Improved systemic delivery of insulin by condensed drug loading in a dimpled suppository

Matsumoto, Akira; Murakami, Kazunori; Watanabe, Chie; Murakami, Masahirô

doi:10.5582/ddt.2017.01072

Cited by 6 publications

(6 citation statements)

References 34 publications

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“…In order to achieve focused drug release in a specific direction, we have recently demonstrated that the condensation of insulin within a limited surface area or the dimple of a hard-fat suppository, which releases a high concentration of insulin only toward the mucosal side within a limited area, reduces blood glucose levels following rectal administration (40). This supports our concept shown in Figure 1.…”

Section: Discussionsupporting

confidence: 77%

Janus microspheres for enhanced enteral drug delivery: Preparation and orientated attachment to a Caco-2 monolayer

Matsumoto

Watanabe

Murakami

2019

DD&T

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Section: Discussionsupporting

confidence: 77%

Janus microspheres for enhanced enteral drug delivery: Preparation and orientated attachment to a Caco-2 monolayer

Matsumoto

Watanabe

Murakami

2019

DD&T

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“…Furthermore, dimple-type suppositories were developed by Matsumoto et al (2017) to improve the rectal delivery of poorly absorbable drugs such as peptides and oligonucleotides. These suppositories have one or more dimples on the surface where drugs are embedded.…”

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

“…In addition, limiting the drug concentration toward the surface of the suppository increases its contact with the rectal mucosal surface and creates a concentration gradient for passive absorption of the drug across the mucosa. Interestingly, in vitro release studies showed that the time to 50% drug release was dependent on the melting point of the lipid used for sealing the dimples and not on the number of dimples (Matsumoto et al, 2017).…”

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

“…In addition, there are an increasing number of studies investigating the potential of rectal drug delivery for the treatment of more chronic conditions, including diabetes (Matsumoto et al, 2017; Shi et al, 2019), infections (das Neves et al, 2013; Ham and Buckheit, 2017; Nunes et al, 2018), hypertension (Abou el Ela Ael et al, 2016), asthma (Shiohira et al, 2009), chronic anal fissure (Ivanova et al, 2019), and cancer (Lo et al, 2013; Seo et al, 2013; Ye et al, 2016; Din et al, 2017). Although encouraging results were reported in these studies, with many designed for sustained release activity, they generally did not evaluate the formulations over a long study period.…”

Section: Considerations For Translational Developmentmentioning

confidence: 99%

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Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Hua

2019

Front. Pharmacol.

129

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Although the oral route is the most convenient route for drug administration, there are a number of circumstances where this is not possible from either a clinical or pharmaceutical perspective. In these cases, the rectal route may represent a practical alternative and can be used to administer drugs for both local and systemic actions. The environment in the rectum is considered relatively constant and stable and has low enzymatic activity in comparison to other sections of the gastrointestinal tract. In addition, drugs can partially bypass the liver following systemic absorption, which reduces the hepatic first-pass effect. Therefore, rectal drug delivery can provide significant local and systemic levels for various drugs, despite the relatively small surface area of the rectal mucosa. Further development and optimization of rectal drug formulations have led to improvements in drug bioavailability, formulation retention, and drug release kinetics. However, despite the pharmaceutical advances in rectal drug delivery, very few of them have translated to the clinical phase. This review will address the physiological and pharmaceutical considerations influencing rectal drug delivery as well as the conventional and novel drug delivery approaches. The translational challenges and development aspects of novel formulations will also be discussed.

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“…One study suggested rectal administration of insulin condensed dimple suppository since secretory degrative enzymes are much lower in the rectum than that of the stomach [66]. Insulin was condensed in a dimple with Labrasol ® as absorption enhancer, then it was covered by sealing materials to direct its release toward rectal mucosa only and prevent insulin dilution by rectal fluid, hence offering a higher concentration gradient and improved absorption.…”

Section: Rectal Administrationmentioning

confidence: 99%

Recent Advances and Future Prospects of Non-Invasive Insulin Delivery Systems

2019

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Non-invasive insulin delivery systems have been of global interest. The goal of many studies was to optimize suitable delivery formulation capable of producing comparable insulin bioavailability and safety that match or supersedes conventional delivery by the invasive subcutaneous (SC) injections. Historically, Pfizer have not secured US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) marketing approval yet. Different technologies to improve insulin's permeation and absorption through different routes are in the pipelines. This review discusses several non-invasive strategies that have been appropriately tested and duly approved by the FDA. Other delivery systems are in different phases of development, ranging from in vitro studies to phase 3 clinical trials, providing indications towards the prospects of next-generation delivery systems. This review covers studies published in the past 10 y using Scopus, Clinicaltrials.gov, PubMed and Google scholar databases. The outcomes of this review indicate that the door is still open for more innovative, efficient and convenient non-invasive insulin delivery systems than currently available which may take several years before we can see a game changer in the market. ® , Oral-Lyn ™ I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s

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Improved systemic delivery of insulin by condensed drug loading in a dimpled suppository

Cited by 6 publications

References 34 publications

Janus microspheres for enhanced enteral drug delivery: Preparation and orientated attachment to a Caco-2 monolayer

Janus microspheres for enhanced enteral drug delivery: Preparation and orientated attachment to a Caco-2 monolayer

Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Recent Advances and Future Prospects of Non-Invasive Insulin Delivery Systems

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