How Special Nanoparticles Deliver Cancer Drugs Directly to Tumors

This patent describes tiny fat-based particles, called lipid nanoparticles, designed to carry cancer drugs directly to tumor cells using a special protein (ApoE3) on their surface, avoiding a common, potentially problematic ingredient.

What it covers

This patent describes a tiny, engineered package called a lipid nanoparticle for delivering therapeutic agents. This nanoparticle has a core made of fats like cholesterol ester and triglycerides (Claim 1, 4), surrounded by a phospholipid layer. A key feature is the human recombinant ApoE3 protein bonded to its surface (Claim 1), which acts like a guide to target specific cells. Importantly, this ApoE3 bonding happens without using Polysorbate 80 (Claim 1), an ingredient sometimes associated with adverse reactions. The nanoparticle is precisely sized (between 20 and 150 nm) and has specific electrical and uniformity properties (Claim 1). For example, it can carry an anticancer drug like Docetaxel (Claim 10) and deliver it more effectively to cancer cells, showing a lower IC50 and higher selectivity compared to the drug's original formulation (Claim 10, 11).

What it doesn't cover

• —Lipid nanoparticles that use Polysorbate 80 to bond ApoE3 to their surface (Claim 1).
• —Nanoparticles outside the specified size range of 20 to 150 nanometers (Claim 1).
• —Nanoparticles with a Z-potential outside the range of -25 to -5 millivolts (Claim 1).
• —Nanoparticles with a PDI dispersion value outside the range of 0.08 to 0.30 (Claim 1).
• —Drug delivery systems that do not incorporate human recombinant ApoE3 as the apolipoprotein component (Claim 1).
• —Nanoparticles where the therapeutic agent is not dissolved within the lipid core (Claim 7).

The clever bit

The clever aspect is the precise engineering of a lipid nanoparticle that incorporates human recombinant ApoE3 on its surface for targeted delivery, specifically ensuring this attachment occurs without the use of Polysorbate 80. This combination aims to enhance drug efficacy and reduce formulation-related side effects.

Why it matters

Targeted drug delivery is a critical area in medicine, especially for cancer treatment, as it aims to increase drug effectiveness while reducing harmful side effects on healthy tissues. This patent offers a method to improve the delivery of potent drugs like Docetaxel by making them more selective for cancer cells. The specific exclusion of Polysorbate 80 addresses a known formulation challenge, potentially leading to safer and more effective drug products.

Real-world examples

• 1.Targeted chemotherapy formulations for various cancers
• 2.Improved drug delivery systems for potent anticancer drugs
• 3.Nanoparticle-based therapies designed to cross biological barriers