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Novel Weight Loss Medications on the Horizon: Needle-Free Options Emerge
A new wave of innovative weight loss medications is nearing availability, promising to eliminate the need for injections. Millions have turned to drugs like Ozempic, Mounjaro, Wegovy, and Zepbound, or their generic counterparts, to achieve weight loss, fundamentally changing the landscape of obesity medicine. These treatments, now widely recognized, have become mainstream, promoted by celebrities and featured in pervasive advertisements. However, these current weight loss drugs are typically administered via injections, a significant obstacle for individuals with needle aversion.
Transdermal Delivery: A Pain-Free Alternative
The latest advancements in obesity medicine are shifting towards less invasive methods, such as creams and patches. These transdermal drug delivery systems offer a needle-free approach to medication administration. Dr. Nicholas Perricone, a respected dermatologist and anti-aging specialist with extensive experience in transdermal drug platforms, suggests this technology could empower numerous individuals who are hesitant about injections to benefit from these weight loss drugs and achieve their health goals.
Topical Gel Formulation of Tirzepatide Under Development
Dr. Perricone is actively developing a topical gel form of tirzepatide, the active ingredient in Mounjaro. He aims to collaborate with Eli Lilly, Mounjaro’s manufacturer, to further develop and distribute this innovative formulation. He believes this approach is promising and possesses unique advantages.
Microneedle Patches: Minimally Invasive Technology
Another promising avenue of research involves developing a small patch, roughly the size of a thumbnail, embedded with microscopic needles. These microneedles are designed to deliver potent doses of weight-loss medication. The minute needles are engineered to penetrate the skin superficially, avoiding deeper pain receptors and blood vessels, rendering them suitable even for those with intense needle phobia.
Topical Tirzepatide Gel: How It Works
Dr. Perricone’s laboratory is concentrating on creating a topical gel formulation of tirzepatide.
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- Skin Penetration: ‘It’s definitely possible to penetrate the skin, reaching the dermalvascular system [blood vessels deep within the skin], enabling systemic circulation and delivering the benefits without an injection,’ Dr. Perricone stated.
- Simple Application: ‘Application is straightforward—simply apply it to your wrist, rub your wrists together, and it absorbs into the skin within approximately one minute, circulating throughout the body.’
Currently, this gel formulation remains experimental, requiring preclinical and human trials before it can be considered for FDA approval.
Semaglutide Creams: Skinvisible Pharmaceuticals’ Innovation
Beyond Dr. Perricone’s work, Skinvisible Pharmaceuticals, based in Las Vegas, is also innovating in topical weight loss treatments. They are formulating a cream version of semaglutide, the active peptide in Ozempic and Wegovy. This cream is designed to enhance skin penetration by tenfold compared to conventional topical drugs, providing a sustained release of medication over six hours.
Clinical Trial Results: Promising Skin Penetration
Trials evaluating the effectiveness of incorporating semaglutide into a cream have yielded encouraging results. Researchers reported that almost 70 percent of the key drug effectively permeated the skin layers at a consistent rate.
- Dual-Action Formula: The cream formulation contains a GLP-1 agonist, similar to semaglutide’s mechanism, combined with a CB-1 receptor antagonist, aiming to curb appetite and stimulate fat breakdown.
- Sustained Release: Skinvisible’s cream technology acts as a delivery mechanism, encapsulating and gradually releasing the peptides.
- Laboratory Testing: Applied to test skin in laboratory settings, scientists measured peptide penetration depth and duration.
Effectiveness and Bioavailability: Ongoing Research
Studies revealed that approximately 10 percent of the medication within the cream permeated the skin over a six-hour period, offering a more controlled and gradual drug delivery compared to injections. However, the efficacy of this delivery method in living tissue remains under investigation. Clinical trials in individuals seeking weight loss are yet to be conducted, and the bioavailability—the proportion of the drug utilized by the body—is still to be determined.
Injectable semaglutide boasts a bioavailability of 50 to 80 percent. The bioavailability of the cream formulation is currently uncertain.
Advantages of Topical Formulations: Reduced Side Effects?
GLP-1 drugs have demonstrated significant success in clinical trials, facilitating average weight loss of 15 to 20 percent of body weight. However, because injections deliver the full dose rapidly, they are associated with side effects, prompting a significant portion of patients to discontinue use within a year.
Common side effects of GLP-1 agonists like Ozempic and Wegovy include severe stomach discomfort, nausea, vomiting, constipation, and diarrhea, significantly impacting users’ daily lives.
Topical formulations offer a potentially appealing alternative. Researchers hypothesize that the steady drug release from topicals, compared to the rapid surge from injections, may mitigate debilitating gastrointestinal side effects.
HeroPatch: Microneedle Patch in Clinical Trials
Anodyne Nanotech, based in Boston, is advancing its HeroPatch, a microneedle patch smaller than a postage stamp, towards clinical trials. One side of the patch features hundreds of microscopic, dissolving needles, each finer than a human hair.
- GLP-1 Agonist Delivery: These microneedles contain concentrated doses of a proprietary GLP-1 agonist, similar in function to semaglutide.
- Painless Application: The patch is designed for painless skin penetration.
- Gradual Release: Upon penetrating the skin, the needles dissolve in skin moisture, gradually releasing the medication payload.
- Absorption Mechanism: The surrounding fluid beneath the skin absorbs the medication, enabling deeper tissue penetration.
- Simple Removal: The needles fully dissolve within hours, leaving a disposable empty patch.
HeroPatch Trial Results and Future Potential
Animal trials conducted last year indicated that the HeroPatch delivered a semaglutide equivalent dose of 3.6mg, exceeding the highest maintenance dose of Wegovy (2.4mg). Company data suggests that a single patch provided steady medication release over a week, although full preliminary results are pending release.
Jake Lombardo, CEO and Co-Founder of Anodyne, envisions the HeroPatch as a transformative technology, not only for GLP-1 delivery but also as a versatile platform for managing other chronic conditions, with the potential to revolutionize patient experiences and enhance global health outcomes.