Dissolving Microneedle Patch Integrated with Microspheres for Long-Acting Hair Regrowth Therapy

Abstract

Androgenetic alopecia (AGA) is the most common type of progressive hair loss in both men and women that severely reduces life quality and affects patients’ self-esteem. Due to the shortcomings of traditional therapeutic formulations (e.g., topical minoxidil and oral finasteride), such as low bioavailability, frequent dosing, and significant side effects, there is an urgent need to develop a safe and effective strategy for AGA treatment. Here, we report a water-soluble microneedle (MN) patch integrated with biodegradable minoxidil (MXD)-loaded microspheres for long-acting AGA treatment with reduced administration frequency and improved patient compliance. When the patch pierces the skin, the MNs rapidly dissolve and deliver MXD-encapsulated polylactic-co-glycolic acid (PLGA) microspheres into the skin, which, subsequently act as drug reservoirs for the sustained release of the therapeutics for over 2 weeks. Additionally, the application of the MN patch provided a mechanical stimulation on mouse skin, which was also helpful for hair regrowth. Compared with the topical MXD solutions that have been commercialized on the market and require daily application, the long-acting MN patch contains a much lower drug amount and shows a similar or superior hair regeneration effect in AGA mice while only requiring monthly or weekly administration. These encouraging results suggest a simple, safe, and effective strategy for long-acting hair regeneration in clinics.

Microneedle Delivery Platform Integrated with Codelivery Nanoliposomes for Effective and Safe Androgenetic Alopecia Treatment

“…Notably, the dosage of active ingredients in the KK-NLPs@MNs group (kopexil of 1.5 mg and kopyrrol of 0.75 mg) was much lower than that in the minoxidil group (minoxidil of 6 mg), but exhibited comparable effects, demonstrating the superiority of this MNs delivery system. Additionally, a moderate hair regrowth effect was observed in mice receiving the treatment of blank-NLPs as identified in the abovementioned parameters compared to the model group, possibly attributed to the effect of phosphatidylcholine in the NLPs, whereas those treated with blank-MNs were due to the mechanical stimulation generated by the inserted MNs. ,, The better performance of KK-NLPs@MNs in the treatment of AGA was probably due to the synergistic effects of cotreatment with kopexil and kopyrrol, enhanced skin permeation, and cellular uptake efficiency mediated by NLPs, effective SC disruption, and mechanical stimulation of MNs.…”

“…Additionally, a moderate hair regrowth effect was observed in mice receiving the treatment of blank-NLPs as identified in the abovementioned parameters compared to the model group, possibly attributed to the effect of phosphatidylcholine in the NLPs, whereas those treated with blank-MNs were due to the mechanical stimulation generated by the inserted MNs. 7,61,62 The better performance of KK-NLPs@ MNs in the treatment of AGA was probably due to the synergistic effects of cotreatment with kopexil and kopyrrol, enhanced skin permeation, and cellular uptake efficiency mediated by NLPs, effective SC disruption, and mechanical stimulation of MNs. The regulation of HF formation and cycling involves a complex interplay of intracellular and intercellular signaling molecules.…”

The progress of fabrication designs of polymeric microneedles and related biomedical applications

“…(c) Side view of the MN patch showing drug‐loaded microspheres inside disrupted needle tips. (d) The drug release profile from MNs in vitro, showing a long‐acting capability of the MNs [22] . Copyright 2023, American Chemical Society.…”

Nanodrug Delivery Strategies to Signaling Pathways in Alopecia

“…Yin et al designed minoxidil-loaded PLGA microspheres delivered via microneedles (Figure ). Minoxidil and PLGA in individual organic solutions were mixed with a poly­(vinyl alcohol) solution and evaporated to form microspheres.…”

“…* P < 0.05, ** P < 0.01, and *** P < 0.001. ns indicates no significance. Reproduced from ref . Copyright 2023 American Chemical Society.…”