From Topical to Oral: Formulation Innovation of Minoxidil and New Trends in Hair Loss Treatment
Minoxidil is one of the most classic and widely used drugs for the treatment of androgenetic alopecia (AGA). For decades, topical minoxidil has been regarded as a first-line therapy for both male and female hair loss.
However, for many long-term users, “effective” does not always mean “convenient.”
Traditional topical solutions tend to make hair greasy and flat, affecting daily appearance; even the later-developed foam formulations still require daily repeated application and waiting for the solution to dry. For patients who need long-term adherence to treatment, medication compliance remains a real-world challenge.
Therefore, in recent years, research and development of new formulations of minoxidil have been accelerating. From low-dose oral tablets, to sustained-release tablets, oral solutions, and even sublingual tablets and sublingual sprays, more and more studies are attempting to free hair loss treatment from the limitations of “applying to the scalp every day.”
As DengYueMed, an organization focused on global pharmaceutical information and medical innovation communication, we continue to monitor the formulation evolution and clinical research progress in the field of androgenetic alopecia.
Topical Minoxidil: Effective, but Adherence Remains the Bottleneck
Currently, minoxidil on the market is still mainly available in topical formulations, including 2% and 5% solutions, as well as foam formulations.
Mechanistically, topical minoxidil works by dilating blood vessels around hair follicles and prolonging the anagen phase, thereby promoting hair growth. However, in real-world practice, many patients are unable to maintain long-term use.
A retrospective study involving 400 patients with AGA showed that the discontinuation rate of topical minoxidil reached as high as 86.3%. Even in the absence of obvious adverse effects, many patients still stopped treatment due to cumbersome application, interference with hairstyle, and the need for long-term persistence.
This is precisely why “more convenient drug delivery methods” are becoming an important direction in the field of hair loss treatment.
Low-Dose Oral Minoxidil: From Antihypertensive Drug to Hair Loss Treatment Hotspot
Low-dose oral minoxidil (LDOM) has become a highly discussed topic in the global hair loss field in recent years.
In fact, oral minoxidil is not a new drug. It was originally developed as a vasodilator for hypertension, and it is still available in some countries in 2.5 mg, 5 mg, and 10 mg strengths. However, the FDA label does not approve its use for hair loss treatment.
Nevertheless, in clinical practice, physicians have increasingly used low-dose minoxidil off-label for hair loss treatment, with common LDOM doses typically ≤5 mg/day.
Studies show that:
● The efficacy of LDOM is generally comparable to topical minoxidil, and higher-dose regimens may even be superior;
● In terms of ease of use and patient satisfaction, oral regimens are significantly better than topical ones;
● Patients have lower missed-dose rates and greater hairstyle freedom;
● Many patients find it easier to adhere to long-term treatment.
A cross-sectional study showed that compared with the topical group, patients in the oral group found treatment “simpler and more convenient,” and had a significantly lower discontinuation rate due to difficulty in use.
For long-term therapies, “willingness to adhere” is often as important as the efficacy of the drug itself.
Is Oral Minoxidil Safe?
Safety has always been one of the most concerned issues regarding oral minoxidil.
Since minoxidil was originally an antihypertensive drug, oral administration may lead to certain systemic effects.
A systematic review showed that the most common adverse effects of LDOM include:
● Hypertrichosis
● Initial increased hair shedding
● Peripheral edema (foot swelling)
● Tachycardia
● Blood pressure fluctuations
However, under low-dose conditions, most adverse effects are generally considered controllable.
This has also driven another research direction: how to preserve efficacy while further reducing peak plasma concentrations and cardiovascular risks.
Sustained-Release Oral Tablets: More Stable Drug Concentration
One of the more rapidly advancing new formulations is the sustained-release oral minoxidil VDPHL01 developed by Veradermics Therapeutics.
This formulation works by slowly releasing the drug, allowing minoxidil to act on hair follicles for a longer period while avoiding the rapid peak plasma concentration associated with conventional immediate-release tablets.
In theory, this design offers two core advantages:
● Enhanced sustained hair growth effects;
● Reduced risk of cardiovascular side effects.
Currently, VDPHL01 has entered Phase III clinical trials.
Available Phase II data show that:
● After 4 months of use, hair count in target areas significantly increased;
● More than 90% of male participants reported improved hair coverage;
● No serious cardiac adverse events have been reported so far.
If approved in the future, it may become the first sustained-release oral minoxidil specifically developed for both male and female pattern hair loss.
Oral Solution: More Flexible Dose Adjustment
In addition to tablets, oral solutions are also entering clinical development.
N-1087, developed by Eurofarma, is an oral minoxidil solution currently in Phase III clinical trials.
Compared with fixed-dose tablets, the advantages of oral solution include:
● Easier dose titration;
● Gradual increase to tolerable doses;
● Better suitability for individualized therapy.
The current study protocol uses a stepwise titration approach, starting from 0.75 mg and gradually increasing to 5 mg or the maximum tolerated dose, in order to balance efficacy and safety.
Sublingual Tablets: Bypassing First-Pass Hepatic Metabolism
In recent years, sublingual administration has become a particularly noteworthy new direction for minoxidil delivery.
Traditional oral minoxidil is absorbed via the gastrointestinal tract and then metabolized in the liver into its active form. This process not only produces a “first-pass effect,” but may also enhance systemic hemodynamic effects.
In contrast, sublingual tablets are absorbed directly through the oral mucosa.
Theoretically, this method can:
● Bypass hepatic first-pass metabolism;
● Improve bioavailability;
● Reduce systemic side effects;
● Act more precisely on hair follicles.
The sublingual minoxidil tablet developed by Samson Clinical is currently also in Phase III clinical trials.
Existing studies show that:
● Sublingual tablets increase hair density in a dose-dependent manner;
● Efficacy is comparable to oral 5 mg regimens;
● However, the incidence of palpitations is lower.
This suggests that sublingual administration may become a future option balancing efficacy and safety.Sublingual Spray: A More Flexible New Approach
Compared with sublingual tablets, sublingual sprays further improve dosing flexibility.
A study in Spain developed a minoxidil sublingual spray, in which dosing can be adjusted by the number of sprays, with each spray delivering approximately 0.5 mg.
Potential advantages include:
● Faster absorption;
● More stable administration;
● Easier dose control;
● Potentially fewer adverse effects.
Current safety evaluation results show good tolerability, with adverse event rates similar to or even lower than conventional oral regimens.
Summary
For a long time, the core focus of hair loss treatment has been “whether the drug is effective.” However, increasingly, studies are recognizing that:
What ultimately determines long-term treatment outcomes is not only efficacy, but also whether patients are willing to adhere to therapy.
For patients with hair loss, repeatedly applying medication to the scalp, waiting for it to dry, and the impact on hairstyle and daily life can all gradually reduce adherence.
Therefore, the development of new minoxidil formulations is not merely an improvement in drug delivery methods, but a shift in the entire concept of hair loss treatment—from “simply effective” to “sustainable, long-term, and patient-friendly experience.”
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