Lipid-based novel formulations are advancing menopause management

Menopause is usually diagnosed clinically when a woman hasn’t menstruated for a year due to a decline in ovarian follicular activity. This condition can generally occur around 45–55 years of age. 

In India, there are approximately 150 million women experiencing menopause, as per data shared by the Indian Menopause Society (IMS). The average age of menopause in the country is 46.2 years, as compared to the global average of 51 years.

Menopause is not a sudden event but occurs over several years. Moreover, the hormonal shifts linked to menopause can impact the physical, emotional, mental, and even social well-being of women. A survey conducted last October to coincide with World Menopause Day pointed out that 79 per cent of Indian women feel that menopause has a significant impact on their mental and physical well-being.

Menopause can potentially affect the quality of life

Symptoms experienced during and post the menopausal transition vary significantly from person to person, with some experiencing minimal or no symptoms while others facing severe ones that disrupt daily activities. As per the World Economic Forum, in the UK alone, it is estimated that 14 million working days are lost annually due to menopause and perimenopause. As many as 1 in 10 women experiencing menopausal symptoms resign from their positions at work.

Some common symptoms include hot flashes and night sweats, characterised by sudden sensations of heat in the face, neck, and chest. The physical discomfort, often accompanied by skin flushing, sweating and palpitations, can last several minutes. Other symptoms include menstrual irregularity and flow changes, leading to eventual cessation. Vaginal dryness, painful sexual intercourse and incontinence, insomnia, mood changes, depression and anxiety, are also associated with menopause. Sometimes, bone density is lost, contributing to higher rates of osteoporosis and fractures.

There are also unfavourable shifts in the lipid profile, indicated by a rise in low-density lipoprotein cholesterol (LDL-C) and triglycerides, alongside a decline in high-density lipoprotein cholesterol (HDL-C).

There are complementary medical therapies to manage these symptoms and improve the quality of life while dealing with this life-altering situation. 

Lipid-based drug delivery systems are advancing the frontiers in alleviating menopause-related systems. Here’s a look at how this new technology works. 

Lipid-based delivery formulations for managing menopause

Poorly water-soluble drugs pose a significant challenge in conventional pharmaceutical drug development due to their limited oral bioavailability and therapeutic effectiveness. Lipid-based formulations have emerged as a promising approach to improve the delivery of such drugs by overcoming these challenges.

Several studies have shown that lipid-based formulations significantly enhance drug solubility and dissolution rate compared to conventional formulations. Additionally, encapsulating lipid-based formulations shield the drug from degradation and enhance its stability. Integrating lipid-based formulations into capsules is a promising strategy for improving drug delivery and managing different disorders, ailments, and even bodily conditions like menopause. 

Bilosome-based drug delivery

Progesterone, the natural female sex steroid hormone, is primarily involved in female reproductive functions. It plays a crucial role in preparing the endometrial layer of the uterus for the implantation of a fertilised ovum. The production of progesterone is known to decrease majorly during menopause. 

External administration of progesterone offers several clinical benefits, including the management of secondary amenorrhea, dysfunctional vaginal or uterine bleeding, hormone replacement therapy, treatment of endometrial hyperplasia and contraception.

However, progesterone, classified as a BCS class II drug due to its high lipophilicity, encounters various obstacles with oral delivery. These hurdles include limited water solubility, low oral bioavailability, enzymatic degradation and hepatic first-pass metabolism. Enhancing the oral bioavailability of progesterone remains a critical concern for its long-term treatment.

Today, several innovative lipid vesicular systems are available that enhance the systemic bioavailability of progesterone. Bilosomes are one of them.

A bilosome is an innovative vesicular system integrating bile salts into the bilayer membrane composed of phosphatidylcholine and cholesterol. This combination with bile salts acts as a repellent to bile acids, enhancing the stability of bilosomes compared to liposomes within the gastrointestinal tract (GIT). Moreover, the bilosome system exhibits ultra-deformable properties, further enhancing its functionality.

This improvement is primarily attributed to the vesicles’ enhanced permeability and reduced gastrointestinal tract (GIT) degradation. Thus, the novel bilosome system presents a promising solution to overcome the challenges associated with poor absorption and low oral bioavailability of progesterone.

Phospholipid liposomes to manage menopause-induced anxiety 

In one clinical trial to assess the effectiveness and safety of phospholipid liposomes, a formulation was administered parenterally for managing anxiety and depression associated with menopause. The group treated with phospholipid liposomes exhibited significantly fewer symptoms such as anxious mood, tension, and fear than the placebo group.

Government support is needed to accelerate advancements 

Incorporating lipid-based formulations into menopausal management strategies is a practical and effective approach to improving women’s quality of life during this transformative period. As research in this field continues to evolve, lipid-based delivery systems have the potential to revolutionise menopausal care, offering women tailored and holistic solutions for symptom relief and overall well-being. To catalyse innovation in niche products like lipids-based formulations, the Government must support more research efforts in this field. Offering substantial backing to companies engaged in such research can accelerate advancements. 

Regulatory sanctions, including favourable policies and incentives, can significantly encourage the adoption of lipid-based drug delivery systems to manage natural biological transitions like menopause.