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Platinum-based Dual Loaded Liposomal Formulations

Technology #inv233022016

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Researchers
Tamer Shoeib, Associate Professor Department of Chemistry.
Ayat Zein-El Abedeen, Masters student.
Managed By
Ahmed Ellaithy
Director, Technology Transfer +20226153112
Ingy Darwish
Licensing Officer +20226153130
Patent Protection

Provisional Patent Application Filed

Application

Platinum-based dual loaded liposomal formulations (Oxaliplatin + Satraplatin)  and (Oxaliplatin + Ascorbic Acid) as anti-neoplastic agents for the treatment of colon and rectal cancer.


Problem

Cancer is one of the rapidly growing leading causes of death worldwide where combinational chemotherapy is the most used strategy to control it.

While approximately 65% of all cancer patients worldwide receive Platinum-based chemotherapy, typically only a small fraction (3-7%) of the administered agent reaches its intended target (the DNA in the nucleus of a cancer cell).  This leads to significant reactions with several non-intended targets reducing therapeutic efficacy and causing unpredictable side effects as well as causing high variability in patient response.

Novel drug delivery vehicles are needed to help minimize the interactions of the chemotherapeutic drugs with other non-intended targets.


Technology

Stable liposomal formulations under 200 nm in size were formulated that offer high encapsulation efficiency for Oxaliplatin. These liposomal formulations were used as dual drug loading delivery vehicles for Oxaliplatin and Ascorbic acid (LP-Ox-AA), and Oxaliplatin combined with Satraplatin as a chemotherapeutic agent (LP-Ox-Stp).


The combination of oxaliplatin with chemo-sensitizing agent ascorbic acid in the formulated liposome enhanced the cytotoxic profile of oxaliplatin towards cancer cells. Ascorbic acid also helped improve the encapsulation efficiency (28.5%) and the stability profile of oxaliplatin in the dual loaded liposome. The liposomal encapsulation of ascorbic acid had a stabilizing influence on ascorbic acid upon long-term storage at 4°C.  In addition, the developed liposomal system was capable of encapsulating hydrophobic satraplatin at high levels (49.3%).


The second liposome (LP-Ox-Stp) showed the most efficient controlled release profile, mainly due to the incorporation of hydrophobic satraplatin within the lipid bilayer. LP-Ox-Stp was the most potent in DNA damage induction, even relative to the commercial Lipoxal formulation.


The formulated liposomes were shown to act as successful drug delivery systems for single and combinational chemotherapy .


Advantages

  • Highly stable for 6 months at 4°C maintaining size and particle surface charge.

  • Enhance the cytotoxic efficiency and minimize drug toxicity.


Stage of Development

In-vitro testing on BHK-21, MCF-7 and HepG2