Hair follicle-targeting drug delivery strategies for the management of hair follicle-associated disorders

Gu, Ye; Bian, Qiong; Zhou, Yanjun; Huang, Qiaoling

doi:10.1016/j.ajps.2022.04.003

Cited by 39 publications

(26 citation statements)

References 117 publications

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“…PS could affect the depth of follicular penetration irrespective to the type of nanocarriers. It was stated that infiltration of follicular drugs developed by nanotechnology-based formulations could be enhanced by producing small-size particles to enlarge the surfaces with the stratum corneum [ 15 ]. Follicular targeting could be a remarkable selection to treat acne vulgaris, hirsutism, and androgenetic alopecia [ 16 ].…”

Section: Resultsmentioning

confidence: 99%

Exploring the Synergistic Effect of Bergamot Essential Oil with Spironolactone Loaded Nano-Phytosomes for Treatment of Acne Vulgaris: In Vitro Optimization, In Silico Studies, and Clinical Evaluation

et al. 2023

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The foremost target of the current work was to formulate and optimize a novel bergamot essential oil (BEO) loaded nano-phytosomes (NPs) and then combine it with spironolactone (SP) in order to clinically compare the efficiency of both formulations against acne vulgaris. The BEO-loaded NPs formulations were fabricated by the thin-film hydration and optimized by 32 factorial design. NPs’ assessments were conducted by measuring entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). In addition, the selected BEO-NPs formulation was further combined with SP and then examined for morphology employing transmission electron microscopy and three months storage stability. Both BEO-loaded NPs selected formula and its combination with SP (BEO-NPs-SP) were investigated clinically for their effect against acne vulgaris after an appropriate in silico study. The optimum BEO-NPs-SP showed PS of 300.40 ± 22.56 nm, PDI of 0.571 ± 0.16, EE% of 87.89 ± 4.14%, and an acceptable ZP value of −29.7 ± 1.54 mV. Molecular modeling simulations showed the beneficial role of BEO constituents as supportive/connecting platforms for favored anchoring of SP on the Phosphatidylcholine (PC) interface. Clinical studies revealed significant improvement in the therapeutic response of BEO-loaded NPs that were combined with SP over BEO-NPs alone. In conclusion, the results proved the ability to utilize NPs as a successful nanovesicle for topical BEO delivery as well as the superior synergistic effect when combined with SP in combating acne vulgaris.

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Section: Resultsmentioning

confidence: 99%

Exploring the Synergistic Effect of Bergamot Essential Oil with Spironolactone Loaded Nano-Phytosomes for Treatment of Acne Vulgaris: In Vitro Optimization, In Silico Studies, and Clinical Evaluation

et al. 2023

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“…To facilitate the observation of the insertion depth, PROTAC‐MNs were co‐loaded with Rhodamine B (RhB‐PROTAC‐MNs). In comparison to the untreated porcine skin, RhB‐PROTAC‐MNs can overcome the stratum corneum barrier and effectively transport the encapsulated cargoes to 200–300 µm deep in the skin, where most telogen HFs reside, [ 43 ] as confirmed by the red‐tapered microchannels after the insertion of RhB‐PROTAC‐MNs (Figure 2f). Most of the needles successfully penetrated into the skin, and completely disappeared after 5 min (Figure 2g).…”

Section: Resultsmentioning

confidence: 99%

PROTAC Degraders of Androgen Receptor‐Integrated Dissolving Microneedles for Androgenetic Alopecia and Recrudescence Treatment via Single Topical Administration

et al. 2022

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Androgenetic alopecia (AGA) is a transracial and cross‐gender disease worldwide with a youth‐oriented tendency, but it lacks effective treatment. The binding of androgen receptor (AR) and androgen plays an essential role in the occurrence and progression of AGA. Herein, novel proteolysis targeting chimera degrader of AR (AR‐PROTAC) is synthesized and integrated with dissolving microneedles (PROTAC‐MNs) to achieve AR destruction in hair follicles for AGA treatment. The PROTAC‐MNs possess adequate mechanical capabilities for precise AR‐PROTAC delivery into the hair follicle‐residing regions for AR degradation. After applying only once topically, the PROTAC‐MNs achieve an accelerated onset of hair regeneration as compared to the daily application of the first‐line topical drug minoxidil. Intriguingly, PROTAC‐MNs via single administration still realize superior hair regeneration in AGA recrudescence, which is the major drawback of minoxidil in clinical practice. With the degradation of AR, the PROTAC‐MNs successfully regulate the signaling cascade related to hair growth and activate hair follicle stem cells. Furthermore, the PROTAC‐MNs do not cause systemic toxicity or androgen deficiency‐related chaos in vivo. Collectively, these AR‐degrading dissolving microneedles with long‐lasting efficacy, one‐step administration, and high biocompatibility provide a great therapeutic potential for AGA treatment.

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“…The NLCs with a smaller particle size and occlusive properties can adhere themselves to the stratum corneum and form a thin film on the skin surface, achieving the desired effect of improving the penetration of the formulation as well as increasing hydration. [103][104][105] Angelo et al prepared nanostructured lipid carriers containing clobetasol propionate (NLC-CLO), which showed potential for epidermal targeting. [106] The NLC formulation exhibited great potential for CLO accumulation in HFs; the NLC-R6G provided fluorescence within the HFs at depths greater than 900 m (Figure 3e).…”

Section: Npsmentioning

confidence: 99%

Recent Trends in Macromolecule‐Based Approaches for Hair Loss Treatment

Kang

Park

et al. 2023

Macromolecular Bioscience

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Macromolecules are large, complex molecules composed of smaller subunits known as monomers. The four primary categories of macromolecules found in living organisms are carbohydrates, lipids, proteins, and nucleic acids; they also encompass a broad range of natural and synthetic polymers. Recent studies have shown that biologically active macromolecules can help regenerate hair, providing a potential solution for current hair regeneration therapies. This review examines the latest developments in the use of macromolecules for the treatment of hair loss. The fundamental principles of hair follicle (HF) morphogenesis, hair shaft (HS) development, hair cycle regulation, and alopecia have been introduced. Microneedle (MN) and nanoparticle (NP) delivery systems are innovative treatments for hair loss. Additionally, the application of macromolecule‐based tissue‐engineered scaffolds for the in vitro and in vivo neogenesis of HFs is discussed. Furthermore, a new research direction is explored wherein artificial skin platforms are adopted as a promising screening method for hair loss treatment drugs. Through these multifaceted approaches, promising aspects of macromolecules for future hair loss treatments are identified.

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Hair follicle-targeting drug delivery strategies for the management of hair follicle-associated disorders

Cited by 39 publications

References 117 publications

Exploring the Synergistic Effect of Bergamot Essential Oil with Spironolactone Loaded Nano-Phytosomes for Treatment of Acne Vulgaris: In Vitro Optimization, In Silico Studies, and Clinical Evaluation

Exploring the Synergistic Effect of Bergamot Essential Oil with Spironolactone Loaded Nano-Phytosomes for Treatment of Acne Vulgaris: In Vitro Optimization, In Silico Studies, and Clinical Evaluation

PROTAC Degraders of Androgen Receptor‐Integrated Dissolving Microneedles for Androgenetic Alopecia and Recrudescence Treatment via Single Topical Administration

Recent Trends in Macromolecule‐Based Approaches for Hair Loss Treatment

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