Topical Minoxidil Drug Delivery-A Pharmacokinetic View

Male pattern hair loss (MPHL), also known as androgenetic alopecia (AGA), affects a majority of men by the age of 50. In fact around one-third of men are already suffering from AGA by the  age of 30. For those who start losing their hair in their teenage years or 20s, this problem can be especially devastating.


To date, there have only been two US FDA approved treatments for AGA, Minoxidil and Finasteride.

Minoxidil Overview

Minoxidil, an antihypertensive drug is, coincidentally, the first-line topical therapy for alopecia (Male Pattern Baldness). Minoxidil is currently under active pharmacological investigation (Scow et al, 1999).

Minoxidil Pharmacokinetics

Numerous pharmacological factors like bioavailability and bioaccessibility (Heaney and Robert, 2001) determine the efficacy of topical Minoxidil for treating alopecia.

Technically, the bioavailability of a drug is the maximum when dispensed by the intravenous route and dwindles by oral and topical routes due to pharmacokinetic events like incomplete absorption and first-pass metabolism.

Bioaccessibility is the availability of the drug to the cellular membrane from the environment and plays a key role in bioavailability of topical formulations during drug delivery (Lin and Cardenas, 2003).

The Drug Delivery Dilemma in Topical Minoxidil

Bioavailability studies on various topical delivery systems for the delivery of Minoxidil from solution formulations have shown that the drug tends to crystallize soon after its application on the scalp (Chia-Ming Chiang et al, 1989).

Further, the discovery of hair follicular penetration pathways for the drug (Blume-Peytavi et al, 2010) and authentication of its role in the maintenance of the terminal follicles (Uno et al, 1987) illustrate that it is not the visible hair shaft but the hair follicle lodged in the skin that is essentially the target of topical Minoxidil drug delivery.

Hence, topical Minoxidil delivery can be effectual only when the target site (hair follicle) is addressed specifically and directly. Unfortunately, the terminal hair shafts from the neighboring scalp regions and the vellus hairs in the alopecia affected regions act as a potential barrier for the follicular bioaccessibility of the drug.

These hairs not only act as a barrier to the permeability of the drug into the follicles, but also dislocate the drug delivery by wasteful physical absorption.

Further, hair follicles are microscopic structures that need to be fed only by propelling minuscule dimensions of the drug at a given point of time for efficient absorption.

Regrettably, most of the topical Minoxidil brand formulations available in the market, including Kirkland Minoxidil dropper and Rogaine Foam feed the erroneous target (hair) in flawed quantities instead of the actual target –the hair follicles.

Regenepure Minoxidil Spray Device – an Ideal Topical Drug Delivery Solution

Regenepure Minoxidil SprayRegenepure Precision 5% Minoxidil Spray is a hand- operated aerosol spray atomizer device (Carlisle and Rodney, 2004) that can create an aerosol mist from a minoxidil solution formulation enclosed in an airtight container.

Regenepure spray devices are designed to make a perfect spray impact on the follicles with an ideal spray velocity. The calibrated spray nozzle capacity and the drop size of the device in terms of Sauter Mean Diameter (SMD) ensures high velocity impingement of Minoxidil aerosol on the micro-target site passing effectively through the micro-gaps in between hair strands (Lipp and Charles, 2012).

Thus, Regenepure Precision 5% Minoxidil Spray ideally addresses all the pharmacokinetic factors discussed in contrast to Kirkland Minoxidil dropper that delivers macro-sized drops of the drug sans any velocity and Rogaine Foam that just reaches the hair shaft like a shampoo instead of the follicles beneath.
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