- Lexaria recently completed its animal study HOR-A22-1 showing its patented DehydraTECH(TM) technology dramatically enhanced the oral delivery of estradiol, a type of estrogen hormone
- The use of DehydraTECH resulted in ~900% higher peak concentration of estradiol in the bloodstream compared to the control, as well as a 2,000% increase in the levels of estrone
- Estrone is a type of estrogen that can be reversibly made from estradiol in certain tissues within the female body
- The study HOR-A22-1 also revealed that DehydraTECH resulted in 1,500% and 12,500% higher exposure to estradiol and estrone over time, respectively, compared to the control
- Lexaria also announced the closing of a public offering that raised approximately $2 million in gross proceeds
Lexaria Bioscience (NASDAQ: LEXX), a global innovator in drug delivery platforms, recently reported that it had completed its animal study HOR-A22-1, which showed that the company’s patented DehydraTECH(TM) technology platform significantly enhanced the oral delivery of the estrogen hormone estradiol (https://ibn.fm/ywP2y).
Performed in 20 female Sprague-Dawley rats, the pharmacokinetic study compared a DehydraTECH-estradiol formulation to a generic estradiol composition, both containing 10 mg/kg of estradiol, to evaluate the ability of DehydraTECH to enhance the delivery properties of the orally administered hormone. Once dosing was completed, blood was collected up to 48 hours post-dosing, with the concentration of estradiol and estrone determined thereafter.
Estradiol is a major female sex hormone and the most common form of estrogen in women of childbearing age. It is normally made in the ovaries (although it is also manufactured in the testicles in men, albeit in small quantities) but can be administered as an oral tablet, topical gel or patch, cream, or injection to reduce the symptoms of menopause and protect bone health. It is also found in birth control products. Put simply, estradiol is an important element of therapeutic products in the women’s health sector. On the other hand, Estrone is the only type of estrogen that females continue to manufacture after menopause. It is primarily made in the adrenal glands (in both males and females), although it is also reversibly manufactured from estradiol in tissues found in the mammary gland, uterus, and liver, a factor that informed the study’s measurement of estrone levels.
The study found that the DehydraTECH-estradiol composition resulted in a maximum concentration in the bloodstream (“Cmax”) of 5.65 ng/mL, which was approximately 900% higher than the control formulation’s Cmax (0.63 ng/mL). Additionally, the use of the DehydraTECH-formulation resulted in a 2,000% increase in the levels of the estrone metabolite, also measured using the Cmax parameter: DehydraTECH-estradiol resulted in a Cmax of 6.49 ng/mL compared to the control’s 0.302 ng/mL.
Additionally, the study evaluated the area under the curve (“AUC”), a parameter that gave insight into the total delivery of estradiol over time as well as the extent of exposure to estrone. The AUC was 3.9 hr.ng/mL for estradiol and 32.6 hr.ng/mL for estrone when the DehydraTECH-processed composition was used. In comparison, the AUC after administering the control was non-detectable for both estradiol and estrone, as it was below 0.25 ng/mL, the lower limit of quantitation of the assay. This means the AUC findings were 1,500% and 12,500% greater than the control for estradiol and estrone, respectively.
Considered an additional step that is readily incorporated into the formulation and manufacturing process of existing or new orally ingestible and topical products, DehydraTECH has been shown to improve the proportion of the drug delivered into the bloodstream (bioavailability) and the absorption of drugs into the brain tissue. Among the drugs that can benefit from these improvements is oral estradiol, which has minimal bioavailability (2% to 10%) due to gut and liver metabolism (https://ibn.fm/kbdx1). This, according to Lexaria, often necessitates high dosages to achieve the desired beneficial effect; but this can, in turn, lead to unwanted side effects. Thus, incorporating DehydraTECH into the manufacturing process of oral estradiol and potentially other human hormone therapies may enhance their oral delivery.
The animal study HOR-A22-1, which is part of Lexaria’s efforts to pursue multiple paths to success by investigating several large market opportunities, represents a foray into the hormone replacement market estimated to grow from $31.06 billion in 2019 to an estimated $46.50 billion by 2027, a 5.1% CAGR (https://ibn.fm/PnAIK).
Meanwhile, Lexaria also announced the closing of its public offering of 2,106,000 units, each consisting of one share of common stock and one warrant to purchase one share of common stock. The offering generated approximately $2.0 million in gross proceeds.
For more information, visit the company’s website at www.LexariaBioscience.com.
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