2019
DOI: 10.1126/scitranslmed.aay2602
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A once-a-month oral contraceptive

Abstract: Poor patient adherence to oral contraceptives is the predominant cause of failure of these therapies, leading to unplanned pregnancies that can negatively affect female health worldwide. To improve patient adherence, we developed an oral contraceptive that is administered once a month. Here, we describe the design and report in vivo characterization of a levonorgestrel-releasing gastric resident dosage form in pigs.

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Cited by 35 publications
(32 citation statements)
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“…is significantly limited due to several biological barriers, which include the propensity for enzymatic and acidic degradation in the gastrointestinal (GI) tract and considerably limited permeation across the intestinal mucosal and epithelial cell layers. [4][5][6] Although permeation enhancers like caprates have shown some promise with a GLP-1 peptide drug approved for clinical use, the oral bioavailability of the drug from this formulation is only about 1%. 7 While particles such as liposomes can encapsulate and protect therapeutics against enzymatic degradation, the negatively charged, hydrophobic mucosal membrane lining the intestinal epithelium presents significant steric hindrance to the diffusive transport of such particulate systems.…”
Section: Introductionmentioning
confidence: 99%
“…is significantly limited due to several biological barriers, which include the propensity for enzymatic and acidic degradation in the gastrointestinal (GI) tract and considerably limited permeation across the intestinal mucosal and epithelial cell layers. [4][5][6] Although permeation enhancers like caprates have shown some promise with a GLP-1 peptide drug approved for clinical use, the oral bioavailability of the drug from this formulation is only about 1%. 7 While particles such as liposomes can encapsulate and protect therapeutics against enzymatic degradation, the negatively charged, hydrophobic mucosal membrane lining the intestinal epithelium presents significant steric hindrance to the diffusive transport of such particulate systems.…”
Section: Introductionmentioning
confidence: 99%
“…Given the challenges associated with food effects with respect to physically disturbing the development of transient privileged regions for enhanced transport systems ( 18 ), the capability of withstanding the physical interaction with ingested matter could support a reduction in variability of absorption of drugs. We and our collaborators have previously developed a series of systems to enhance oral drug delivery, ranging from contraceptives to biologics (insulin) ( 15 , 16 , 34 ). Here, we describe a system capable of supporting the delivery of a biologic through the enhancement of a microneedle patch that can interface and transiently fix itself through physical interaction to the mucosa to support enhanced delivery of a biologic.…”
Section: Discussionmentioning
confidence: 99%
“…For instance, Kirtane et al . proposed that an orally administered long-acting gastric resident dosage form composed of V-shaped six polymer arms loaded LNG and connected by an elastomer core, which allowed it to be folded into a capsule for easy oral administration [ 10 ]. After the capsule dissolved in the stomach, the device would form recoils in a larger size than that of the pylorus, so that it could be fixed there and release the drug constantly and steadily (Fig.…”
Section: Advanced Biomaterials For Contraception By Various Routesmentioning
confidence: 99%
“…In recent years, biomaterials-based long-acting reversible contraception has received increasing attention from the viewpoint of fundamental research and practical applications mainly owing to improved delivery routes and controlled drug delivery [ 8 – 10 ]. “Biomaterials are those materials—be it natural or synthetic, alive or lifeless, and usually made of multiple components—that has been engineered to interact with biological systems for a medical purpose—either a therapeutic (treat, augment, repair, or replace a tissue function of the body) or a diagnostic one.” [ 11 , 12 ].…”
Section: Introductionmentioning
confidence: 99%