatin Cisplatin PEGylated liposomes
NSCLC, gastric, pancreatic,
breast, head and neck
cancers
PC, cholesterol, DPPG, DSPE-
PEG2000Da
110 Phase III
Thermodox Doxorubicin
Lyso-lipid temperature
sensitive liposomes
Hepatocellular carcinoma and
breast cancer
DPPC, MSPC, DSPE-PEG2000Da 175 Phase III
(Phatsapong Y, et al., 2016)
Liposomal Formulations of Anticancer Drugs in
Clinical Trials
 Liposomes
• Clodronate Liposome
• Fluorescent Liposome
• Liposomal Doxorubicin
• Immunoliposomes
 Phospholipids
• Phosphatidic Acid & Lysophosphatidic Acid
• Phosphatidylcholine & Lysophosphatidylcholine
• Phosphatidylethanolamine & Lysophosphatidylethanolamine
• Phosphatidylglycerol & Lysophosphatidylglycerol
• Phosphoinositide & Lysophosphatidylinositol
• Phosphatidylserine & Lysophosphatidylserine
• Cardiolipin
• Ether Lipids
 Other Lipids
Liposome Development Services
Products
Creative Biolabs’ Liposome Services and Products
 Functional Liposome Development Service
• Conventional Liposome
• Long Circulating Liposome
• Stimuli-Responsive Liposome
• Immunoliposome
• Cationic Liposome
• Magnetic Liposome
• Polysaccharide Coated Liposome
 Liposomal Formulation Development Service
• Liposome Encapsulated Small Molecule Drugs
/Protein/Peptide/Prodrug/Nucleic Acids
• Liposome-Based Adjuvant
 Liposome Analysis and Characterization Service
Our custom liposome services can regulate the solubility of
encapsulated small organic molecules, protect the embedded
agents from degradation, and achieve site-specific delivery.
11
12
Email: info@creative-biolabs.com
Web: www.creative-biolabs.com

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Liposomal Delivery Systems in Cancer Therapy - Creative Biolabs

  • 1. Liposomal Delivery Systems in Cancer Therapy Email: info@creative-biolabs.com Web: www.creative-biolabs.com
  • 2. CONTENT 2 7. Creative Biolabs’ Liposome Services & Products 1. Background 2. Introduction of Liposomes 3. Functional Liposome Development 4. Two Major Methods for Liposome Drug Loading 5. Liposomal Drug Delivery System for Cancer Therapy 6. Liposomal Formulations of Anticancer Drugs in Clinical Trials
  • 3. 3 Background Cancer is a life-threatening disease, causing approximately 3.4 million deaths worldwide. The first-line treatment for cancer is the surgical removal of solid tumors, radiotherapy and chemotherapy. However, these methods have many limitations that need to be resolved. • Surgical resection is not suitable for tumors that are invisible or uncertain. • Radiotherapy effectively destroys cancer cells while also damaging non-cancer cells. • Most APIs used in chemotherapy are highly cytotoxic to cancer cells and normal cells. • Some anticancer agents are highly hydrophobic, resulting in low bioavailability. Targeting the tumor vasculatures is essential for cancer treatment. Encapsulating anticancer drugs in liposome systems provides a safe platform for targeted drug delivery for cancer treatment.
  • 4. 4 Liposomes, first discovered by Alee Bangham in 1963, are the most studied nanostructures for advanced drug delivery. Liposomes are artificial spherical vesicles prepared from natural phospholipids, and have one or more lipid bilayers with discrete aqueous spaces. Because of their amphiphilic properties in aqueous media-unique hydrophilic heads and hydrophobic tails, they are suitable for a range of pharmaceutical and biomedical applications. For instance, hydrophobic compounds enter the double membrane, while hydrophilic compounds are encapsulated in the water core. Introduction of Liposomes Due to their biocompatibility and drug encapsulation ability, liposomes are a promising nanocarrier for drug delivery. Nutrient Hydrophobic tail nonpolar chains Hydrophobic head polar region
  • 6. 6 Functional Liposome Development Preparation of the PEGylated DOTAP–DOPE liposomes and lipoplexes (Sara P, et al., 2021)
  • 7. Two Major Methods for Liposome Drug Loading (Griffin P , et al., 2021) 7
  • 8. Liposomal Drug Delivery System for Cancer Therapy (Aleksandra B , et al., 2021) 8
  • 9. The Advantages of Liposomal Drug Delivery System • Minimizing targeted therapies and toxic side effects of drugs • Enhancing the bioavailability of hydrophobic anti-cancer drugs • Reducing the clearance of anti-tumor drugs by immunity • Enhancing drug solubility • Prolonging the systemic circulation time of delivered anti-tumor drugs • Providing targeted drug delivery • Improving multidrug-resistance • Protecting drugs against their surrounding environment 9 Liposomes have a role
  • 10. 10 Product Name Encapsulated Drugs Type of Liposomes Indications Lipid Composition Particle Size (nm) Status ATI-1123 Docetaxel Protein stabilized liposomes NSCLC, gastric, pancreatic cancer, and soft tissue sarcoma Phospholipids, cholesterol, human serum albumin, and sucrose 60-80 Phase I MCC-465 Doxorubicin Antibody conjugated PEGylated liposomes Stomach cancer DPPC, maleimidated DPPE, PEG, GAH 143 Phase I EndoTAG-1 Paclitaxel Cationic liposomes Solid tumors DOTAP, DOPC 180–200 Phase II LEP-ETU Paclitaxel Anionic liposomes Metastatic breast cancer DMPC, DOPC, DSPC, cholesterol, and cardiolipin 100–160 Phase II CPX-351 Cytarabine and daunorubicin (5:1) Bilamellar liposomes Acute myeloid leukemia DSPC, DSPG and cholesterol 100 Phase III Lipoplatin Cisplatin PEGylated liposomes NSCLC, gastric, pancreatic, breast, head and neck cancers PC, cholesterol, DPPG, DSPE- PEG2000Da 110 Phase III Thermodox Doxorubicin Lyso-lipid temperature sensitive liposomes Hepatocellular carcinoma and breast cancer DPPC, MSPC, DSPE-PEG2000Da 175 Phase III (Phatsapong Y, et al., 2016) Liposomal Formulations of Anticancer Drugs in Clinical Trials
  • 11.  Liposomes • Clodronate Liposome • Fluorescent Liposome • Liposomal Doxorubicin • Immunoliposomes  Phospholipids • Phosphatidic Acid & Lysophosphatidic Acid • Phosphatidylcholine & Lysophosphatidylcholine • Phosphatidylethanolamine & Lysophosphatidylethanolamine • Phosphatidylglycerol & Lysophosphatidylglycerol • Phosphoinositide & Lysophosphatidylinositol • Phosphatidylserine & Lysophosphatidylserine • Cardiolipin • Ether Lipids  Other Lipids Liposome Development Services Products Creative Biolabs’ Liposome Services and Products  Functional Liposome Development Service • Conventional Liposome • Long Circulating Liposome • Stimuli-Responsive Liposome • Immunoliposome • Cationic Liposome • Magnetic Liposome • Polysaccharide Coated Liposome  Liposomal Formulation Development Service • Liposome Encapsulated Small Molecule Drugs /Protein/Peptide/Prodrug/Nucleic Acids • Liposome-Based Adjuvant  Liposome Analysis and Characterization Service Our custom liposome services can regulate the solubility of encapsulated small organic molecules, protect the embedded agents from degradation, and achieve site-specific delivery. 11