Delivering Benefits Through Optimized Ingredients and Dosage Form Solutions

Delivery systems in the dietary supplement space encompass several strategies: ingredients optimized for absorption, physical dosage form solutions, and a combination of the two. At the end of the day, the goal is to ensure the ingredients in a formula deliver the advertised benefits. Marketing is another factor. Being able to claim an ingredient is highly bioavailable, or being able to deliver an effective dose in as few tablets, capsules, or gummies as possible, are great ways to stand out on the shelf. Whatever your goals for delivering your formulas, understanding the possibilities and limitations of the various options goes a long way toward achieving them.

Big Picture on Bioavailability

Bioavailability is a very important factor. It means an ingredient is being maximally absorbed by the body to deliver the intended benefits. There are several ways ingredient suppliers can enhance the bioavailability of ingredients, many of which are effective, but it’s important to be able to separate realistic claims from marketing hype. For example, greater bioavailability does not necessarily equal greater effectiveness.

“Simply increasing systemic exposure does not guarantee a better outcome if the bioactive is not delivered in the right form, at the right site, or in a way the body can meaningfully utilize,” notes Trisha Sugarek MacDonald, PhD, MS, marketing development manager for Akay Bioactives, an Oterra company.

Tanja Kokkinis, communications and brand manager for Pharmako Biotechnologies, agrees. “Ultimately, what really matters is how the ingredient behaves once it’s in the body, whether it’s used efficiently and delivers a genuine benefit,” she adds. “In some cases, pushing absorption higher doesn’t necessarily translate to better outcomes, and it can actually present other challenges, such as stability issues or inconsistent performance.”

In the case of botanical actives, for example, MacDonald notes that in actives such as polyphenols, the reported bioavailability includes both free and conjugated metabolites. “While these forms are more water-soluble and circulate at higher levels in plasma, they may have reduced cellular permeability and lower biological activity compared to the unconjugated, or free, bioactive form,” she explains. “From a functional standpoint, what matters most is the availability of the active form at the target site, along with the kinetics of delivery.”

To address this, Akay utilizes a fenugreek fiber hydrogel matrix, called FenuMat, to embed bioactives, protect them from digestion, and control the release. This is beneficial for ingredients like curcumin. “[Curcumin] is inherently poorly absorbed, with very low levels of ‘free’ curcumin detected in circulation due to rapid metabolism and conjugation in the intestine and liver,” MacDonald explains. “These conjugated forms are larger [molecular weight >500 Da; eg, curcumin glucuronide ~544.5 Da], more hydrophilic, and generally less efficient at crossing cell membranes compared to the smaller, lipophilic free form [molecular weight ~368 Da], which is more biologically active and better able to cross physiological barriers such as the blood-brain barrier.”

A curcumin complex formulated with FenuMat was shown in a randomized, double-blind, crossover study to significantly increase the bioavailability of free curcuminoid by 45.5-fold, compared to standard curcumin.¹

Another way to enhance bioavailability and absorption is by using liposomal technology. Liposomes are sphere-shaped vesicles composed of phospholipid bilayers and a liquid core that are designed to mimic cell membranes. This allows them to enter the bloodstream, where they can reach their target in higher concentrations.² While liposomes can be highly effective, brands should still be dubious of liposomal ingredients that overpromise.

“Ingredients marketed around advanced delivery, like liposomes, need to be evaluated in the context of how they perform in a finished product, how stable they are, and whether the delivery benefit is maintained through the manufacturing process and everyday use,” says Kokkinis. “Bioavailability needs to support effectiveness rather than [be] treated as the benefit on its own.”

What Does Bioavailability Mean for Dose Size?

One advantage of enhancing bioavailability is a smaller effective dose, allowing the manufacturer to use smaller capsules or tablets and for the end user to take fewer. Consumers want supplements “that are more convenient, easier to take, and more consistent in how they perform,” says Kokkinis. “Better delivery can allow manufacturers and brands to simplify dosing that can reduce pill fatigue and design products that fit more desirably into a consumer’s daily routine.”

While supplements need to fit neatly into consumers’ routines, consumers also care deeply about efficacy, says MacDonald. “It’s not just about using less; it’s also about delivering the right amount in a form the body can actually utilize for that structure/function benefit,” she explains. “And, increasingly, consumers recognize that efficacy matters and are more willing to invest in products that deliver real results rather than spend on options that fall short and ultimately waste money.”

“Smaller doses are often the result of improved delivery rather than the primary goal,” adds Kokkinis. “The focus is really on improving the overall experience, in terms of both consumer compliance and product performance.”

How to Choose the Right Dosage Form

The final dosage form should complement the characteristics of the active ingredients. “Formats like tablets, gummies, capsules, and softgels all place different demands on an ingredient during production and digestion,” says Kokkinis. “Liposomal systems in particular can be sensitive to heat, pressure, moisture, and even dehydration. If the dosage form isn’t aligned with the delivery technology, the benefit can be reduced, or in some cases, risk being lost entirely.”

“Even highly optimized ingredients can lose effectiveness if placed into a format that does not support their delivery characteristics,” offers MacDonald. “For example, poorly dispersible actives in a beverage or gummy may result in sedimentation, inconsistent dosing, or reduced absorption. Similarly, compression forces in tablets or excipient interactions can impact release profiles.”

Softgels are one example of a dosage form that is used to protect, stabilize, and enhance the effectiveness of ingredients, such as omega-3 fatty acids, which are prone to oxidation. Gelita, for example, offers gelatin-based softgels that can offer rapid release (Rapisol) for products like nootropics and sleep support formulas, as well as delayed release (Delasol) to transport oxidation-prone ingredients. There is also the problem of crosslinking to consider.

“Evolving market demands and the rise of nutraceuticals such as botanicals, with reactive ingredients like polyphenols, aldehydes, and ketones, have created stability challenges for softgel manufacturers,” explains Angie Rimel, marketing communications manager for Gelita. “These ingredients have a tendency to crosslink with gelatin softgel shells. Additional factors, such as storage, temperature, and humidity, can exacerbate and accelerate crosslinking too.”

For this purpose, the company offers a portfolio of softgels (RXL) that reduce gelatin’s ability to interact with reactive molecules.

Hard capsules are another reliable option. Lonza Capsugel, for example, recently launched an organic-certified hard capsule (Organicap) made from pullulan, which is ideal for preventing the degradation of oxygen-sensitive ingredients because of its high oxygen barrier. “[The capsules] feature a high oxygen barrier, nonreactive shell, excellent polymer stability, and proven filling performance,” says Kristin Dalton, associate director, product management, specialty polymers for Lonza Capsugel. “This allows for optimal stability and protection, which means formulators can be confident that the potency of their most sensitive organic powder ingredients is preserved.”

Vegan capsule options, such as HPMC (hydroxypropyl methylcellulose), also offer advantages for hydroscopic ingredients, such as functional mushrooms.

An accessible format for consumers, but one that can be challenging to work with, is gummies. “Balancing palatability and effectiveness in gummy formulations is a key challenge, especially as consumers expect both great taste and real health benefits from their supplements,” says Rimel. “We work closely with our partners to help them achieve this balance by leveraging ingredient expertise and innovative technologies.”

For example, the company’s collagen peptides and gelatins are designed to be neutral in flavor, with high solubility. “[This] allows formulators to incorporate effective doses of actives like collagen, vitamins, or botanicals without negatively impacting flavor or texture,” she explains. “This is crucial for consumer acceptance, especially in products with higher functional loads.”

Additionally, flavor maskers, natural flavors, and sweeteners are also used to offset challenging flavor notes from active ingredients. Managing flavor and texture while also delivering effective doses is the primary challenge of gummy manufacturing.

This is only a small snapshot of the complex landscape of delivery systems. Still, it illustrates the nuances and complexities that inform how products are formulated to deliver the ideal user experience and maximal benefit to consumers.

References

1. Kumar D, Jacob D, Subash PS, et al. Enhanced bioavailability and relative distribution of free (unconjugated) curcuminoids following the oral administration of a food-grade formulation with fenugreek dietary fibre: a randomised double-blind crossover study. J Funct Foods. 2016;22:578-587. doi:10.1016/j.jff.2016.01.039
2. Straus M. Lively liposomes. Nutritional Outlook. November 15, 2024. Accessed April 17, 2026. https://www.nutritionaloutlook.com/view/lively-liposomes