Solid effervescent formulations as new approach for topical minoxidil delivery

Pereira, Maíra N.; Schulte, Heidi Luise; Duarte, Natane Castelo Branco; Lima, Eliana Martins; Barreto, Lívia Cristina Lira de Sá; Gratieri, Taís; Cunha-Filho, Marcílio

doi:10.1016/j.ejps.2016.10.016

Cited by 41 publications

(20 citation statements)

References 28 publications

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“…[ 8 , 9 , 10 , 11 ]. A number of other drug delivery systems which vary in structure and compositions, such as niosomes [ 12 ], penetration-enhancing vesicles [ 4 , 13 ], foams [ 14 , 15 ], lipid nanocarriers [ 16 , 17 , 18 ], microbubbles [ 19 ], microneedles [ 19 , 20 , 21 , 22 , 23 ], inclusion complexes [ 2 , 24 , 25 ], lecithin microparticles [ 26 ], and effervescent formulations [ 27 ], have been developed to enhance the skin permeation of drugs including MXD. However, the limitations mentioned earlier have not yet been addressed.…”

Section: Introductionmentioning

confidence: 99%

Oleic Acid Nanovesicles of Minoxidil for Enhanced Follicular Delivery

Kumar

Singh

Handa³

et al. 2018

Medicines

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Current topical minoxidil (MXD) formulations involve an unpleasant organic solvent which causes patient incompliance in addition to side effects in some cases. Therefore, the objective of this work was to develop an MXD formulation providing enhanced follicular delivery and reduced side effects. Oleic acid, being a safer material, was utilized to prepare the nanovesicles, which were characterized for size, entrapment efficiency, polydispersity index (PDI), zeta potential, and morphology. The nanovesicles were incorporated into the emugel Sepineo® P 600 (2% w/v) to provide better longer contact time with the scalp and improve physical stability. The formulation was evaluated for in vitro drug release, ex vivo drug permeation, and drug deposition studies. Follicular deposition of the vesicles was also evaluated using a differential tape stripping technique and elucidated using confocal microscopy. The optimum oleic acid vesicles measured particle size was 317 ± 4 nm, with high entrapment efficiency (69.08 ± 3.07%), narrow PDI (0.203 ± 0.01), and a negative zeta potential of −13.97 ± 0.451. The in vitro drug release showed the sustained release of MXD from vesicular gel. The skin permeation and deposition studies revealed superiority of the prepared MXD vesicular gel (0.2%) in terms of MXD deposition in the stratum corneum (SC) and remaining skin over MXD lotion (2%), with enhancement ratios of 3.0 and 4.0, respectively. The follicular deposition of MXD was 10-fold higher for vesicular gel than the control. Confocal microscopy also confirmed the higher absorption of rhodamine via vesicular gel into hair follicles as compared to the control. Overall, the current findings demonstrate the potential of oleic acid vesicles for effective targeted skin and follicular delivery of MXD.

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Section: Introductionmentioning

confidence: 99%

Oleic Acid Nanovesicles of Minoxidil for Enhanced Follicular Delivery

Kumar

Singh

Handa³

et al. 2018

Medicines

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“…To observe clinical efficacy of topical minoxidil for FPHL, subjects must use the drug for at least 24 weeks; however, in practice, most subjects use the drug for less than 30 days. The main reason for low compliance with topical minoxidil use is the poor cosmetic properties of the drug 5,6 . To address these shortcomings, we have developed a novel “After Minoxidil” spray that removes excess minoxidil from hair while leaving minoxidil on the scalp.…”

Section: Discussionmentioning

confidence: 99%

Novel “After Minoxidil” spray improves topical minoxidil compliance and hair style manageability

Kovacevic¹,

Ma²,

Shapiro

et al. 2020

J of Cosmetic Dermatology

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Background Topical minoxidil is the only US FDA‐approved drug for the treatment of female pattern hair loss (FPHL). While the safety profile of topical minoxidil is excellent, the efficacy of minoxidil in hair growth is extremely low. A recent survey of 8000 people observed that only 4% of hair loss patients using an over‐the‐counter minoxidil were very satisfied with their results. In contrast, in clinical studies with an intervening physician, approximately 30%‐40% of patients demonstrate an appreciable benefit. Compliance with topical drug regimens is often a major obstacle, limiting their effectiveness. Topical minoxidil leaves a greasy residue on the hair, which is especially problematic for women who do not wash their hair daily. Aims We set out to develop an “After Minoxidil” companion spray to minoxidil that removes residual minoxidil from the hair, where it is not needed, yet leaves minoxidil on the scalp where it is required. We hypothesized that improving the cosmetic properties of minoxidil would improve patient compliance with the drug and subsequently improve clinical outcomes. Methods A cohort of 20 FPHL patients was recruited to use the novel “After Minoxidil” spray and report changes in hair quality on a Likert scale. Results In our cohort of FPHL patients, the novel “After Minoxidil” spray restored ease of styling and reduced greasiness to preminoxidil level in 65% and 85% of subjects, respectively. The average reduction in perceived greasiness was 78%. Importantly, 70% of subjects interviewed stated they would likely continue to use the minoxidil and “After Minoxidil” treatment regimen for 6 months, vs 0% willing to use minoxidil alone. Conclusion The novel “After Minoxidil” spray improved ease of hair styling and reduced greasiness following application of topical minoxidil; thus, the novel “After Minoxidil” spray may help improve drug compliance and efficacy.

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“…Several studies have been devoted to the development of formulations aiming to increase minoxidil skin permeation and/or penetration into the hair follicles. Pereira and coworkers (2016) developed solid effervescent formulation of minoxidil sulfate, demonstrating an increase in the drug permeation highly dependent on the concentration of the effervescent mixture in the formulation [21]. Mura and coworkers (2013) studied the influence of penetration enhancing vesicles on transdermal minoxidil administration.…”

Section: In Vitro Follicular Penetration Of Minoxidilmentioning

confidence: 99%

Quality evaluation of minoxidil topical solutions obtained from magistral pharmacies

Dartora¹,

Bona²,

Santos³

et al. 2019

Drug Anal. Res.

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The objective of this study was to evaluate quality parameters of magistral topical solutions containing minoxidil (A, B and C), comparing the results with the ones obtained for the industrial formulation. Organoleptic tests, evaluation of the pH and density, centrifuge test, drug content determination, comparison of indicated dosages and in vitro follicular penetration of minoxidil were performed. Regarding the organoleptic properties, differences in color and viscosity were observed between the magistral (composed of minoxidil sulfate) and the industrial formulations (composed of minoxidil base). For pH values, the magistral solutions presented considerably more acidic pH, compared to the industrial sample. For the density test, the samples with the highest ethanol percentages (B and C) presented lower density. In the centrifuge test, none of the samples showed changes. Considering the drug content test, only the industrial sample and the magistral sample C showed drug percentage within the expected (90-110%), indicating lack of correction factor determination by the magistral pharmacies. Furthermore, it was observed that the dosage indicated by the magistral pharmacies do not correspond to the dose indicated by the industry, being significantly lower. All topical solutions tested presented hair follicle penetration of minoxildil, without statistical difference. The results indicate that there is a failure in the magistral pharmacies regarding the production and the indication of dosage of minoxidil topical solutions.

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Solid effervescent formulations as new approach for topical minoxidil delivery

Cited by 41 publications

References 28 publications

Oleic Acid Nanovesicles of Minoxidil for Enhanced Follicular Delivery

Oleic Acid Nanovesicles of Minoxidil for Enhanced Follicular Delivery

Novel “After Minoxidil” spray improves topical minoxidil compliance and hair style manageability

Quality evaluation of minoxidil topical solutions obtained from magistral pharmacies

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