Tacrolimus Buccal Mucoadhesive Patches for Controlled Release

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Solution Overview

Problem

Tacrolimus administration poses challenges due to poor bioavailability, erratic absorption, and high toxicity risks, particularly in patients with altered consciousness, oropharyngeal dysphagia, intestinal obstruction, or paralytic ileus, where oral and intravenous routes are problematic, necessitating a safe and efficient drug delivery system.

Innovation Solution

A buccal mucoadhesive patch formulation of tacrolimus using solid lipid nanoparticles (SLNs) in a polymeric matrix for transbuccal administration, providing both immediate and controlled release, avoiding first-pass metabolism and ensuring stable systemic concentration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral tacrolimus tablets are compounded and administered through NG tube, then tacrolimus can be delivered to patients with altered consciousness or intestinal obstruction, but the lipophilic compound gets adsorbed onto the PVC NG tube causing erratic bioavailability and low tacrolimus concentration

Engineering Contradiction:

Improveability to administer to patients with altered consciousnessVSAvoidbioavailability consistency

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses a mucoadhesive patch as an intermediary delivery system that adheres to the buccal mucosa, providing a reliable alternative route that avoids the adsorption problem with NG tubes while maintaining ease of administration in patients with altered consciousness

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If oral tacrolimus is administered to patients with acute diarrhoea, then the drug can be delivered, but rapid absorption through denuded intestinal mucosa leads to higher than intended peak concentration and increased toxicity risk

Engineering Contradiction:

Improveability to deliver drug orallyVSAvoidnephrotoxicity risk

Core Design Contradiction:

Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the drug delivery from the problematic intestinal route and relocates it to the buccal mucosa, thereby avoiding the harmful rapid absorption that occurs in patients with diarrhoea and denuded intestinal mucosa

Inventive Principle:

Principle #2Taking out (Extraction)

3Speed

If intravenous tacrolimus is administered to achieve therapeutic levels, then the drug can be delivered directly to systemic circulation, but high concentration bolus infusions may lead to dysrhythmias, QT prolongation, neurotoxicity, and nephrotoxicity

Engineering Contradiction:

Improverate of drug delivery to systemic circulationVSAvoidcardiac and neurotoxicity

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent employs a mucoadhesive patch that provides dynamic controlled release of tacrolimus, allowing the drug to be delivered to systemic circulation without the harmful effects of high-concentration bolus infusions while maintaining therapeutic levels

Inventive Principle:

Principle #15Dynamics

4Ease of manufacture

If immediate-release formulations of tacrolimus are used, then the predominant form of the drug can be utilized, but there is large interindividual variability in intestinal absorption with average bioavailability of only 25%

Engineering Contradiction:

Improveavailability of immediate-release formulationsVSAvoidbioavailability consistency

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The patent introduces a buccal mucoadhesive patch as an intermediary delivery system that bypasses the unreliable intestinal absorption pathway, providing consistent and reliable drug delivery while maintaining the simplicity of immediate-release formulation manufacturing

Inventive Principle:

Principle #24Intermediary (Mediator)

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 buccal patch achieves efficient drug delivery with reduced doses by 30-50%, maintaining steady tacrolimus levels in the systemic circulation, improving patient compliance, and minimizing toxicity risks.

Implementation Method 1

buccal mucoadhesive patch formulation of tacrolimus

Methodology Applied

Scientific EffectMucoadhesion: Adhesive

Implementation Method 2

delivery of the tacrolimus through the transbuccal route to the systemic circulation

Methodology Applied

Scientific EffectTransbuccal absorption: Absorption (physical)

Implementation Method 3

providing both immediate and controlled release

Methodology Applied

Scientific EffectControlled release: Diffusion

Implementation Method 4

solid lipid nanoparticles (SLNs) in a polymeric matrix

Methodology Applied

Scientific EffectSolid lipid nanoparticle dissolution: Melting

Data Source

PatentUS20250319019A1Buccomucoadhesive patch-based drug delivery system for tacrolimus

Publication Date: 2025.10.16 PATTANAIK SMITA

AI summary

The present disclosure relates to buccal mucoadhesive patch formulation of tacrolimus loaded in the solid lipid nanoparticles and using the polymeric carrier matrix and pharmaceutically acceptable additives to deliver tacrolimus through the trans buccal route to the systemic circulation. The overall exposure to tacrolimus with the tacrolimus buccal mucoadhesive patch formulation of present invention is considerably higher compared to the conventional oral administration for equivalent dose. It provides an immediate and controlled release of tacrolimus by avoiding the first pass metabolism and providing a steady concentration of tacrolimus in the systemic circulation.