Options for Delivery of Bioidentical Hormones


Options for Delivery of Bioidentical Hormones – Gel or Cream

Applied to the skin, the hydro-alcoholic gels have been shown to have good absorption in most, but not all, individuals. Patients see a relatively immediate effect and maintain a consistent level of the hormone in the bloodstream. The Transdermal or skin route avoids the first- pass through the liver and results in fewer metabolites. Patients with a personal or family history of blood clots should consider the topical gels instead of oral hormones.

The most researched ‘areas for application’of the topical gels are the chest, abdomen, and arms. The hydro-alcoholic gel should be applied to dry skin and left to dry for 2-3 minutes. The skin surface must be free of moisturizers, oils, or lotions.

Another benefit of the gels is the ability to increase or decrease the dosage as indicated by symptoms. A partial dose may be added in the evening. Some people metabolize hormones slowly and only need to use a small amount of gel once daily. Other people require larger doses applied twice daily.

Topical hydro-alcoholic gels seem to be more consistently absorbed than creams. Most of the research on absorption of hormones has been done with the gels. Physical activity and sweating can alter the amount of hormone delivered.

Creams applied to the mucous membranes of the vagina and labia have been extensively researched and are consistently absorbed. This route may be the preferred method of delivery in women.This method of delivery would not cause a buildup in the fat cells. It would also help with vaginal dryness, symptoms of urinary urgency, frequency, and repeated urinary tract infections, without a separate hormone preparation (e.g. vaginal estriol with testosterone) being prescribed.

Oral Capsules
Capsules are the most convenient. They absorb best with a meal that has natural fat in it. Oral capsules work best for someone who is hormonally stable without fluctuations.

Oral delivery is not the best route for testosterone. Testosterone converts to estradiol in the liver and is degraded rapidly. Oral delivery of conventional HRT increases the risk of blood clots. However, oral estradiol increases the good cholesterol, HDL. Oral progesterone is helpful for sleep.

Sublingual Drops and Lozenges
Sublingual delivery is also convenient. The drops or lozenge is placed under the tongue or against the buccal mucosal and allowed to absorb. Patients should try not to swallow the saliva.

The sublingual drops make it easy to increase or decrease the dose but tend to dry out (some brands). They are helpful with the wide fluctuations of peri-menopause or for the relief of migraine headaches.

The sublingual route has the advantage of bypassing the liver. A lower dose of progesterone can be used with less sedation from the metabolites compared to the oral route.

Sublingual lozenges may be used for delivery of testosterone in men and women.

Vaginal Creams and Suppositories
These are used for specific symptoms of vaginal dryness, urinary incontinence, urgency, frequency, and repeated urinary tract infections. You do get systemic absorption with vaginal delivery (see above).

Testosterone and Estradiol pellets may be implanted under the skin with a minor, 5 minute office procedure. These implants have been extensively researched and have been shown to consistently deliver hormones in both men and women for 3-6 months. Subcutaneous pellets are the best, most consistent, most convenient, and cost effective method to deliver hormone replacement therapy.

Each person is a unique individual. No two people absorb or metabolize hormones in the same way. If you are active and/or do aerobic exercise you may metabolize, or use up, hormones more rapidly. A higher dose of hormones or twice daily dosing may be needed to keep levels optimal. If you are sedentary or overweight, you may store, or build up, higher levels of hormones. You may need lower doses or alternate day dosing. You may have to try different delivery systems to see which is right for you. Sometimes a combination of delivery systems is best. If you have trouble with alcohol (you can feel one drink), have liver problems, or are sensitive to drugs, you may want to avoid the oral route. If there is a personal or family history of blood clots you should also avoid the oral route of delivery. You may find that you metabolize hormones slowly and need very small doses. If you have fluctuations in your own hormone levels you may need to adjust the amount of hormone cream you use.

Pay attention to your symptoms and feel free to work with your compounding pharmacist. Do not make changes based on symptoms of one or two day’s duration. Stay on the same dosage for at least 7-10 days before making changes. See ‘Monitoring Hormone Levels’ & ‘Hot Flashes’.

Higher Doses Required  Lower Doses Required 
Thin, very little body fat
Aerobic exercise, active
High metabolism
No problems with alcohol or OTC drugs like benedryl or sleeping pills
Poor absorption  Excess fatty tissue, overweight
(may also build up higher levels
when cream applied to skin)
Sedentary, little or no exercise
Slow metabolism
Sensitivity to alcohol or drugs
Good absorption 

Women who are not sleeping well may want to use their hormones at night. They may also want to add oral progesterone which can help with sleep.