Propylene glycol free 5% minoxidil lotion formulation: cosmetic acceptability, local tolerability, clinical efficacy and in-vitro skin absorption evaluations

Barbareschi, M.; Vescovi, Veronica; Starace, Michela; Piraccini, Bianca Maria; Milani, Massimo

doi:10.23736/s0392-0488.20.06554-2

Cited by 8 publications

(7 citation statements)

References 30 publications

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“…The comparison was performed by in vitro diffusion through a semi-permeable membrane, by ex vivo permeation through porcine ear skin, and finally by determination of the residual drug amount in the skin after previous ex vivo permeation. In conventional MXD solutions, propylene glycol (PG) is used to dissolve the drug [ 23 ]; therefore, it was used as the solubilizer in the comparative gel. MXD gels represent a more advantageous dosage form compared to the solutions through higher adhesion to the skin.…”

Section: Introductionmentioning

confidence: 99%

Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels

Špaglová

Čuchorová

Čierna

et al. 2021

Gels

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Micro- and nanoemulsions are potential drug solubilizers and penetration enhancers through the high surfactant/co-surfactant content. This study aimed to evaluate the influence of minoxidil (MXD) solubilized in the microemulsions (MEs) on drug release by in vitro/ex vivo diffusion through the semi-permeable membrane Spectra/Por® (Spectrum Laboratory, Gardena, CA, USA) and porcine ear skin. Moreover, a residual amount of drug in the skin after ex vivo diffusion was evaluated. The reference MER, lecithin-containing MEL, and gelatin-containing MEG were characterized in terms of their size, polydispersity index, density, viscosity, electrical conductivity and surface tension. Based on the in vitro diffusion, it can be argued that MEL slowed down the drug release, while MER and MEG have no significant effect compared to the sample, in which propylene glycol (PG) was used as a solubilizer. Determination of the residual drug amount in the skin after 6 h of the ex vivo permeation was demonstrated as the most valuable method to evaluate the effectiveness of the ME’s application. The results indicate that the most optimal MXD permeation enhancers in alginate gel were the natural surfactants containing MEs. MXD solubilization in MEG and MEL had caused more than 5% of the drug remaining in the skin, which is almost a 1.5-fold higher amount compared to the reference gel.

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Section: Introductionmentioning

confidence: 99%

Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels

Špaglová

Čuchorová

Čierna

et al. 2021

Gels

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“…In patients with contact dermatitis, a patch test should be performed to identify the allergen. In the case of irritation or allergy from propylene glycol, a propylene-glycol-free formulation can be prescribed to reverse the sensitization process and enhance drug acceptability and tolerability [ 9 , 29 , 30 ]. In such cases, the foam form is preferred over the liquid form, as it does not contain any propylene glycol, usually required for the liquid formulation to serve as a vehicle that dissolves hydrophobic minoxidil in water [ 31 ].…”

Section: Discussionmentioning

confidence: 99%

Compliance to Topical Minoxidil and Reasons for Discontinuation among Patients with Androgenetic Alopecia

Zari

2023

Dermatol Ther (Heidelb)

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Introduction: This study assessed the levels of compliance to topical minoxidil (TM) among male and female patients with androgenetic alopecia (AGA) and analyzed the factors associated with minoxidil discontinuation. Method: A retrospective study was conducted among 400 consecutive patients with AGA who presented to a dermatology clinic and who were prescribed minoxidil 2% or 5% in the past 5 years. Demographic factors, other previous treatments, and minoxidil parameters including the dose (2% or 5%), total duration of use, treatment results, and side effects were collected. Result: The mean age of the patients was 32.41 years [standard deviation (SD) 8.18], and 66.5% were female. The majority of patients (82.5%) did not receive any previous treatment for AGA. Of the total patients, 345 (86.3%) have discontinued minoxidil. Discontinuation rate showed no association with sex (p = 0.271), age

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“…However, PG frequently induces local irritation 4 : For this reason, a PG-free MNX formulation was developed and is commercially available. 5 MNX acts as an arteriolar vasodilatation that opens potassium channels, playing a key role in cell proliferation. 4 In addition, it is able to prolong the anagen phase in the dermal papilla by inducing β-catenin activity.…”

Section: Introductionmentioning

confidence: 99%

“…Minoxidil solutions generally contain propylene glycol (PG), useful for the solubilization and penetration of MNX. However, PG frequently induces local irritation 4 : For this reason, a PG‐free MNX formulation was developed and is commercially available 5 . MNX acts as an arteriolar vasodilatation that opens potassium channels, playing a key role in cell proliferation 4 .…”

Section: Introductionmentioning

confidence: 99%

Efficacy of the association of topical minoxidil and topical finasteride compared to their use in monotherapy in men with androgenetic alopecia: A prospective, randomized, controlled, assessor blinded, 3‐arm, pilot trial

Rossi,

Caro

2023

J of Cosmetic Dermatology

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PurposeTopical minoxidil (MNX) 2%–5% and oral finasteride (F) 1 mg/day are the only two pharmacological treatments authorized for androgenetic alopecia (AGA). Recently, a 2.2 mg/mL topical formulation of F was developed to minimize the systemic adverse effects associated with the oral formula. MNX and F act through different mechanisms; therefore, their association could improve clinical efficacy. To evaluate the efficacy of the association of 5% MNX and 0.25% topical F compared to their use in monotherapy, a 6‐month, prospective, randomized, assessor‐blinded trial was conducted.Patients and MethodsForty‐two males, mean age 24 ± 3 years, with AGA (I–VII of Norwood‐Hamilton Grading Scale), treatment naive or free from any therapy for at least 6 months, were enrolled and randomly assigned to three arm treatment groups (2:1:1): group A (n = 19, the subjects applied 5% MNX in the morning and F spray in the evening), group B (n = 12, the subjects applied F spray in the evening), and group C (n = 11, the subjects applied 5% MNX twice daily). The efficacy of treatments was evaluated at baseline and after 3 and 6 months using a global photography score (GPAS; from −3 to +3) and trichoscopy evaluation and assessed by an investigator unaware of treatment allocation. At baseline and after treatments, the serum levels of follicle‐stimulating hormone (FSH), luteinizing hormone (LH), dehydroepiandrosterone sulfate (DHEA‐S), and testosterone were also evaluated.ResultsAll treatments resulted in an increase in hair density compared to baseline. However, this improvement was significant only for group A (MNX + F), both at three (+56 density/cm2, p < 0.05) and six (+81 density/cm2, p < 0.001) months. The mean change from baseline in hair density was higher for group A compared to other groups and statistically different compared to group B (F) (p < 0.01), both after 3 and 6 months. Group A showed a global photographic assessment score (GPAS) significantly higher compared to group B (p < 0.001) and group C (p < 0.05) both at 3 and 6 months (2.0 ± 0.7 vs. 0.6 ± 0.8 and 1.3 ± 0.6; respectively). A significantly greater percentage of subjects in Group A achieved a GPAS score of ≥2 in comparison with Groups B and C both after 3 and 6 months (79% vs. 8% and 41%, respectively). No significant differences were observed in mean hair diameter and hormonal levels between the three groups. Good tolerability was observed in all treated groups.ConclusionThe association of 5% MNX lotion and 0.25% F in spray formulation in patients with AGA showed a significantly higher clinical and instrumental efficacy compared to the monotherapies, with comparable tolerability and safety profile.

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Propylene glycol free 5% minoxidil lotion formulation: cosmetic acceptability, local tolerability, clinical efficacy and in-vitro skin absorption evaluations

Cited by 8 publications

References 30 publications

Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels

Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels

Compliance to Topical Minoxidil and Reasons for Discontinuation among Patients with Androgenetic Alopecia

Efficacy of the association of topical minoxidil and topical finasteride compared to their use in monotherapy in men with androgenetic alopecia: A prospective, randomized, controlled, assessor blinded, 3‐arm, pilot trial

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