pH-dependent ileocolonic drug delivery, part II: preclinical evaluation of novel drugs and novel excipients

Broesder, Annemarie; Kosta, Anne-Marijke M A C; Woerdenbag, Herman J.; Nguyen, Duong Nhat; Frijlink, Henderik W.; Hinrichs, Wouter L. J.

doi:10.1016/j.drudis.2020.06.012

Cited by 5 publications

(3 citation statements)

References 148 publications

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“…Analysis of fecal samples from our study cohort confirmed that riboflavin was indeed higher in our intervention groups compared with placebo. Although riboflavin reaches the colon, a more targeted colon delivery by enterically protected capsules may give a better response at lower concentration by avoiding the interfering effects of small intestinal uptake by the host (Broesder et al, 2020 ).…”

Section: Discussionmentioning

confidence: 99%

Riboflavin Supplementation Promotes Butyrate Production in the Absence of Gross Compositional Changes in the Gut Microbiota

Liu

Sadabad

Gabarrini

et al. 2022

Antioxidants & Redox Signaling

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Aims: We performed a randomized, placebo-controlled trial, RIBOGUT, to study the effect of 2 weeks supplementation with either 50 or 100 mg/d of riboflavin on (i) Faecalibacterium prausnitzii abundance, (ii) gut microbiota composition, (iii) short-chain fatty acid (SCFA) profiles, and (iv) the satiety and gut hormones. Results: Neither dose of riboflavin, analyzed separately, impacted the abundance of F. prausnitzii , and only minor differences in SCFA concentrations were observed. However, combining the results of the 50 and 100 mg/d groups showed a significant increase in butyrate production. While the gut bacterial diversity was not affected by riboflavin supplementation, the complexity and stability of the bacterial network were enhanced. Oral glucose tolerance tests showed a trend of increased plasma insulin concentration and GLP-1 after 100 mg/d supplementation. Innovation: Dietary supplements, such as vitamins, promote health by either directly targeting host physiology or indirectly via gut microbiota modulation. Here, we show for the first time that riboflavin intervention changes the activity of the microbiota. The butyrate production increased after intervention and although the composition did not change significantly, the network of microbial interactions was enforced. Conclusion: This RIBOGUT study suggests that oral riboflavin supplementation promotes butyrate production in the absence of major shifts in gut microbiota composition. Identifier: NCT02929459.

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Section: Discussionmentioning

confidence: 99%

Riboflavin Supplementation Promotes Butyrate Production in the Absence of Gross Compositional Changes in the Gut Microbiota

Liu

Sadabad

Gabarrini

et al. 2022

Antioxidants & Redox Signaling

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“…From a preclinical point of view, although most laboratory studies have employed mice as animal models to evaluate the efficiency of polyantibiotic therapies and also nanomedicines, we believe that pigs can be considered as appropriate animal models to check the efficiency of pH‐sensitive nano‐DDSs, due to better similarity between the pH values of the porcine stomach and the human stomach. [ 280,335 ] The pig stomach shows other similarities with the human stomach, such as a cylindrical epithelium and the lack of non‐glandular areas. [ 336 ] A recent review by Ansari and Yamaoka provided some insights regarding appropriate animal models for assessing pathogenesis (e.g., pathogenic roles of virulence factors, potential ability of host‐related factors in the pathogenesis of H. pylori , etc.)…”

Section: The Proposed Solution Using Nanostructured Ddss Against H Py...mentioning

confidence: 99%

Future Nanotechnology‐Based Strategies for Improved Management of Helicobacter pylori Infection

Kamankesh,

Yadegar,

Llopis‐Lorente

et al. 2023

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Helicobacter pylori (H. pylori) is a recalcitrant pathogen, which can cause gastric disorders. During the past decades, polypharmacy‐based regimens, such as triple and quadruple therapies have been widely used against H. pylori. However, polyantibiotic therapies can disturb the host gastric/gut microbiota and lead to antibiotic resistance. Thus, simpler but more effective approaches should be developed. Here, some recent advances in nanostructured drug delivery systems to treat H. pylori infection are summarized. Also, for the first time, a drug release paradigm is proposed to prevent H. pylori antibiotic resistance along with an IVIVC model in order to connect the drug release profile with a reduction in bacterial colony counts. Then, local delivery systems including mucoadhesive, mucopenetrating, and cytoadhesive nanobiomaterials are discussed in the battle against H. pylori infection. Afterward, engineered delivery platforms including polymer‐coated nanoemulsions and polymer‐coated nanoliposomes are poposed. These bioinspired platforms can contain an antimicrobial agent enclosed within smart multifunctional nanoformulations. These bioplatforms can prevent the development of antibiotic resistance, as well as specifically killing H. pylori with no or only slight negative effects on the host gastrointestinal microbiota. Finally, the essential checkpoints that should be passed to confirm the potential effectiveness of anti‐H. pylori nanosystems are discussed.

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“…Therefore, in this study, we developed a ColoPulse coated pellet formulation containing both sulfasalazine and caffeine with a similar pulsatile release profile, which can be used in future clinical studies. Clinical studies in humans are recommended to confirm that this pH-dependent pellet system can be used in humans as a marker for colonic delivery [2], as the pH profile of individual dogs can differ from that of humans [18].…”

Section: Introductionmentioning

confidence: 99%

Formulation and In Vitro Evaluation of Pellets Containing Sulfasalazine and Caffeine to Verify Ileo-Colonic Drug Delivery

et al. 2021

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The ColoPulse coating is a pH-dependent coating that can be used to target drug release to the ileo-colonic region. ColoPulse coated tablets and capsules have demonstrated their targeting capabilities in vivo in more than 100 volunteers and patients. However, so far the ColoPulse coating has not been used for multi-particulate pellet formulations. The sulfasalazine–caffeine method can be used to confirm ileo-colonic drug delivery in vivo. Caffeine serves as a release marker in this method, while sulfasalazine serves as a marker for colonic arrival. In this study, extrusion–spheronization was used to produce microcrystalline cellulose based pellets containing both caffeine and sulfasalazine. Dissolution tests revealed that a superdisintegrant, i.e., croscarmellose sodium or sodium starch glycolate, should be incorporated in the formulation to achieve acceptable release profiles for both sulfasalazine and caffeine. However, acceptable release profiles were only obtained when the pelletizing liquid consisted of ethanol/water 1/1 (v/v) but not with pure water. This phenomenon was ascribed to the differences in the degree of swelling of the superdisintegrant in the pelletizing liquid during the granulation process. The pellets were coated with the ColoPulse coating and showed the desired pH-dependent pulsatile release profile in vitro. In future clinical studies, ileo-colonic targeting should be verified.

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pH-dependent ileocolonic drug delivery, part II: preclinical evaluation of novel drugs and novel excipients

Cited by 5 publications

References 148 publications

Riboflavin Supplementation Promotes Butyrate Production in the Absence of Gross Compositional Changes in the Gut Microbiota

Riboflavin Supplementation Promotes Butyrate Production in the Absence of Gross Compositional Changes in the Gut Microbiota

Future Nanotechnology‐Based Strategies for Improved Management of Helicobacter pylori Infection

Formulation and In Vitro Evaluation of Pellets Containing Sulfasalazine and Caffeine to Verify Ileo-Colonic Drug Delivery

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