UNILIPO Publishes Research on AR-Targeting asiRNA Nanoliposomes in ACS Applied Materials & Interfaces
New Publication: UNISOUL® RNAiG
A study jointly conducted by UNILIPO’s R&D Lab, led by Dr. Fang Wang, and Professor Jiaheng Zhang’s team at Harbin Institute of Technology, Shenzhen, has been published in ACS Applied Materials & Interfaces (IF 8.5; JCR Q1). The paper describes a topical asiRNA nanoliposome system targeting the androgen receptor (AR).
The paper refers to the material as ITD; UNILIPO markets it as UNISOUL® RNAiG.
What Problem Does This Technology Address?
The androgen receptor (AR) is a shared molecular target involved in androgenetic alopecia, acne, and seborrheic dermatitis. When androgens bind to AR, the resulting complex enters the cell nucleus and regulates gene activity, influencing protein production.
Androgenetic alopecia: AR signaling influences factors such as IGF-1 and TGF-β1, shortening the hair growth phase and contributing to follicle miniaturization. Over time, hairs become finer and less numerous.
Seborrheic dermatitis and excess oil: AR regulates genes involved in lipid production, contributing to increased oil-gland activity and oil accumulation on the skin.
Acne: AR promotes the growth and development of oil-producing cells, contributing to excess oil, blocked follicles, and inflammation.
Limitations of Existing Drugs
Existing treatments act through different mechanisms, each with potential limitations.
Oral drugs. Oral treatments include 5α-reductase inhibitors such as finasteride and AR antagonists such as spironolactone. These act throughout the body and may cause systemic side effects.
Topical drugs. Topical treatments such as minoxidil may take time to produce results, may not fully address hair loss, and may require continued use to maintain their effects.
Research Strategy: Silence AR Locally
UNILIPO’s approach uses asiRNA to reduce AR expression locally in skin cells. By targeting receptor production, the strategy aims to interrupt androgen signaling before its downstream effects occur.
Development Results: UNISOUL® RNAiG
To address the instability and limited skin penetration of nucleic acid ingredients, the team developed a cationic ionic-liquid liposome delivery system called UNISOUL® RNAiG. The system delivers AR-targeting asiRNA into deeper skin layers without needles.
The researchers evaluated its effects on hair loss, oil production, and acne using cell studies, animal models, and preliminary human trials.
Enhanced Transdermal Delivery
Confocal images showing delivery of FAM-labeled asiRNA into HFDPC and TM3 cells using UNISOUL® RNAiG and the Lipo6000 positive control.
Images taken at 4 and 16 hours showed fluorescence at depths of 700-1,100 μm, concentrated around hair follicles. By comparison, unencapsulated asiRNA in the PBS group showed limited penetration through the stratum corneum, the skin’s outermost layer.
For context: The human stratum corneum is approximately 10-20 μm thick, the epidermis 100-200 μm, and the dermis 1-2 mm. The reported signal depth corresponds to deeper skin regions containing hair follicles.
Hair-Loss Reduction
Cell Level
In a DHT-stimulated cell model used to study hair loss, UNISOUL® RNAiG significantly reduced AR protein expression, with a greater reduction than the 100 nM minoxidil positive control.
In a DHT-induced hair-loss cell model, UNISOUL® RNAiG significantly downregulated AR protein expression, outperforming the 100 nM minoxidil positive control.
Animal Model
In a DHT-induced C57BL/6 mouse model, UNISOUL® RNAiG at 5 or 10 nmol, administered three times weekly, visibly improved hair regrowth. The effects were comparable to those of 5% minoxidil applied once daily.
qRT-PCR analysis showed reduced expression of AR, DKK-1, TGF-β2, IL-6, and IL-1α, which are associated with hair-growth suppression. Expression of VEGF and β-catenin, which support hair growth and blood vessel formation, increased.
H&E staining showed improvements in hair follicle count, hair-bulb diameter, and skin thickness.
CD31 immunofluorescence showed a higher density of small blood vessels around hair follicles, suggesting improved local blood supply.
Human Trial
Thirty-two participants with androgenetic alopecia (pattern hair loss) applied the UNISOUL® RNAiG formulation daily for 28 days.
Hair shedding decreased progressively:
1. Day 7: 27.90%
2. Day 14: 36.68%
3. Day 28: 48.59%
Sebum Control
Cell Level
In SZ95 sebocytes stimulated with DHT and palmitic acid (PA), UNISOUL® RNAiG reduced lipid accumulation as its concentration increased. At 50 nM, it produced a greater reduction than spironolactone.
The treatment reduced expression of genes involved in lipid synthesis and uptake, including FASN, SREBP1c, and CD36. It increased expression of PPARα, which is involved in fatty acid breakdown.
Animal Model
In mouse skin, 4-HNE fluorescence, an indirect marker of lipid peroxidation, decreased as the dose increased. The 10 nmol group showed a greater reduction than the minoxidil comparison group.
Human Trial
Thirty participants with acne and oily skin applied the formulation for 28 days. Instrument-based measurements showed an average 24.92% reduction in sebum levels.
Acne Reduction
Antibacterial Effect
A plate-count assay showed a 99.57% inhibition rate against Propionibacterium acnes. The researchers attributed this effect to the carrier material’s antibacterial properties.
Anti-Inflammatory Effect
In a P. acnes-induced SKH-1 mouse model, UNISOUL® RNAiG at 10 nmol, administered three times weekly over seven days, produced faster improvement in acne lesions than the isotretinoin comparison treatment.
qRT-PCR analysis showed reduced expression of AR, TNF-α, IL-8, IL-1α, MMP2, and ICAM-1, and increased expression of IL-4 and TGF-β1.
Human Trial
The same 30 participants were assessed for both oil production and acne. Alongside reduced oil levels, researchers reported:
1. Inflammatory papules: 67.74% reduction
2. Pustules: 58.82% reduction
3. Comedones: 28.06% reduction
4. Pillsbury acne severity score: 29.09% reduction
Safety Profile
No itching, allergic reactions, or skin flaking were reported, and no irritation was observed among the assessed participants.
Technology Application and Outlook
UNISOUL® RNAiG was developed to address two challenges for nucleic acid skincare ingredients: instability and limited delivery through the skin. The preliminary studies reported beneficial effects without observed skin irritation in the assessed participants.
This approach focuses on a shared target rather than combining multiple active ingredients. By targeting AR signaling, UNISOUL® RNAiG is designed to address hair loss, excess oil, inflammation, and acne through a common mechanism.
UNILIPO has incorporated UNISOUL® RNAiG into products including the Salicylic Acid Sebum-Control Renewing Serum and the Anti-Hair-Loss Follicle-Activating Essence. Additional products are planned.
A related patented ingredient, UNISOUL® RNAiW, uses RNA interference to target MITF, a key regulator of melanin production. Clinical research reported skin-brightening effects, supporting further investigation and product development.
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