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Lipid nanoparticles containing pharmaceutical and/or nutraceutical agents and methods thereof

A nanoparticle, unsaturated fatty acid technology, applied in the field of nanoparticles, can solve problems such as active compound delivery

Pending Publication Date: 2022-03-04
BOARD OF RGT THE UNIV OF TEXAS SYST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present disclosure solves the problems in the art regarding in vivo delivery of active compounds by providing nanoparticles and methods of using nanoparticles to efficiently deliver one or more active compounds to target tissues

Method used

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  • Lipid nanoparticles containing pharmaceutical and/or nutraceutical agents and methods thereof
  • Lipid nanoparticles containing pharmaceutical and/or nutraceutical agents and methods thereof
  • Lipid nanoparticles containing pharmaceutical and/or nutraceutical agents and methods thereof

Examples

Experimental program
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example 1

[0174] Example 1. Solid lipid nanoparticle formulation of 4-(N)-docosahexaenoyl 2',2'-difluorodeoxycytidine with potent broad-spectrum antitumor activity.

[0175] The present example discloses a solid lipid nanoparticle (SLN) formulation comprising DHA-dFdC with improved apparent water solubility and chemical stability. SLN further comprised a lecithin / glyceryl monostearate emulsion in water emulsified with D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) and Tween 20. The resulting DHA-dFdC-SLN has a diameter of 102.2 ± 7.3 nm and increases the solubility of DHA-dFdC in water to at least 5.2 mg / mL, more than 200 times higher than its intrinsic water solubility. In comparison, the waxy solid of DHA-dFdC was unstable when stored at room temperature even in the presence of vitamin E as an antioxidant. However, DHA-dFdC in the lyophilized DHA-dFdC-SLN powder was not significantly degraded after one month of storage under the same conditions. DHA-dFdC-SLN also exhib...

example 2

[0213] Example 2. Oral SLN formulations with improved DHA-dFdC bioavailability.

[0214] Certain nanocarriers (e.g., SLNs, liposomes, nanoemulsions, micelles, and polymeric nanoparticles) improve drug resistance by increasing apparent drug solubility, reducing drug degradation in the gastrointestinal tract, and / or improving drug absorption. Oral delivery of cancer drugs, thus gaining some attention (Date, et al., J. Controlled Release, 2016, 240, 504-526; Thanki, et al., J. Controlled Release 2013, 170, (1), 15-40; Lin , et al., J. Food Drug Analysis, 2017, 25, (2), 219-234). This example discloses that DHA-dFdC-SLN surprisingly enables oral administration of a highly lipophilic compound, DHA-dFdC.

[0215] Materials and methods

[0216] Materials and cell lines. Mannitol, Tween 20, GMS, TPGS, sodium chloride (NaCl), hydrochloric acid (HCl, 37%), potassium dihydrogen phosphate (KH 2 PO 4 ), sodium hydroxide (NaOH), and Tween 80 were from Sigma-Aldrich (St. Louis, MO). Ge...

example 3

[0244] Example 3. Additional SLN formulations.

[0245] DHA-dFdC with different concentrations of TPGS

[0246] DHA-dFdC (5 mg), 3.5 mg soybean lecithin, 0.5 mg glyceryl monostearate and different amounts (0.4375 mg, 0.875 mg or 1.75 mg) of TPGS were mixed and dispersed in 800 μl deionized and filtered (0.22 μm) in hot water (80°C). The mixture was vortexed, sonicated for 10 min, and then kept on a hot plate at 80 °C while stirring at 800 rpm for 5 min. Separately, 55 mg of Tween 20 was dissolved in 1 ml of hot water, and 200 ml of this solution was added dropwise to the mixture until the final concentration was 1% (v / v) Tween 20. The emulsion was cooled to room temperature while stirring to form nanoparticles.

[0247] The particle diameter, polydispersity index (PDI) and zeta potential of the nanoparticles were determined using a Malvern Zeta Sizer Nano ZS (Westborough, MA). The results are summarized in Figures 12A-12C and Table 5. Nanoparticles prepared with 0.4375m...

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Abstract

Disclosed are nanoparticles comprising: an active compound, or a pharmaceutically acceptable salt or prodrug thereof, the active compound comprising a nucleobase analog moiety covalently linked to an omega-3 polyunsaturated fatty acid moiety; a pegylated vitamin E compound; and at least one oil phase component. Also disclosed are methods for treating a subject having a disease comprising administering to the subject a therapeutically effective amount of the disclosed nanoparticles. The compositions and methods are useful for the treatment of diseases, such as tumors, by delivering a range of active compounds, including, for example, 4-(N)-docosahexaenoyl 2 ', 2'-difluorodeoxycytidine (DHA-dFdC) or other hydrophobic and / or lipophilic anti-cancer agents. The compositions and methods are further useful for delivering pharmaceutical agents and / or nutritional agents via a variety of routes of administration. Methods of making the nanoparticles are also disclosed.

Description

[0001] Statement Regarding Federally Sponsored Research [0002] This invention was made with support under Government Grant No. CA179362 awarded by the National Institutes of Health. The government has certain rights in this invention. technical field [0003] The present disclosure relates generally to nanoparticles, more particularly lipid-based nanoparticles and / or solid lipid nanoparticles, particularly nanoparticles that can incorporate and deliver pharmaceutical and / or nutraceutical agents. In some embodiments, nanoparticles are well suited for the incorporation and delivery of omega-3 fatty acids, nucleoside analogs, and / or derivatives thereof that are useful in some instances as anticancer therapeutics. Nanoparticles generally enable controlled and sustained release of these beneficial agents, deliver the agent to desired tissues, such as tumors, and generally increase the water solubility and bioavailability of the agent, thereby stabilizing and increasing the amoun...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/70A61K47/14A61K47/55A61K9/51
CPCA61K31/7068A61K47/542A61K47/6929A61P35/00A61K47/34A61K9/0053A61K47/26A61K9/1641A61K47/14
Inventor 崔正荣索朗热·瓦尔德斯
Owner BOARD OF RGT THE UNIV OF TEXAS SYST
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