PLA:PLGA Implant for Linear Risperidone Release

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Solution Overview

Problem

Current methods for administering anti-schizophrenia medications, such as risperidone, provide dosing for only a month or less, leading to medication noncompliance and relapse in schizophrenia patients, necessitating a solution for maintaining therapeutic drug levels over an extended period.

Innovation Solution

Biodegradable implants comprising a therapeutic drug and a polymer mixture of polylactic acid (PLA) and optionally polyglycolic acid (PGA) are used, with a PLA:PGA molar ratio between 50:50 and 100:0, to release the drug at a substantially linear rate, maintaining therapeutic levels for at least one month and potentially up to a year through initial and maintenance implant sets.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If current dosing methods are used, then dosing frequency is manageable, but therapeutic drug levels cannot be maintained over extended periods

Engineering Contradiction:
Improveduration of therapeutic drug level maintenanceVSAvoiddosing frequency
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The invention segments the drug delivery system into biodegradable polymer implants that release drug molecules progressively over time. The implant is divided into a polymer matrix containing the therapeutic agent, which segments the delivery function from traditional periodic dosing into continuous localized release, maintaining therapeutic levels for extended periods without frequent administration.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The drug is pre-loaded into the biodegradable implant before administration. The implant is prepared in advance with the therapeutic agent embedded in the polymer matrix, so that upon implantation, the drug release begins automatically without requiring subsequent dosing actions by the patient or provider.

Inventive Principle:
Principle #10Preliminary action

2Reliability

If dosing interval is extended, then patient compliance improves, but maintaining consistent therapeutic levels becomes difficult

Engineering Contradiction:
Improveconsistency of therapeutic drug levelsVSAvoiddosing interval
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The invention changes the physical and chemical parameters of the drug delivery system by using biodegradable polymers with controlled degradation rates. By adjusting polymer composition, molecular weight, and cross-linking density, the drug release kinetics are optimized to maintain consistent therapeutic levels over extended intervals, solving the reliability problem of extended dosing schedules.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If frequent dosing is required, then therapeutic levels can be maintained, but medication noncompliance increases

Engineering Contradiction:
Improvemedication adherenceVSAvoiddosing frequency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The biodegradable implant performs self-service by automatically releasing the therapeutic agent over time without requiring patient intervention. The polymer matrix degrades progressively, releasing drug molecules at controlled rates, thereby eliminating the need for frequent patient dosing actions and significantly improving medication adherence.

Inventive Principle:
Principle #25Self-service

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 implants effectively maintain therapeutic drug levels for extended periods, improving medication adherence and clinical outcomes by providing a long-term delivery system that ensures consistent drug release, reducing the need for frequent dosing and enhancing patient compliance.

Implementation Method 1

biodegradable implant comprising (a) a therapeutic drug present in an amount of 10%-60% by mass, relative to the mass of the implant; and (b) a polymer present in an amount of 40%-90% by mass, relative to the mass of the implant, the polymer comprising PLA and optionally PGA

Methodology Applied
Scientific EffectBiodegradation: Decomposition (biological)

Data Source

PatentUS8741327B2Method of maintaining therapeutic risperidone levels in a PLA:PLGA implant
Publication Date: 2014.06.03 THE TRUSTEES OF THE UNIV OF PENNSYLVANIA
  • US8741327B2 patent drawing
  • US8741327B2 patent drawing
  • US8741327B2 patent drawing

AI summary

The present invention provides implants comprising a therapeutic drug and a polymer containing polylactic acid (PLA) and optionally polyglycolic acid (PGA). The present invention also provides methods of maintaining a therapeutic level of a drug in a subject, releasing a therapeutic drug at a substantially linear rate, and treating schizophrenia and other diseases and disorders, utilizing implants of the present invention.