Tolmetin sodium-loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks

Akl, Mohamed A.; Ismael, Hatem R.; Abd-Allah, Fathy I.; Kassem, Alla A; Samy, Ahmed M.

doi:10.1080/03639045.2018.1534858

Cited by 26 publications

(19 citation statements)

References 51 publications

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“…One of the main advancements in conventional rectal dosage forms is the development of liquid suppositories, which more closely resemble semi-solid dosage forms rather than solid dosage forms. This includes the development of liquid suppositories containing thermosensitive polymers (Miyazaki et al, 1998; Fakhar Ud and Khan, 2019), mucoadhesive polymers (Koffi et al, 2008; Ye et al, 2016; Xu et al, 2017; Shi et al, 2019), or a combination of thermosensitive and mucoadhesive polymers (Choi et al, 1998; Yun et al, 1999; Ryu et al, 1999; Koffi et al, 2008; Barakat, 2009; Lo et al, 2013; Liu et al, 2018; Akl et al, 2019). Poloxamers are the most commonly used thermosensitive polymers in pharmaceutical formulation.…”

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

“…They are nontoxic amphiphilic molecules that exhibit reverse thermal gelation. This allows them to remain in a liquid state at room temperature and convert into a gel consistency at body temperature, thereby allowing ease of administration into the body, reduced leakage, restricted spreading in the rectal cavity, and improved contact with the rectal mucosal surface (Yong et al, 2001; Barakat, 2009; Akl et al, 2019). Poloxamer molecules form small micellar units at room temperature and large micellar cross-linked network at body temperature (Akl et al, 2019).…”

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

“…This allows them to remain in a liquid state at room temperature and convert into a gel consistency at body temperature, thereby allowing ease of administration into the body, reduced leakage, restricted spreading in the rectal cavity, and improved contact with the rectal mucosal surface (Yong et al, 2001; Barakat, 2009; Akl et al, 2019). Poloxamer molecules form small micellar units at room temperature and large micellar cross-linked network at body temperature (Akl et al, 2019). However, poloxamer gels on their own can have inadequate mucoadhesion, weak mechanical strength, and high permeability to water (Yong et al, 2001; Barakat, 2009; Akl et al, 2019).…”

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

“…Poloxamer molecules form small micellar units at room temperature and large micellar cross-linked network at body temperature (Akl et al, 2019). However, poloxamer gels on their own can have inadequate mucoadhesion, weak mechanical strength, and high permeability to water (Yong et al, 2001; Barakat, 2009; Akl et al, 2019).…”

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

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Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Hua

2019

Front. Pharmacol.

137

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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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Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

Section: Conventional Rectal Drug Delivery Approachesmentioning

confidence: 99%

See 2 more Smart Citations

Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Hua

2019

Front. Pharmacol.

137

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“…The diazepam rectal gel demonstrated good safety and efficacy in the management of seizures in children and adults [ 117 , 118 ]. In addition, thermo-sensitive gel formulations using polymers such as poloxamers are being developed to allow the formulation to remain in a liquid state at room temperature for the ease of application, but undergo gelation at body temperature in order to prolong retention time, with reduced leakage [ [119] , [120] , [121] ].…”

Section: Rectal Deliverymentioning

confidence: 99%

Transmucosal drug administration as an alternative route in palliative and end-of-life care during the COVID-19 pandemic

Lam

Cheung

Chow

et al. 2020

Advanced Drug Delivery Reviews

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The Coronavirus disease 2019 (COVID-19) pandemic has led to a surge in need for alternative routes of administration of drugs for end of life and palliative care, particularly in community settings. Transmucosal routes include intranasal, buccal, sublingual and rectal. They are non-invasive routes for systemic drug delivery with the possibility of self-administration, or administration by family caregivers. In addition, their ability to offer rapid onset of action with reduced first-pass metabolism make them suitable for use in palliative and end-of-life care to provide fast relief of symptoms. This is particularly important in COVID-19, as patients can deteriorate rapidly. Despite the advantages, these routes of administration face challenges including a relatively small surface area for effective drug absorption, small volume of fluid for drug dissolution and the presence of a mucus barrier, thereby limiting the number of drugs that are suitable to be delivered through the transmucosal route. In this review, the merits, challenges and limitations of each of these transmucosal routes are discussed. The goals are to provide insights into using transmucosal drug delivery to bring about the best possible symptom management for patients at the end of life, and to inspire scientists to develop new delivery systems to provide effective symptom management for this group of patients.

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Selective Pd^II‐Catalyzed Acylation of Pyrrole with Aldehydes. Application to the Synthesis of Celastramycin Analogues and Tolmetin

et al. 2020

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The PdII‐catalyzed C‐2 acylation of pyrrole with aldehydes in the presence of TBHP as oxidant has been studied for the synthesis of di(hetero)aryl ketones. The use of 2‐pyrimidine as directing group leads to 2‐acylpyrroles in moderate to good yields, although 2,5‐diacylpyrroles are obtained as by products. This side‐reaction could be avoided using 3‐methy‐2‐pyridine as directing group, obtaining selectively 2‐acylpyrroles. The reaction has been extended to a series of aromatic and heteroaromatic aldehydes, obtaining the best results with electron rich aromatic aldehydes. The methodology has been applied in the synthesis of pyrrolomycin alkaloid Celastramycin analogues and for an improved synthesis of Tolmetin, a nonsteroidal anti‐inflammatory drug.

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Tolmetin sodium-loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks

Cited by 26 publications

References 51 publications

Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Transmucosal drug administration as an alternative route in palliative and end-of-life care during the COVID-19 pandemic

Selective Pd^II‐Catalyzed Acylation of Pyrrole with Aldehydes. Application to the Synthesis of Celastramycin Analogues and Tolmetin

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Tolmetin sodium-loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks

Cited by 26 publications

References 51 publications

Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Physiological and Pharmaceutical Considerations for Rectal Drug Formulations

Transmucosal drug administration as an alternative route in palliative and end-of-life care during the COVID-19 pandemic

Selective PdII‐Catalyzed Acylation of Pyrrole with Aldehydes. Application to the Synthesis of Celastramycin Analogues and Tolmetin

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Product

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About

Selective Pd^II‐Catalyzed Acylation of Pyrrole with Aldehydes. Application to the Synthesis of Celastramycin Analogues and Tolmetin