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Triptorelin

Decapeptyl, Trelstar, Gonapeptyl, Pamorelin

Quick Stats
Studies 178
Trials 100
Score 3
2021 pubmed 22 citations

Silk fibroin double-layer microneedles for the encapsulation and controlled release of triptorelin.

Lu. Xiaoyan X; Sun. Yiying Y; Han. Meishan M; Chen. Daoyuan D; Wang. Aiping A; Sun. Kaoxiang K

Key Findings

  • Silk fibroin microneedles can encapsulate triptorelin as ~1 µm crystals
  • Release of triptorelin lasts up to 168 hours and can be slowed by increasing β‑sheet content
  • In rats the patch maintained castration‑level testosterone for ≥7 days

Practical Outcomes

  • For biohackers this suggests a potential skin‑patch alternative to frequent injections for hormone control, but it’s still an animal study. The technology isn’t commercially available yet and human safety/efficacy data are missing, so it’s a promising concept rather than a ready‑to‑use protocol.

Summary

Scientists made a tiny patch with silk‑based microneedles that can hold the hormone‑blocking peptide triptorelin and release it slowly through the skin. In rats the patch kept testosterone very low for at least a week, showing it could work as a long‑acting, needle‑free way to suppress sex hormones.

Abstract

A double-layer silk fibroin microneedles (SF-MNs) was proposed for the transdermal delivery of triptorelin. Two-step pouring and centrifugation were employed to prepare SF-MNs. Triptorelin was wrapped in MNs in the form of microcrystals with a size of ∼1 μm. β-sheet nanocrystals (the secondary structure of silk fibroin) were adjusted in content by methanol-vapor treatment to manipulate the characteristics of SF-MNs prepared with two concentrations of silk fibroin. The mechanical strength of MNs was measured and analyzed in proportion to the β-sheet content. The triptorelin in MNs could be released sustainedly in phosphate-buffered saline for 168 h, and the release amount decreased with increasing β-sheet content. The Ritger-Peppas equation was employed to fit the release data. A linear decreasing relationship was observed between the diffusion coefficient and increased β-sheet content. After administration to rats, SF-MNs exhibited long-term testosterone inhibition and maintained castration levels for ≥7 d. Manipulable mechanical properties and release behavior combined with biocompatibility and biodegradability render SF-MNs as viable long-term transdermal delivery devices for triptorelin.

Study Information

Provider

pubmed

Year

2021

Date

2021-12-28T00:00:00.000Z

DOI

10.1016/j.ijpharm.2021.121433

Citations

22

References

41