Oral thin film offers better absorption

October 27, 2015

Article

The area of nutriceutical supplementation for ocular conditions appears to be more contentious than ever. Questions are heatedly argued every day regarding a number of topics, some of which follow. Is this component (nutriceutical) more effective than that component? Does mesozeaxanthin make a difference? Does too much of a good thing-zinc-do more harm than good? Should supplementation be directed by genetic testing results? Does supplementation with omega 3 free fatty acid (FFA) not create a positive effect in ocular disorders?

But the elephant in the room is: “even with the best possible supplementation, is the component getting absorbed efficiently and effectively for utilization.” This concern is clouded by urban legends replete on the Internet regarding recovery of vitamins that have not been absorbed. They are reported to be resting in the bottoms of septic systems.¹

I would posit that recommendations for supplementation without regard to availability for absorption offers questionable value and casts a cloud over any “study” extolling the benefits of supplementation.

The question becomes: Is it possible to bypass the gut to minimize the effects of the unpredictable gastrointestinal system while maximizing absorption?”

As recently as September 2014, a study emphasized the importance of defining the bioavailability of the delivery of the AREDS formulas.²

Nutriceuticals and health

In a perfect world, we would all have magnificent genes obtained from parents without flaws. We would all eat only nutritious foods, exercise, meditate, not eat too much red meat, eat more vegetables, and so on. But that is not human nature-we just cannot resist that stuffed-crust pizza. And then we look for the “magic bullet” to undo all of our nutritional and behavioral sins. “Let’s have a Diet Coke with that stuffed-crust pizza.”

We are all given a bucket of genes and have to deal with what we are given. That being said, there are a number of behavioral characteristics that impact negatively or positively on the manifestation of those genetic tendencies.

• Good genes + smoking = a bad outcome

• Bad genes + smoking = a worse outcome

• Good genes + obesity = a bad outcome

• Bad genes + obesity = a worse outcome

• Bad genes + the trifecta (obesity + smoking + no exercise) = the worst of the worst outcomes

The rest of the story is that even in the worst of situations, modification of behavior and nutritional supplementation in the presence of a non-ideal diet appears to have a positive effect on morbidity and mortality. So we all swallow nutriceuticals with no sense of the bioavailability of what we are taking.

Next: A hard pill to swallow

A hard pill to swallow

Often we try to supplement in the presence of conflicting matters such as dry mouth, making swallowing even more difficult. A 2004 Harris poll cited that a large percentage (40 percent) of American adults have experienced difficulty swallowing pills, even though most have had no problems swallowing food or liquid.³

Of those who experience difficulty swallowing their medications, 14 percent have delayed taking doses of their medication, eight percent have skipped a dose, and four percent have discontinued using their medication.

Another surprising finding is that fewer than one quarter of adults who have difficulty swallowing their medication have ever discussed the problem with a health professional. For a scant 14 percent of these patients surveyed, their health professional brought up the topic of pill-swallowing difficulty, and only 10 percent initiated the conversation themselves.

Other studies support this finding, reporting that 26 percent of patients experienced difficulty with swallowing tablets.⁴ Children and the elderly in extended care facilities are also reported to have similar problems.^5-8

Add to this, potential impact factors that include issues such as:

• Do we take our supplements with or without food? Fat-soluble vitamins have to bind to fat to be delivered.

• How important is drinking water or other fluids with the supplement?

• Do certain foods or beverages alter absorption of supplements?

• How does the health status of the gastrointestinal system impact the absorption of swallowed medications?

A large number of Americans suffer from digestive disorders largely associated with inflammatory conditions.⁹ (See Table 1.)

Bariatric surgery also alters this absorption dynamic in a very significant manner, and those patients must be carefully supplemented and monitored.¹⁰

The pharmacokinetics of any food, drug, or supplement is critical to the ultimate efficacy. The delivery system affects drug absorption. Intra-oral and sublingual delivery are the most efficient delivery systems other than injection.

Both spray and sublingual bypass the concerns associated with difficulty swallowing as well as potential gastrointestinal impact factors. It appears that “melting in the mouth” will enhance the efficacy of absorption.¹¹

Next: Oral thin film technology applied to nutritional supplements

Oral thin film technology applied to nutritional supplements

The oral mucosa affords a unique environment for systemic drug delivery. The oral mucosa is highly vascularized, allowing any drug diffusing across the oral mucosa membranes direct access to the systemic circulation via capillaries and venous drainage while bypassing the hepatic metabolism.

Typically, oral delivery through the gastric tract that presents a drastic change in gastrointestinal (GI) tract pH (from pH 1–2 in the stomach to 7–7.4 in the distal intestine) creates unpredictability.

Likewise, there is an unpredictable GI transit as well as the presence of numerous digestive enzymes coexisting with variable intestinal flora. In contrast to this challenging situation of the GI tract, absorption via the oral cavity offers more favorable opportunities.

Currently, the best example of the use of oral thin film technology (water soluble polymers that rapidly dissolve on the tongue) is the application to breath-refreshment strips. However, many types of drugs may be efficiently delivered by this system, and there is considerable development regarding this delivery system.

Depending upon the application, the disintegration time, which is manipulated by the molecular weight of the polymer film bases, is between 30 seconds to minutes. The onset of action is more rapid than an orally disintegrating tablet and any form of gastrointestinal absorption.¹²

There is little to no risk of aspiration with this delivery system. Additionally, because of bypassing the GI system, it is posited that lower doses would yield higher concentrations. The thin film is also more stable and can be more target-specific than other forms of delivery, which may lead to lower potential dosing of the individual components.¹³

Oral thin film technology also allows for selective distribution. For example, in Macustrips (Macular Health), lutein is designed to release in the oral cavity (mouth), whereas the zinc is designed to release in the GI (gut). The lutein encapsulation is formulated to keep the lutein in a dissociated form. This then makes the lutein more easily absorbed. The zinc encapsulation is designed to release slowly in the gut, providing a more sustained release leading to a more even and longer lasting blood level of zinc.

The current composition of the Macustrip is:

• 500 mg Vitamin C

• 400 IU Vitamin E

• 25 mg zinc

• 10 mg lutein

• 2 mg zeaxanthin

The zinc encapsulation also helps with taste management. Unencapsulated zinc has a very metallic and unpleasant aftertaste.

Conclusion

With advances in delivery systems via the intraoral system to enhance absorption rates, problems associated with taking pills and tablets may soon be alleviated. The oral film technology offers efficient, effective, and safe delivery while effectively maintaining increased absorption.

References:

1. Coughlin E. Are you flushing your vitamins down the toilet? Ezine Articles. Available at: http://ezinearticles.com/?Are-you-Flushing-Your-Vitamins-Down-the-Toilet?&id=298493. Accessed 5/20/15.

2. Johnson EJ, Vishwanathan R, Rasmussen HM, Lang JC. Bioavailability of AREDS1 micronutrients from softgel capsules and tablets: a pilot study. Mol Vis. 2014 Sep 11;20:1228-42.

3. Schwarz Pharma. Press release. 40% of American Adults Report Experiencing Difficulty Swallowing Pills; National Survey Shows Many Failed to Take Medication as Directed Because of Difficulty Swallowing Pills. Available at: http://www.thefreelibrary.com/40%25+of+American+Adults+Report+Experiencing+Difficulty+Swallowing...-a0112187875. Accessed 5/20/15.

4. Avery-Smith W, Dellarosa DM. Approaches to treating dysphagia patients with brain injury. Am J Occup Ther. 1994 Mar;48(3):235-9.

5. Lindgren S, Janzon L. Prevalence of swallowing complaints and clinical findings among 50-79 year-old men and women in an urban population. Dysphagia. 1991;6(4):187-92.

6. Hanawa T, Watanabe A, Tsuchiya T, Ikoma R, Hidaka M, Sugihara M. New oral dosage form for elderly patients: preparation and characterization of silk fibrion gel. Chem Pharm Bul (Tokyo). 1995 Feb;43(2):284-8.

7. Mallet L. Caring for the elderly patient. J Am Pharm Assoc. 1996 Nov;NS36(11):628.

8. Porter S.C. Novel drug delivery: Review of current trends with oral solid dosage forms. Am Pharm Rev. 2009;85:28–35.

9. Digestive Disorders. Total Health Institute. Available at: http://www.totalhealthinstitute.com/digestive-disorders/. Accessed 5/20/15.

10. Stein J, Stier C, Raab H, Weiner R. Review article: The nutritional and pharmacological consequences of obesity surgery. Aliment Pharmacol Ther. 2014 Sep;40(6):582-609.

11. Thosar MM. Intra oral sprays-An overview. Int J of Pharm & Life Sci. 2011 Nov;2(11):1235-1246.

12. Patil SL, Mahaparale PR, Shivnikar MA, Tiwari SS, Pawar KV, Sane PN. Fast dissolving oral films: An innovative drug delivery system and dosage form. Int J Res Rev Pharm App Sci. 2012;2(3):482-496.

13. Biradar S. Bhagavati, S, Kuppasad I. Fast Dissolving Drug Delivery Systems: A Brief Overview. Internet J Pharmacol. 2005;4(2):2009-2021.