What is “Biotinoyl Tripeptide-1” and what is it used for?

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

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

The value of biotinoyl tripeptide-1 for the skin is primarily based on its ability to slow skin aging and aid in skin healing.

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

Indeed, tripeptide-1, i.e., GHK, can interact with fibroblasts. In models of oxidative stress induced by hydrogen peroxide, this peptide was able to limit collagen degradation, measured by hydroxyproline quantification, while upregulating expression of the COL-1 gene encoding type I collagen. In parallel, a significant decrease in the expression of the metalloproteinase MMP-1, an enzyme involved in collagen fiber fragmentation, was observed. Moreover, a partial inhibition of elastase activity, responsible for elastin degradation, was recorded. These results illustrate biotinyl-GHK’s ability to preserve the extracellular matrix.

However, in the absence of clinical studies, caution should be exercised.

Biotinoyl tripeptide-1 is particularly prized in haircare products, where it is used to support hair health and stimulate growth. This active ingredient acts at several levels of the hair follicle. First, the peptide helps reinforce the anchoring of hair within the scalp, thereby limiting shedding. Biotinyl-GHK also stimulates the synthesis and organization of certain structural proteins, such as laminin-5 and type IV collagen. These molecules form the basement membrane that separates the dermal compartment from the epithelial compartment, creating a stable scaffold for hair follicles and enhancing the hair’s mechanical strength.

Furthermore, biotinoyl tripeptide-1 supports the proliferation of keratinocytes in the hair bulb. It acts by modulating the expression of Ki-67, a marker protein of active cell division, thereby enabling more efficient cell renewal and promoting 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 primary androgen involved in androgenetic alopecia. By modulating this hormonal pathway, biotinoyl tripeptide-1 helps to limit the shortening of hair growth phases and the progressive miniaturization of hair follicles, the main phenomena responsible for hair thinning and loss.

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

Initially, experiments in vitro were performed on human dermal papilla cells (HHDPC), which are involved in regulating the hair cycle. After 72 hours of serum exposure 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 achieved with minoxidil, used as a positive control, with no statistically significant difference between them. Notably, a higher concentration of 2.50% had no effect on cell growth, suggesting that the peptide’s activity depends on a specific concentration window beyond which the biological signal is not delivered. Meanwhile, a decrease in reactive oxygen species production was measured, indicating reduced follicular oxidative stress, a known factor that can disrupt hair growth.

The study also investigated the serum’s impact on 5α-reductase expression, the enzyme responsible for converting testosterone into DHT. In DHT-stimulated HHDPC cells, serum treatment enabled a significant reduction in the expression of this enzyme. At a 1.25% concentration, 5α-reductase inhibition was equivalent to that observed with minoxidil, indicating effective modulation of this hormonal pathway involved in the progressive miniaturization of hair follicles.

These results in vitro were supplemented by a clinical trial conducted with 40 participants experiencing hair loss. Each volunteer had one treated area and one untreated area on the scalp. The product was applied twice daily for 90 days. In male participants, the outcomes showed a significant increase in hair mass as early as day 15, along with 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 demonstrates that formulations incorporating biotinoyl tripeptide-1 can act at multiple levels of the hair follicle and support the growth of hair—including scalp hair as well as other hair types (eyelashes, eyebrows...).

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

The analysis of the safety profile of biotinyl-GHK can also rely on the understanding of its components, particularly biotin, which has been more extensively studied. An evaluation by the CIR’s independent expert panel highlighted the lack of specific data on biotin’s potential to cause irritation or sensitization when applied topically. However, given the large number of people exposed daily to this vitamin, the experts concluded that if biotin had a high potential for skin irritation or sensitization, clinical cases would already have been reported in the scientific literature, which has not occurred to date.

This same evaluation further indicates that biotin does not present a risk of phototoxicity, as UV‐absorption data show no concerning interaction with ultraviolet radiation. Regarding systemic toxicity, experts assessed deliberately conservative exposure scenarios, including daily application of a product containing up to 0.6% biotin. Even under these conditions—and assuming an estimated 10% skin absorption—the systemic exposure remained consistent with biotin’s low toxic potential, since it is rapidly metabolized and eliminated by the body without any risk of accumulation. Moreover, biotin is not considered mutagenic or teratogenic and is suitable for use during pregnancy.

Thus, although specific data on biotinyl-GHK remain limited, the totality of available evidence suggests a favorable 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).