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US 11,141,383 B1Granted
Drug loaded flexible chitoplexes nanoparticles
AssigneeKing Abdulaziz University
InventorsTarek A. Ahmed, Abdelsattar M. Omar
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Abstract
Chitosan-coated, flexible lipid-based nanoparticles are provided. The nanoparticles (“chitoplexes”) comprise an interior comprising a mixture of a phospholipid, an edge activator, a charge inducing agent, and a statin; and an exterior chitosan coating which encapsulates the interior mixture. The chitoplexes exhibit enhanced bioavailability with respect to delivering the statins encapsulated therein to a subject, for example, for the treatment of cancer.
Claims9
A flexible chitosan-coated formulation, comprising
- an interior comprising
- at least one phospholipid,
- at least one edge activator,
- at least one charge inducing agent, and
- at least one statin, wherein the at least one statin is rosuvastatin, and
- an exterior coating of chitosan that encapsulates the interior,
- wherein
- the at least one phospholipid is present in an amount of from 1:1-1:4 statin to phospholipid molar ratio;
- the at least one edge activator is present in an amount of from 0.01-0.04% (w/v) based on the total formulation volume;
- the at least one charge inducing agent is present in an amount of 10 to 20% w/w of the total lipid;
- the at least one statin is present in an amount of 0.01 to about 0.5% (w/v), and
- the chitosan is present in an amount of 0.4-0.6% (w/v) to provide an entrapment efficiency of at least 80%, a zeta potential of −15 to +30 millivolts, and an IC50 of about 142.5 μM for cell viability at 24 hours after treatment of colorectal cancer cells,
- wherein a diameter of the flexible chitosan-coated nanoparticle ranges from 100 to 600 nm.
10 more elements
A method of making a flexible chitosan-coated formulation, comprising
- preparing a liposomal interior comprising
- at least one phospholipid,
- at least one edge activator,
- at least one charge inducing agent, and
- rosuvastatin,
- and
- coating the liposomal interior with an exterior coating of chitosan that encapsulates the interior,
- wherein
- the at least one phospholipid is added in an amount of from 1:1-1:4 rosuvastatin to phospholipid molar ratio;
- the at least one edge activator is added in an amount of from 0.01-0.04% (w/v) based on the total formulation volume;
- the at least one charge inducing agent is added in an amount of 10 to 20% w/w of the total lipid;
- the rosuvastatin is added in an amount of 0.01 to about 0.5% (w/v), and
- the chitosan is added in an amount of 0.4-0.6% (w/v) to provide an entrapment efficiency of at least 80%, a zeta potential of −15 to +30 millivolts, and an IC50 of about 142.5 μM for cell viability at 24 hours after treatment of colorectal cancer cells,
- wherein a diameter of the flexible chitosan-coated nanoparticle ranges from 100 to 600 nm.
11 more elements
Dependencies are inferred from the claim text.