Advanced Lipid Technologies® (ALT®) is Sancilio & Company’s (SCI) proprietary drug delivery platform, which leverages SCI’s patented and trade secreted formulation and manufacturing techniques to create lipophilic drug products capable of increased bioavailability, avoidance of the first pass effect, and elimination of the food effects commonly associated with oral administration.
Although almost half of all promising pharmaceuticals are lipophilic compounds, the industry has historically faced significant disadvantages orally delivering these compounds. As a result, many drugs have failed approval because (1) they were converted to a salt form which performed sub-optimally compared to the native lipid, (2) the “Food Effect” – the need to take the product with food – leads to wild bioavailability inconsistency due to varying levels of food and patient compliance, (3) the “First Pass Effect” – the destruction of a significant portion of the delivered API by the liver before the body has an opportunity to transport the API to the appropriate treatment area in the body leads to liver toxicity and the need to introduce significantly more API than otherwise needed, and (4) difficulty making soft gel capsules leads companies to formulate into other dosage forms.
The Food Effect
The body’s natural process to absorb lipids is extremely inefficient. Because the body’s natural lipid absorption process relies upon fats and bile salts, which the body emits into the intestine in response to eating, 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 when taking 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, meaning they create uncomfortable side effects 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 whether co-consumed with food. Commissioning a study to evaluate SCI’s discovery, SCI found that SCI’s formulation provided a similar bioavailability to the current Omega-3 drugs when administered to subjects who concurrently consumed a high-fat meal, but SCI’s formulation had significantly more bioavailability than the currently prescribed Omega-3 products when the subjects skipped a meal. To learn more about this project see SC401.
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. 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.
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. For further information, please contact us at Development@sancilio.com.