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Randomized Controlled Trial
. 2023 Aug;25(8):2236-2242.
doi: 10.1111/dom.15101. Epub 2023 May 3.

Orlistat mouth rinse: Using the tongue to deliver antiobesity medication in a double-blind randomized crossover pilot trial

Stefany D Primeaux  1   2 , Robert Dubin  3 , Frank L Greenway  4
Affiliations
Randomized Controlled Trial

Orlistat mouth rinse: Using the tongue to deliver antiobesity medication in a double-blind randomized crossover pilot trial

Stefany D Primeaux et al. Diabetes Obes Metab. 2023 Aug.

Abstract

Aim: To investigate the effects of an orlistat mouth rinse on the intake of a high-fat meal.

Methods: A double-blind, balanced order, crossover study was conducted in participants (n = 10, body mass index 25-30 kg/m2 ) assigned to receive placebo or orlistat (24 mg/mL) prior to a high-fat meal. Participants were divided into low- or high-fat consumers based on calories consumed from fat following placebo administration.

Results: The orlistat mouth rinse decreased total and fat calories consumed during the high-fat meal in high-fat consumers, and did not alter calories consumed in low-fat consumers (P < 0.05).

Conclusions: Orlistat decreases long-chain fatty acid (LCFA) absorption by inhibiting lipases that breakdown triglycerides. Orlistat mouth rinse decreased fat intake in high-fat consumers, suggesting that orlistat inhibited the detection of LCFAs from the high-fat test meal. Lingual delivery of orlistat is predicted to eliminate the risk of oil incontinence and promote weight loss in individuals who prefer fat.

Keywords: fat sensing; obesity; orlistat; tongue.

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Conflict of interest statement

Disclosure: FLG’s institution receives royalties from licensing a copyright of the Food Craving inventory and shares a small percentage with FLG as one of the creators of the questionnaire. FLG has received consulting fees from the following entities: Altimune, Nutriceutical Corporation, Pfizer, Novmeta Pharma, Jenny Craig, General Nutrition Corporation, Basic Research LLC, Gedeon Richter Pharma, Jazz Pharmaceuticals, and Dr. Reddy’s Laboratories. The following patents were issued and assigned to FLG’s institution: orlistat and geranium oil mouth rinse; synergy of MLR-1023 and menthol; palatable methionine restricted food. The following patents are pending and assigned to FLG’s institution: synergy of albuterol and amylin agonist; synergy of naringenin and beta carotene. FLG participated on the Medpace Board for a registration trial of a drug. FLG owns stock in the following entities: Slim Health Nutrition, Ketogenic Health Systems, Novmeta Pharma, UR Labs, Inc., Rejuvenate Bio, Inc., Energesis Pharmaceuticals, Inc., and Plensat, Inc. Patent(s) issued and assigned to SDP’s institution: orlistat and geranium oil mouth rinse. RD has no conflicts of interest to disclose.

Figures

Figure 1.
Figure 1.
Consumption of a high fat meal was assessed following application of an orlistat mouth rinse. A. Total caloric intake of the test meal was not altered by orlistat, compared to placebo, mouth rinse, when assessed in the full cohort. B. The number of calories from fat during the test meal was not altered by the orlistat mouth rinse in the full cohort. Data is shown as mean α SEM, p=ns.
Figure 2.
Figure 2.
Participants were divided into low- and high-fat consumers based on a medial split analysis from fat calories consumed during the test meal following application of the placebo mouth rinse. A. High-fat consumers consumed more total calories than low-fat consumers and application of orlistat mouth wash decreased total caloric intake in high-fat consumers. B. High-fat consumers consumed more calories from fat during the test meal and orlistat mouth rinse decreased fat calorie intake in high-fat consumers. Data is shown as mean α SEM, * p< .05, **p<.0001.
Figure 3.
Figure 3.
Hormone receptors and their location on taste receptor cells. Hormone location and functions in taste buds. CB1R, cannabinoid receptor type 1; CCK, cholecystokinin; CCK-A, CCK receptor A; GLP-1, glucagon-like peptide 1; GhrelinR; ghrelin receptor; NPY, neuropeptide Y; ObRb, leptin receptor; VIP, vasoactive intestinal peptide; VPAC1&2, VIP receptors; YR, NPY receptor. Reproduced with permission from Besnard et al.
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