What is ‘Biotinoyl Tripeptide-1’ and what is it used for?

Biotinoyl tripeptide-1, also known as biotinyl-GHK, is an active ingredient obtained by conjugating biotin (vitamin B8) with a short peptide made up of three amino acids: glycine, histidine and lysine (GHK). This combination gives the molecule a hybrid, vitamin-like and peptidic structure designed to enhance its interaction with biological tissues.

Moreover, this helps to stabilise biotin, which is a water-soluble vitamin. From a chemical standpoint, biotinoyl tripeptide-1 belongs to the family of biomimetic peptides, that is to say small protein fragments inspired by sequences naturally present in the body. Its relatively low molecular weight facilitates its penetration into the epidermis.

The benefit of biotinoyl tripeptide-1 for the skin lies primarily in its ability to slow cutaneous ageing and to aid in skin repair.

These two processes are closely linked to the extracellular matrix of the dermis, whose integrity underpins mechanical strength, elasticity and the skin’s regenerative capacity. With age or repeated insults, the balance between synthesis and degradation of dermal components shifts, resulting in progressive fragmentation of collagen, alteration of fibres of elastin and a decline in glycosaminoglycans. Biotinyl-GHK can support these structures.

Indeed, the tripeptide-1, that is GHK, can interact with fibroblasts. In models of oxidative stress induced by hydrogen peroxide, this peptide has limited collagen degradation, as measured by hydroxyproline quantification, while increasing the expression of the COL-1 gene encoding type I collagen. Simultaneously, a significant decrease in the expression of the metalloproteinase MMP-1, an enzyme involved in the fragmentation of collagen fibres, was observed. Moreover, partial inhibition of elastase activity, responsible for elastin degradation, was recorded. These findings illustrate the capacity of biotinyl-GHK to preserve the extracellular matrix.

However, in the absence of clinical studies, it is advisable to exercise caution.

Biotinoyl tripeptide-1 is particularly valued in haircare cosmetics, where it is used to support hair health and stimulate its growth. This active compound acts at various levels of the hair follicle. First, the peptide helps to strengthen the anchorage of the hair to the scalp, thereby limiting its shedding. Biotinyl-GHK also stimulates the synthesis and organisation of certain structural proteins, such as laminin-5 and type IV collagen. These molecules form the basement membrane separating the dermal compartment from the epithelial compartment, providing a stable support for hair follicles and enhancing the mechanical resistance of hair.

Furthermore, biotinoyl tripeptide-1 supports the proliferation of keratinocytes in the hair bulb. It acts by modulating the expression of Ki-67, a protein indicative of active cell division, thereby enabling more efficient cell renewal and favouring the hair growth phase, also known as the anagen phase. Finally, the peptide also influences local hormonal regulation by reducing the production of dihydrotestosterone (DHT), the principal androgen involved in androgenetic alopecia. By modulating this hormonal pathway, biotinoyl tripeptide-1 contributes to limiting the shortening of hair growth phases and the progressive miniaturisation of hair follicles, the primary processes responsible for thinning and hair loss.

The mechanisms of action of biotinoyl tripeptide-1 in topical hair application are supported by experimental and clinical data, notably through a recent study on a hair serum formulated with this peptide and an extract of Phyllanthus emblica. This study aimed to assess the product’s impact on hair follicle health, both in cell models and in human subjects, within the context of hair loss.

Initially, tests in vitro were conducted on human hair dermal papilla cells (HHDPCs), which are involved in regulating the hair cycle. After 72 hours of exposure to the serum at concentrations of 0.625% and 1.25%, a significant increase in cell proliferation was observed, with growth rates reaching 148.24% and 143.59%, respectively compared to the control group. These results were comparable to those obtained with minoxidil, used as a positive control, with no statistically significant difference between the two. It is noteworthy that a higher concentration of 2.50% showed no effect on cell growth, suggesting that the peptide’s activity depends on a concentration window beyond which the biological signal is no longer delivered. Simultaneously, a reduction in the production of reactive oxygen species was measured, indicating a decrease in follicular oxidative stress, a known factor that disrupts hair growth.

The study also investigated the effect of the serum on 5α-reductase expression, the enzyme responsible for converting testosterone into DHT. In DHT-stimulated HHDPCs, treatment with the serum was found to significantly reduce the expression of this enzyme. At a concentration of 1.25%, the inhibition of 5α-reductase was equivalent to that observed with minoxidil, indicating effective modulation of this hormonal pathway involved in the progressive miniaturisation of hair follicles.

These results in vitro were complemented by a clinical trial involving 40 participants with hair loss. Each volunteer had a treated area and an untreated area on the scalp. The product was applied twice daily for 90 days. In the male participants, the results demonstrated a significant increase in hair mass as early as day 15, as well as a progressive improvement in hair density and terminal hair density on days 30 and 45. In women, improvements in hair density and quality were also measured.

Overall, this study highlights that formulations incorporating biotinoyl tripeptide-1 can act at multiple levels of the hair follicle and support the growth of scalp hair and other hairs (eyelashes, eyebrows...).

To date, there are no published studies specifically evaluating the safety profile of biotinoyl tripeptide-1 when applied to the skin or hair. However, the scientific literature does not report any cases of adverse effects associated with its use in cosmetic products, despite its presence for several years in formulations intended for the skin, scalp, eyelashes and eyebrows. This provides an initial reassuring indication, even though it cannot replace dedicated studies.

The analysis of the safety profile of biotinyl-GHK can also draw on knowledge of its constituents, particularly biotin, which has been more widely studied. An evaluation conducted by the independent expert panel of the CIR emphasised the absence of specific data regarding biotin’s potential to cause irritation or sensitisation when applied to the skin. Nevertheless, given the large number of individuals exposed to this vitamin on a daily basis, the experts judged that, if biotin possessed a high potential for skin irritation or sensitisation, clinical cases would have been reported in the scientific literature, which is not the case to date.

This same assessment also indicates that biotin poses no risk of phototoxicity, with UV absorption data showing no concerning interaction with ultraviolet radiation. Regarding systemic toxicity, experts considered deliberately high exposure scenarios, including daily application of a product containing up to 0.6% biotin. Even under these conditions, and taking into account an estimated skin absorption of 10%, the systemic exposure remained consistent with biotin’s low toxic potential, since it is rapidly metabolised and eliminated by the body without risk of accumulation. Furthermore, biotin is not regarded as mutagenic or teratogenic, and is suitable for use by pregnant women.

Thus, although data specific to biotinyl-GHK remain limited, the overall body of available evidence suggests a favourable safety profile.

• CASTELO-SOCCIOA L. & al. A review of the use of biotin for hair loss. Skin Appendage Disorders (2017).

• Cosmetic Ingredient Review Expert Panel. Amended safety assessment of biotin as used in cosmetics. Cosmetic Ingredient Review (2017).

• QU L. & al. Role of peptide-cell surface interactions in cosmetic peptide application. Frontiers in Pharmacology (2023).

• CHEN H. & al. The synergistic effect of phototherapy and active substances on hair growth. Journal of Photochemistry and Photobiology B: Biology (2024).

• CIURBA A. & al. Peptides: Emerging candidates for the prevention and treatment of skin senescence: A review. Biomolecules (2025).

• INAL O. & al. Current approaches in cosmeceuticals: Peptides, biotics and marine biopolymers. Polymers (2025).

• YEN F.-L. & al. Safety profile and efficacy of Biosea revive serum for hair growth through in vitro assessment and clinical evaluation. Cosmetics (2025).