PTH Microprojection Arrays for Pulsatile Transdermal Delivery
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Solution Overview
Problem
Existing methods for administering parathyroid hormone (PTH) suffer from low bioavailability, skin irritation, and inconvenient administration, particularly for osteoporosis treatment, and lack a pulsatile delivery profile that mimics subcutaneous injection.
Innovation Solution
A microprojection array with PTH in a water-soluble polymer matrix is applied to the skin, allowing microprotrusions to penetrate and detach within minutes, achieving rapid PTH delivery and a pulsatile pharmacokinetic profile.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If subcutaneous injection is used to administer PTH, then bioavailability and pharmacokinetic profile are improved, but patient compliance and convenience deteriorate due to injection burden
Solution Approach 1:
The patent replaces the mechanical injection system (needles, syringes) with a transdermal delivery system using microprojections that penetrate the skin barrier to deliver PTH directly into the dermis, eliminating the need for subcutaneous injection while maintaining effective drug delivery
Solution Approach 2:
The patent introduces the skin as an intermediary delivery route between the PTH formulation and systemic circulation, using microprojections as mediators to traverse the stratum corneum barrier and deposit the peptide hormone in the dermal layer where it can be absorbed into circulation
2Ease of operation
If conventional transdermal delivery is used, then patient compliance is improved, but bioavailability deteriorates due to skin barrier penetration limitations
Solution Approach 1:
The patent segments the skin barrier into two distinct zones: the stratum corneum (outer layer) which the microprojections penetrate, and the dermis (inner layer) where the PTH is delivered. This segmentation allows the system to overcome the barrier function of the stratum corneum while targeting the dermis for effective absorption
Solution Approach 2:
The patent changes the physical parameters of the delivery system by using microprojections with specific dimensional characteristics (micrometer-scale diameter, millimeter-scale length) that enable penetration through the stratum corneum barrier, transforming the delivery mechanism from passive diffusion to active mechanical penetration
3Duration of action of stationary object
If continuous PTH delivery is used, then sustained bone building effect is achieved, but pulsatile pharmacokinetic profile deteriorates compared to subcutaneous injection
Solution Approach 1:
The patent implements periodic administration of PTH through discrete microprojection arrays applied at intervals (e.g., daily or weekly), creating pulsatile delivery cycles that mimic the physiological pulsatile secretion of PTH by the parathyroid gland, thereby maintaining the desired pharmacokinetic profile
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 method provides high bioavailability and rapid pharmacokinetics, reducing skin irritation and enabling self-administration with a delivery profile superior to subcutaneous injection.
Implementation Method 1
inserting all or a portion of the plurality of microprotrusions into the skin
Implementation Method 2
each microprotrusion comprising an end portion distal to the base and an upper portion proximal to the base, at least the end portion comprising parathyroid hormone (PTH) in a water-soluble polymer matrix
Data Source
AI summary
A method and a drug delivery system for transdermally administering parathyroid hormone (PTH) in a pulsatile fashion are provided, where the drug delivery system comprises an array of microprojections each comprising PTH.


