Advanced Lipid Technologies ® (ALT®) is Sancilio & Company’s (SCI) proprietary drug delivery platform. Our technology leverages patented and trade secreted formulation and manufacturing techniques to create lipophilic drug products capable of overcoming challenges associated with oral administration.
- Increased bioavailability
- Avoidance of the First Pass Effect
- Elimination of the Food Effect
- Reduction of clinical variability
- Enhanced consistency of efficacy
Lipophilic Drug Challenges
Although almost half of all promising pharmaceuticals are lipophilic compounds, the industry has historically faced significant disadvantages orally delivering these compounds. The natural digestion and metabolic processes of the body pose a large hurdle to overcome. Prescribing drug products to be taken with food can still lead to wild bioavailability inconsistency if patients poorly comply and insufficient food is consumed, known as the “Food Effect.” Moreover, as protective as the liver is to the body, it can prevent active pharmaceutical ingredients (API) from reaching the appropriate treatment area in the body by destroying the API on first pass through the portal system. This “First Pass Effect” not only demands the introduction of significantly more API than otherwise needed, but also leads to liver toxicity. Drug products with lipophilic API that are insufficiently designed to meet these challenges can result in high clinical variability, and ultimately failed approval.
Furthermore, drug formulation decisions may hinder drug efficacy. Companies who choose to convert the lipophilic compound to a salt can inadvertently produce a drug product that performs sub-optimally compared to the native lipid. A company may also shy away from one of the most effective means of oral delivery for these compounds because of the difficulty in manufacturing softgel capsules, resulting in dosage forms with less efficacy. Poor formulation decisions at the front end prevent promising drugs from ever reaching the market. Advanced Lipid Technologies® can be a solution.
The Food Effect
The body’s natural process to absorb lipids is extremely inefficient. While the body may absorb nutrients from any other food on an empty stomach, it takes fat to digest fat. Enough fatty food has to make it to the small intestine to stimulate the gall bladder to release the necessary fats and bile salts to properly absorb any lipids through the intestinal lining. Lipophilic medications are treated as lipids by the body and require the same formation of micelles for absorption. Typical dosage requirements state that such medications are to only be taken with food – which varies in the amount of fat, or has no fat if the patient fails to eat food with the drug.
For instance, a patient taking an Omega-3 medication for lowering triglycerides would likely decide to avoid a fatty meal, if they eat at all. As a result, much of the omega-3 oils are never absorbed. Uncomfortable side effects then occur while having little bioavailability or effect.
Seeing this issue as a challenge, SCI scientists sought to create a better dosage form for Omega-3 drugs. Employing the ALT platform, SCI scientists created a dosage form that significantly increased the bioavailability of Omega-3 drugs regardless of food consumption. Commissioning our own study to evaluate this discovery, SCI found that when administered to subjects who concurrently consumed a high fat meal, our formulation provided a similar bioavailability to the current Omega-3 drugs. However, when the subjects skipped a meal, SCI’s formulation had significantly more bioavailability than the currently prescribed Omega-3 products. To learn more about this project, see SC401.
The ALT platform is a unique patented formulation engineered to spontaneously form micelles and effectively mimic the natural release of fats and bile salts while circumventing the needed signals to the digestive system. Right utilization of the Advanced Lipid Technologies with your lipophilic drug can reduce or overcome the Food Effect for your drug products.
First Pass Effect
The liver can be killer on drugs and drugs can be killer on the liver. Neither of these scenarios are good for the patient or the pharmaceutical company struggling to bring a product to market. Yet, a hydrophilic compound suffers from exactly this challenge, absorbing readily through the GI tract but encountering the liver soon after. Natural lipid absorption can avoid the First Pass Effect but is extremely inefficient. Unfortunately, when a lipophilic drug is converted to a hydrophilic compound, the lipophilic compound is cursed with some of the main disadvantages of hydrophilic drugs, including the First Pass Effect.
When a hydrophilic API is administered to patients, the API pays the liver a visit prior to traveling to its intended destination. Many of these compounds can be toxic to the liver and, as a result, greatly increase the product’s side-effect profile. In addition, because the liver (just doing its job) destroys a significant portion of the API that passes through the liver, the dosage form needs to contain significantly more API than is needed for actual treatment. Not only does this cause more side-effects, this extra-large dosage size drives costs through the roof. Rather than transforming a lipophilic API into a hydrophilic API and suffering through the disadvantages associated with hydrophilic API absorption, pharmaceutical companies can now take a different route – deliver the lipids as nature intended.
Lipophilic APIs in their native form are often much more effective than lipids converted into their hydrophilic cousins. Because SCI’s ALT technology hijacks the body’s natural lipid absorption process to efficiently deliver lipids, we’ve enabled pharmaceutical delivery of lipophilic APIs without the First Pass Effect. As a result, manufacturers using ALT-enhanced APIs will likely see significantly lower API cost, less variability in bioavailability of the compound, and happier patients.
Delivery Solutions for Lipophilic Drugs
If your lipophilic drug suffers from poor bioavailability, first pass effect, food effect, lack of stability or high clinical variability, we can help. Contact SCI today for more information about how our Advanced Lipid Technologies ® platform can be used to improve your lipophilic compound delivery.