Optimizing pH-sensitive and time-dependent polymer formula of colonic pH-responsive pellets to achieve precise drug release

Song, Lijun; Liang, Liping; Shi, Xiaoying; Chen, Honglang; Zhao, Shuai; Chen, Wenfeng; Zhou, Ruoxia; Zhao, Wenbin

doi:10.1016/j.ajps.2018.05.012

Cited by 11 publications

(2 citation statements)

References 29 publications

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“…In brief, caffeine and the excipients were dispersed in the coating media and then sprayed onto inert microcrystalline cellulose spheres using a fluid bed through a Wurster tube with continuous inlet air that dries the liquid in the dispersion, to obtain various layers consisting of caffeine and release-controlling polymers. The applied release-controlling polymeric system was based on methacrylate copolymers, which control the release of caffeine in both a pH-dependent and pH-independent manner 29 , 30 . Thereby, the release mechanism of the polymeric system was mainly driven by the swellability and permeability of the copolymers 31 .…”

Section: Methodsmentioning

confidence: 99%

A novel bedtime pulsatile-release caffeine formula ameliorates sleep inertia symptoms immediately upon awakening

Dornbierer

Yerlikaya

Wespi

et al. 2021

Sci Rep

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Sleep inertia is a disabling state of grogginess and impaired vigilance immediately upon awakening. The adenosine receptor antagonist, caffeine, is widely used to reduce sleep inertia symptoms, yet the initial, most severe impairments are hardly alleviated by post-awakening caffeine intake. To ameliorate this disabling state more potently, we developed an innovative, delayed, pulsatile-release caffeine formulation targeting an efficacious dose briefly before planned awakening. We comprehensively tested this formulation in two separate studies. First, we established the in vivo caffeine release profile in 10 young men. Subsequently, we investigated in placebo-controlled, double-blind, cross-over fashion the formulation’s ability to improve sleep inertia in 22 sleep-restricted volunteers. Following oral administration of 160 mg caffeine at 22:30, we kept volunteers awake until 03:00, to increase sleep inertia symptoms upon scheduled awakening at 07:00. Immediately upon awakening, we quantified subjective state, psychomotor vigilance, cognitive performance, and followed the evolution of the cortisol awakening response. We also recorded standard polysomnography during nocturnal sleep and a 1-h nap opportunity at 08:00. Compared to placebo, the engineered caffeine formula accelerated the reaction time on the psychomotor vigilance task, increased positive and reduced negative affect scores, improved sleep inertia ratings, prolonged the cortisol awakening response, and delayed nap sleep latency one hour after scheduled awakening. Based on these findings, we conclude that this novel, pulsatile-release caffeine formulation facilitates the sleep-to-wake transition in sleep-restricted healthy adults. We propose that individuals suffering from disabling sleep inertia may benefit from this innovative approach.Trials registration: NCT04975360.

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Section: Methodsmentioning

confidence: 99%

A novel bedtime pulsatile-release caffeine formula ameliorates sleep inertia symptoms immediately upon awakening

Dornbierer

Yerlikaya

Wespi

et al. 2021

Sci Rep

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“…After 24 h, swollen pellets were extracted from the medium, blotted to dryness, and weighed (W2). The swelling index was computed using equation 2 [16,17].…”

Section: Swelling Index (% W/w)mentioning

confidence: 99%

Formulation of Mesalamine-Loaded Rectal Mucoadhesive Pellets for the Treatment of Inflammatory Bowel Disease Using 32full Factorial Design

VAJA

DETROJA

2022

Int J App Pharm

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Objective: The objective of the present work was to optimize a rectal suppository containing mucoadhesive pellets of Mesalamine to achieve local yet sustained release of Mesalamine for once-a-day administration for the therapy of Inflammatory Bowel Disease. Methods: Thus, the present work involves forming mucoadhesive pellets of mesalamine by extrusion spheronization, which were then loaded into a suppository to be administered rectally. The pellets were evaluated for mucoadhesion strength, swelling potential, morphology, particle size, drug release, drug loading and retention time. Results: The optimized batch of pellets using Eudragit RLPO as the release retardant, carrageenan as a mucoadhesive polymer and other excipients had a mucoadhesion strength of 0.143 N, a swelling index of 50.50 %, and 44 % and 75 % drug was released from them at the end of 6 and 15 h respectively. The pellets-loaded cocoa butter suppositories had a melting range of 35–37 °C, disintegrated within 8–9 min and had a hardness of 4–5 kg/cm3. A comparison of the in vitro drug release profile from the mucoadhesive pellets and the mucoadhesive pellets-loaded suppositories showed a closeness in the % cumulative drug release indicating that cocoa butter did not interfere in the release of the drug from the pellets. Conclusion: Mucoadhesive Pellets were successfully developed by extrusion spheronizer technique and incorporated into suppositories. In vitro study revealed a release profile that warranted a once-a-day regimen leading to a reduction in the requirement of the drug and hence the side effects.

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Design and optimization of pH-sensitive Eudragit nanoparticles for improved oral delivery of triclabendazole

Real

Gagliano

Sonsini

et al. 2022

International Journal of Pharmaceutics

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Optimizing pH-sensitive and time-dependent polymer formula of colonic pH-responsive pellets to achieve precise drug release

Cited by 11 publications

References 29 publications

A novel bedtime pulsatile-release caffeine formula ameliorates sleep inertia symptoms immediately upon awakening

A novel bedtime pulsatile-release caffeine formula ameliorates sleep inertia symptoms immediately upon awakening

Formulation of Mesalamine-Loaded Rectal Mucoadhesive Pellets for the Treatment of Inflammatory Bowel Disease Using 32full Factorial Design

Design and optimization of pH-sensitive Eudragit nanoparticles for improved oral delivery of triclabendazole

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