Rapamycin Crystalline Surface Drug Delivery Composition

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Oral administration of rapamycin suffers from poor bioavailability and fluctuating peak and trough blood levels, leading to adverse toxic effects due to dose-dependent immunosuppressive requirements, necessitating a stable therapeutic window.

Innovation Solution

A drug delivery composition comprising a bioabsorbable polymer and rapamycin in crystalline form, designed for controlled release, utilizing techniques such as cluster SIMS, TOF-SIMS, AFM, X-ray spectroscopy, and Raman spectroscopy to optimize surface active agent content and release profiles, suitable for injection into various sites for targeted therapy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration of rapamycin is used, then the drug can be administered conveniently, but the bioavailability is poor and blood levels fluctuate

Engineering Contradiction:

Improveadministration convenienceVSAvoidbioavailability and blood level stability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The drug delivery system segments the rapamycin release into multiple phases using a core-shell structure with inner and outer polymer layers, each controlling different aspects of drug release to achieve stable blood levels

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent introduces polymer matrices (PLGA, PLA, PGA) as intermediary carriers that control drug release kinetics, replacing direct oral absorption with controlled polymer-mediated release to stabilize blood levels

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If dose-dependent immunosuppressive therapy is required, then therapeutic effectiveness is achieved, but adverse toxic effects occur when blood levels are too high

Engineering Contradiction:

Improveimmunosuppressive effectivenessVSAvoidadverse toxic effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The controlled release system provides feedback-controlled drug delivery where the polymer degradation rate and drug release rate are coupled, automatically adjusting release to maintain therapeutic levels without toxic peaks

Inventive Principle:

Principle #23Feedback

Solution Approach 2:

The patent changes the physical and chemical parameters of drug delivery by using crystalline versus amorphous rapamycin forms and different polymer compositions to precisely control release kinetics and maintain blood levels within the therapeutic window

Inventive Principle:

Principle #35Parameter changes

3Reliability

If rapamycin is administered to maintain therapeutic blood levels, then immunosuppression is effective, but fluctuating peak and trough levels cause toxicity

Engineering Contradiction:

Improvetherapeutic blood level maintenanceVSAvoidblood level stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The implant provides continuous drug release over extended periods (weeks to months) through controlled polymer degradation, eliminating the fluctuating peak-trough pattern of conventional dosing and maintaining steady therapeutic levels

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The drug is pre-loaded into the polymer matrix in a controlled manner during manufacturing, with the release profile predetermined by the polymer structure and composition before implantation

Inventive Principle:

Principle #10Preliminary action

Data Source

PatentUS10293050B2Macrolide dosage forms

Publication Date: 2019.05.21 MICELL MEDTECH INC

AI summary

Provided is a drug delivery composition comprising at least one polymer and at least one active agent; wherein the active agent is present in crystalline form on at least one region of an outer surface of the composition and wherein active agent surface content is adjusted to provide a selected active agent release profile.