OPTICORE™, an innovative and accurate colonic targeting technology

Varum, Felipe; Freire, Ana Cristina; Bravo, Roberto; Basit, Abdul W.

doi:10.1016/j.ijpharm.2020.119372

Cited by 66 publications

(36 citation statements)

References 75 publications

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“…Specifically, ulcerative colitis is characterised by inflammation of the colon and the rectum. Despite being an inflammatory condition of the distal gastrointestinal tract, the majority of efforts for new treatments have revolved around the development of oral therapies [3] , [4] , [5] . However, oral delivery in ulcerative colitis is challenging as potentially only a fraction of the administered drug might reach the intended site of action.…”

Section: Introductionmentioning

confidence: 99%

3D printed tacrolimus suppositories for the treatment of ulcerative colitis

Seoane-Viaño

Ong

Luzardo-Álvarez

et al. 2021

Asian Journal of Pharmaceutical Sciences

Self Cite

100

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Ulcerative colitis is a global health problem, affecting millions of individuals worldwide. As an inflammatory condition localised in the large intestine, rectal delivery of immunosuppressive therapies such as tacrolimus is a promising strategy to maximise drug concentration at the site of action whilst minimising systemic side effects. Here, for the first time, self-supporting 3D-printed tacrolimus suppositories were prepared without the aid of moulds using a pharmaceutical semi-solid extrusion (SSE) 3D printer. The suppositories were printed vertically in three different sizes using combinations of two lipid pharmaceutical excipients (Gelucire 44/14 or Gelucire 48/16) and coconut oil. Although both suppository formulations had the appropriate viscosity characteristics for printing, the Gel 44 formulation required less energy and force for extrusion compared to the Gel 48 system. The Gel 44 disintegrated more rapidly but released tacrolimus more slowly than the Gel 48 suppositories. Although the tacrolimus release profiles were significantly different, both suppository systems released more than 80% drug within 120 min. DSC and XRD analysis was inconclusive in determining the solid-state properties of the drug in the suppositories. In summary, this article reports on the fabrication of 3D printed self-supporting suppositories to deliver personalised doses of a narrow therapeutic index drug, with potential benefits for patients with ulcerative colitis.

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Section: Introductionmentioning

confidence: 99%

3D printed tacrolimus suppositories for the treatment of ulcerative colitis

Seoane-Viaño

Ong

Luzardo-Álvarez

et al. 2021

Asian Journal of Pharmaceutical Sciences

Self Cite

100

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“…91,92 For example, fermentable carbohydrate coatings have been developed for accurate colonic drug delivery. 93,94 Supplied with information on a drug compound, ML can quickly and accurately assess formulation options without bias. 95 Due to the complex nature of formulation science, deep ML techniques are especially useful.…”

Section: Figurementioning

confidence: 99%

Harnessing machine learning for development of microbiome therapeutics

et al. 2021

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The last twenty years of seminal microbiome research has uncovered microbiota's intrinsic relationship with human health. Studies elucidating the relationship between an unbalanced microbiome and disease are currently published daily. As such, microbiome big data have become a reality that provide a mine of information for the development of new therapeutics. Machine learning (ML), a branch of artificial intelligence, offers powerful techniques for big data analysis and predictionmaking, that are out of reach of human intellect alone. This review will explore how ML can be applied for the development of microbiome-targeted therapeutics. A background on ML will be given, followed by a guide on where to find reliable microbiome big data. Existing applications and opportunities will be discussed, including the use of ML to discover, design, and characterize microbiome therapeutics. The use of ML to optimize advanced processes, such as 3D printing and in silico prediction of drug-microbiome interactions, will also be highlighted. Finally, barriers to adoption of ML in academic and industrial settings will be examined, concluded by a future outlook for the field.

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“…Studies with Phloral were continued by Varum et al [119], which explored the relationship between the manufacturing process and the behavior of the coating tablets. Moreover, a new 5-ASA formulation based on Phloral technology embedded into OPTICORE ® technology was recently developed by this research team [48]. This coating technology consists of combining an alkaline inner layer to accelerate drug release with an enteric outer layer consisting of a mixture of Eudragit S and resistant starch, in order to combine pH and bacterial drug release strategies.…”

Section: Oral Cdds Following a Dual Or Combined Approachmentioning

confidence: 99%

“…Therefore, pH-sensitive polymers were the first strategy to achieve colonic drug delivery. Enteric polymers that are most commonly used are copolymers of metacrylic acid and methyl metacrilate (Eudragit ® S, Eudragit ® L, Eudragit ® FS, Eudragit ® L30D-55, Eudragit ® P4135F) HPMCAS-LF (hypromellose acetate succinate), HP50 (hydropromellose phthalate50), and HP55 (hydropromellose phthalate55) [ 48 , 49 , 50 ]. These materials could be used to coat tablets, capsules, matrix, liposomes, and so on, in order to successfully encapsulate drugs with different lipophilia [ 49 , 51 ].…”

Section: Oral Cdds For Ibd Managementmentioning

confidence: 99%

New Insights of Oral Colonic Drug Delivery Systems for Inflammatory Bowel Disease Therapy

Teruel

González‐Álvarez

Bermejo

et al. 2020

IJMS

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Colonic Drug Delivery Systems (CDDS) are especially advantageous for local treatment of inflammatory bowel diseases (IBD). Site-targeted drug release allows to obtain a high drug concentration in injured tissues and less systemic adverse effects, as consequence of less/null drug absorption in small intestine. This review focused on the reported contributions in the last four years to improve the effectiveness of treatments of inflammatory bowel diseases. The work concludes that there has been an increase in the development of CDDS in which pH, specific enzymes, reactive oxygen species (ROS), or a combination of all of these triggers the release. These delivery systems demonstrated a therapeutic improvement with fewer adverse effects. Future perspectives to the treatment of this disease include the elucidation of molecular basis of IBD diseases in order to design more specific treatments, and the performance of more in vivo assays to validate the specificity and stability of the obtained systems.

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OPTICORE™, an innovative and accurate colonic targeting technology

Cited by 66 publications

References 75 publications

3D printed tacrolimus suppositories for the treatment of ulcerative colitis

3D printed tacrolimus suppositories for the treatment of ulcerative colitis

Harnessing machine learning for development of microbiome therapeutics

New Insights of Oral Colonic Drug Delivery Systems for Inflammatory Bowel Disease Therapy

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