Tocotrienol Nanoparticle Formulations for Targeted Cancer Delivery

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Solution Overview

Problem

Current drug delivery methods for Vitamin E compounds, such as tocotrienol, fail to effectively target and deliver a therapeutic amount to specific areas in mammals, particularly for cancer treatment, due to inefficiencies in existing delivery methods.

Innovation Solution

Development of pharmacological compositions comprising nanoparticles with a mean diameter of less than 1000 nm, containing a therapeutic amount of tocotrienol, a non-tocotrienol lipid, and a surface active agent, which are designed to enhance targeted delivery through specific formulations and delivery methods like intravenous, intraperitoneal, subcutaneous, ocular, oral, transdermal, and inhalation routes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional drug delivery methods are used for Vitamin E compounds, then the delivery system is simple, but the therapeutic amount cannot be effectively delivered to targeted areas

Engineering Contradiction:
Improvetherapeutic amount of tocotrienolVSAvoiddelivery system complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The delivery system is segmented into nanoparticles with specific size ranges (mean diameter less than 1000 nm, preferably less than 400 nm or 250 nm). This segmentation enables targeted delivery to specific areas while maintaining therapeutic efficacy, resolving the contradiction between delivering sufficient therapeutic amount and keeping the system manageable.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent uses composite nanoparticle formulations containing tocotrienol, non-tocotrienol lipids, and surface active agents. This composite approach allows the delivery system to achieve both targeted delivery capability and therapeutic effectiveness simultaneously, overcoming the limitation of conventional simple delivery methods.

Inventive Principle:
Principle #40Composite materials

2Manufacturing precision

If nanoparticle formulations with small mean diameter are used, then targeted delivery is enhanced, but manufacturing precision requirements increase

Engineering Contradiction:
Improveparticle size controlVSAvoidtargeted delivery effectiveness
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

The patent specifies precise parameter ranges for nanoparticle formulation, including mean diameter (less than 1000 nm, preferably less than 400 nm or 250 nm), polydispersity index (below 0.3), and specific weight ratios of components. These controlled parameters ensure both manufacturing feasibility and reliable targeted delivery effectiveness.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality control by specifying different requirements for different aspects of the nanoparticle system: size distribution (polydispersity below 0.3) for uniformity, specific diameter ranges for targeted delivery, and component ratios for stability. This localized quality approach balances manufacturing precision with delivery reliability.

Inventive Principle:
Principle #3Local quality

3Quantity of substance

If high concentration of tocotrienol is delivered, then therapeutic efficacy is improved, but stability of the composition decreases

Engineering Contradiction:
Improvetocotrienol concentrationVSAvoidcomposition stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent formulates tocotrienol with non-tocotrienol lipids and surface active agents in specific ratios (sum of tocotrienol and non-tocotrienol lipid weight equivalent to or greater than the weight of surface active agent). This composite formulation maintains high tocotrienol concentration for therapeutic efficacy while ensuring composition stability through the stabilizing effects of the other components.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent controls the physical and chemical parameters of the formulation, including maintaining specific weight ratios of components and controlling particle size, to achieve a balance between high tocotrienol concentration and composition stability. The specified parameter ranges ensure both therapeutic efficacy and stability over time.

Inventive Principle:
Principle #35Parameter changes

4Adaptability or versatility

If multiple delivery routes are available, then versatility is improved, but selection and optimization complexity increases

Engineering Contradiction:
Improvedelivery route optionsVSAvoidformulation optimization complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The nanoparticle formulation is designed with universal characteristics that enable it to be administered through multiple routes (intravenous, intraperitoneal, subcutaneous, ocular, oral, transdermal, and inhalation). The standardized nanoparticle structure with controlled size and composition provides multi-functionality, allowing the same formulation to work across different delivery routes without requiring separate optimization for each route.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentUS9180113B2Tocotrienol compositions
Publication Date: 2015.11.10 FIRST TECH INT
  • US9180113B2 patent drawing
  • US9180113B2 patent drawing
  • US9180113B2 patent drawing

AI summary

Compositions containing tocotrienol, non-tocotrienol lipids and surface active agents; compositions containing particles having a statin and a tocotrienol wherein the particle size is less than 1000 nm; and microemulsions containing a statin and a tocotrienol are disclosed. Methods relating to the creation of such compositions and the use of such compositions are further disclosed.