Injectable Letrozole Depot via Biodegradable PLA Polymer
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Solution Overview
Problem
Current formulations of letrozole for cancer treatment are limited by the need for daily oral administration, which can negatively impact the quality of life for patients and are not suitable for long-term hormone suppression.
Innovation Solution
A letrozole composition suitable for forming an in situ intramuscular implant using a sterile biodegradable thermoplastic polymer of polylactic acid (PLA), allowing for controlled release of letrozole over a period of at least three months.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If daily oral administration of letrozole is used, then therapeutic effect is maintained, but patient quality of life is negatively impacted and treatment burden increases
Solution Approach 1:
The patent applies preliminary action by pre-forming the letrozole implant before administration. The implant is prepared in advance with controlled release properties, then injected into the patient's muscle tissue. This preliminary preparation allows the drug to be released gradually over time without requiring daily patient intervention, thus maintaining therapeutic effect while improving quality of life.
Solution Approach 2:
The patent implements continuity of useful action through the controlled release mechanism of the implant. The implant continuously releases letrozole over an extended period (months), maintaining steady therapeutic levels in the patient's body without interruption. This eliminates the need for daily dosing while ensuring consistent therapeutic effect throughout the release period.
2Loss of time
If preformed implants are used for prolonged release, then administration frequency is reduced, but high temperatures during preparation cause degradation of active ingredient and generation of toxic impurities
Solution Approach 1:
The patent replaces the thermal extrusion process with a mechanical mixing and injection approach. Instead of using high temperatures to form the implant, the invention mixes letrozole with a biodegradable polymer matrix at controlled temperatures, forms the implant through mechanical means (injection into muscle tissue), and achieves controlled release through the polymer's degradation and diffusion properties. This substitution eliminates thermal degradation while maintaining prolonged release functionality.
3Duration of action of stationary object
If preformed implants are used, then prolonged release is achieved, but surgical procedures with large diameter needles are required for implantation
Solution Approach 1:
The patent applies parameter changes by modifying the physical and chemical properties of the implant formulation to enable minimally invasive administration. The implant is formulated with specific viscosity, particle size distribution, and biodegradable polymer characteristics that allow it to be injected through small-gauge needles. The controlled release parameters are adjusted to ensure sustained drug delivery while maintaining compatibility with minimally invasive injection techniques, thereby reducing surgical procedure complexity.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition provides sustained therapeutic plasma levels of letrozole for hormone suppression, reducing adverse side effects and improving patient quality of life by eliminating the need for daily dosing.
Implementation Method 1
a sterile biodegradable thermoplastic polymer of polylactic acid (PLA)
Implementation Method 2
thermoplastic polymer of polylactic acid (PLA)
Data Source
AI summary
An injectable depot composition suitable for forming an in situ intramuscular implant is provided. The composition includes sterile biodegradable thermoplastic polymer of polylactic acid (PLA), solvent for the PLA, and drug. After administration to a subject, a corresponding implant administers 0.1-2 milligrams of nonsteroidal aromatase inhibitor every day throughout a dosing period of about six months to about one year. The composition is used to treat subjects in need thereof.