Pharmacokinetics of Sublingual Versus Oral Estradiol in Transgender Women. Endocr Pract 2022 Mar;28(3):237-242
Date
11/16/2021Pubmed ID
34781041DOI
10.1016/j.eprac.2021.11.081Scopus ID
2-s2.0-85121347509 (requires institutional sign-in at Scopus site) 4 CitationsAbstract
OBJECTIVE: To investigate the pharmacokinetics of 17β-estradiol (E2) administered orally versus those of 17β-E2 administered sublingually in transgender women.
METHODS: Single doses of 17β-E2 were administered orally (1 mg) to 10 transgender women and then sublingually (1 mg) after a 1-week washout period. Blood samples were collected at baseline (0 hour) and at 1, 2, 3, 4, 6, and 8 hours after dosing. The samples were frozen and analyzed using liquid chromatography mass spectrometry (LC-MS/MS) and immunoassay.
RESULTS: The results demonstrated that sublingual E2 had a significantly higher peak serum E2 concentration of 144 pg/mL, measured using LC-MS/MS, compared with an oral E2 concentration of 35 pg/mL, measured using LC-MS/MS (P = .003). Sublingual E2 peaked at 1 hour and oral E2 peaked at 8 hours, as measured using LC-MS/MS. The area under the curve (AUC) (0-8 hours) for sublingual E2, measured using LC-MS/MS, was 1.8-fold higher than the AUC (0-8 hours) for oral E2, measured using LC-MS/MS. Additionally, sublingual E2 was found to have an increased E2-to-estrone ratio at all time points (1.1 ± 1.0 vs 0.7 ± 0.4, P ≤ .0001), the clinical significance of which is unclear.
CONCLUSION: Oral E2 administered sublingually has a different pharmacokinetic profile, with higher serum E2 levels and AUC (0-8 hours) than traditionally administered oral E2. Multidaily dosing may be necessary to suppress testosterone levels with sublingual E2. The appropriate dosing, efficacy, and safety of sublingual E2, compared with those of other E2 preparations, are unknown.
Author List
Doll E, Gunsolus I, Thorgerson A, Tangpricha V, Lamberton N, Sarvaideo JLAuthor
Jenna Sarvaideo DO Assistant Professor in the Medicine department at Medical College of WisconsinMESH terms used to index this publication - Major topics in bold
Chromatography, LiquidEstradiol
Estrone
Female
Humans
Tandem Mass Spectrometry
Transgender Persons
