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Pharmaceuticals
Special Issues
Recent Advances in Stomach and Intesinal Drug Delivery Systems
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Recent Advances in Stomach and Intesinal Drug Delivery Systems

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (30 November 2022) | Viewed by 5785

Special Issue Editor

Dr. Agustin Rascon-Chu

E-Mail Website
Guest Editor
Coordinación de Tecnología en Alimentos de Origen Vegetal, Centro de Investigación en Alimentación y Desarrollo, A.C., Carretera Gustavo Enrique Astiazarán Rosas No. 46, Col. La Victoria, Hermosillo 83304, CP, Mexico
Interests: drug delivery; micro and nanoparticles; biopolymers; plant and fungi polysaccharides
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

I am delighted to invite you to submit to a Special Issue of the open access journal Pharmaceuticals that will cover the most "Recent Advances in Stomach and Intestinal Drug Delivery Systems".

Stomach and Intestinal Drug Delivery Systems are of great scientific interest, and many relevant innovations have been developed in recent decades. Oral delivery of drugs is one of the most common methods of administration, with high patient compliance. Nevertheless, the gastric system is more complex than it appears, with different difficulties considering all different organs involved. Oral delivery systems represent an important strategy to overcome physiological features, drug solubilisation and bioavailability; the capacity to restrain or locate drug delivery, gut metabolism, absorption, membrane permeability, and even counter-transport processes are a few of many challenges to overcome.

Knowledge, creativity, and innovation characterize the scientific community while undertaking challenges such as drug stabilization and absorption enhancement, new sources of biocompatible materials, and diverse biomaterial sources. Designs for new matrices and vehicles to target specific sites for delivery are ever-growing publications in specialized journals, providing new strategies to alleviate symptoms and treat diseases.

This Special Issue is intended to host research and review papers on the latest and most promising developments on drug-delivery systems for the stomach and intestine, aiming to facilitate improved therapy drug bioavailability, patient compliance, improved efficiency, and targeted delivery.

Dr. Agustin Rascon-Chu
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • stomach delivery
  • intestinal delivery
  • meso–nanostructured carriers
  • micro–nanoparticles/capsules
  • permeability enhancement
  • stability
  • absorption enhancement
  • gut delivery

Published Papers (3 papers)

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Research

14 pages, 2246 KiB  
Article
Arabinoxylans-Based Oral Insulin Delivery System Targeting the Colon: Simulation in a Human Intestinal Microbial Ecosystem and Evaluation in Diabetic Rats
by Ana L. Martínez-López, Elizabeth Carvajal-Millan, Rafael Canett-Romero, Satya Prakash, Agustín Rascón-Chu, Yolanda L. López-Franco, Jaime Lizardi-Mendoza and Valerie Micard
Pharmaceuticals 2022, 15(9), 1062; https://doi.org/10.3390/ph15091062 - 26 Aug 2022
Cited by 7 | Viewed by 1842
Abstract
Arabinoxylans (AX) microcapsules loaded with insulin were prepared by enzymatic gelation of AX, using a triaxial electrospray method. The microcapsules presented a spherical shape, with an average size of 250 µm. The behavior of AX microcapsules was evaluated using a simulator of the [...] Read more.
Arabinoxylans (AX) microcapsules loaded with insulin were prepared by enzymatic gelation of AX, using a triaxial electrospray method. The microcapsules presented a spherical shape, with an average size of 250 µm. The behavior of AX microcapsules was evaluated using a simulator of the human intestinal microbial ecosystem. AX microcapsules were mainly (70%) degraded in the ascending colon. The fermentation was completed in the descending colon, increasing the production of acetic, propionic, and butyric acids. In the three regions of the colon, the fermentation of AX microcapsules significantly increased populations of Bifidobacterium and Lactobacillus and decreased the population of Enterobacteriaceae. In addition, the results found in this in vitro model showed that the AX microcapsules could resist the simulated conditions of the upper gastrointestinal system and be a carrier for insulin delivery to the colon. The pharmacological activity of insulin-loaded AX microcapsules was evaluated after oral delivery in diabetic rats. AX microcapsules lowered the serum glucose levels in diabetic rats by 75%, with insulin doses of 25 and 50 IU/kg. The hypoglycemic effect and the insulin levels remained for more than 48 h. Oral relative bioavailability was 13 and 8.7% for the 25 and 50 IU/kg doses, respectively. These results indicate that AX microcapsules are a promising microbiota-activated system for oral insulin delivery in the colon. Full article
(This article belongs to the Special Issue Recent Advances in Stomach and Intesinal Drug Delivery Systems)
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20 pages, 5182 KiB  
Article
Development of Novel Unfolding Film System of Itopride Hydrochloride Using Box-Behnken Design—A Gastro Retentive Approach
by Shaima Alaithan, Nimbagal Raghavendra Naveen, Prakash S. Goudanavar, Penmetsa Durga Bhavani, Beveenahalli Ramesh, Naga Prashant Koppuravuri, Santosh Fattepur, Nagaraja Sreeharsha, Anroop B. Nair, Bandar E. Aldhubiab, Pottathil Shinu and Rashed M. Almuqbil
Pharmaceuticals 2022, 15(8), 981; https://doi.org/10.3390/ph15080981 - 10 Aug 2022
Cited by 5 | Viewed by 1971
Abstract
Currently, gastro-retentive dosage forms achieved a remarkable position among the oral drug delivery systems. This is a broadly used technique to hold the drug delivery systems for a long duration in the gastro intestine (GI) region, slow drug delivery, and overcome other challenges [...] Read more.
Currently, gastro-retentive dosage forms achieved a remarkable position among the oral drug delivery systems. This is a broadly used technique to hold the drug delivery systems for a long duration in the gastro intestine (GI) region, slow drug delivery, and overcome other challenges related to typical oral delivery such as low bioavailability. The current work aimed to formulate and characterize a new expandable gastro-retentive system through Itopride Hydrochloride (IH)’s unfolding process for controlled release. The IH-loaded unfolding film formulation was optimized using the Box-Behnken design for folding endurance and length of tested layer (LTL). Initially, the formulation was made using several anti-adhesive additives to promote the unfolding mechanism. Citric acid and sodium bicarbonate were selected as anti-adhesives based on these results. The enfolded film in a capsule shell was shown to unroll in the stomach fluids and render drug delivery up to 12 h in acidic conditions. A fabricated system should have dimensions more than the size of the relaxed pyloric sphincter, and as required, >20 mm LTL was identified. This further confirms that the residence period in the stomach is irrelevant to the fed or fasted condition. Based on desirability criteria, the formulation containing 143.83, 0.7982, and 14.6096 Eudragit L100, PEG, and sodium bicarbonate are selected as optimized formulations (O-IH-UF). The optimized formulation was further analyzed for various parameters such as tensile strength, mechanical strength, unfolding nature, degradability, and in vitro release studies. The pharmacokinetic study revealed greater AUC (area under the curve) and long half-life with the designed O-IH-UF formulation, confirming that the unfolding film type can be a favorable drug system for enhancing the bioavailability of low soluble drugs. The results showed that unfolding types of gastro retentive systems could potentiate the drugs with stability issues in an alkaline medium or those with absorption in acidic conditions. Full article
(This article belongs to the Special Issue Recent Advances in Stomach and Intesinal Drug Delivery Systems)
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17 pages, 3847 KiB  
Article
Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen
by Muhammad Usman Munir, Mahnoor Ikraam, Muhammad Nadeem, Syed Haroon Khalid, Sajid Asghar, Ikrima Khalid, Muhammad Irfan, Nayyer Islam, Nyla Ajaz and Ikram Ullah Khan
Pharmaceuticals 2022, 15(7), 856; https://doi.org/10.3390/ph15070856 - 12 Jul 2022
Cited by 6 | Viewed by 1575
Abstract
The aim of this study was to improve the solubility and prevent the ulcerogenic effect of flurbiprofen. Initially, binary and ternary solid dispersions (BSDs and TSDs) of flurbiprofen were prepared by using non-ordered mesoporous silica and gelucire. After preformulation testing (solubility, flow properties, [...] Read more.
The aim of this study was to improve the solubility and prevent the ulcerogenic effect of flurbiprofen. Initially, binary and ternary solid dispersions (BSDs and TSDs) of flurbiprofen were prepared by using non-ordered mesoporous silica and gelucire. After preformulation testing (solubility, flow properties, % yield, and entrapment efficiency), four formulations were selected for further detailed studies. Solid-state characterization of optimized formulations (S1, S6, S7, and S12) showed successful drug incorporation in the solid dispersion at the molecular state without any noticeable interactions. The in vitro solubility and release study showed an increase in solubility and 98–100% of drug release in 30–45 min. The in vivo gastro-protective effect of the optimized formulations containing flurbiprofen and silica (1:1) with 25% w/w gelucire (S6 and S12) showed a reduction in the gastric lesion index (GLI) after four days of treatment. Moreover, histological images of the stomach lining (S6 and S12) illustrated normal epithelial cells and a partially protected mucosal membrane. Thus, TSD exhibited a significant increase in solubility and the dissolution rate and reduced the gastric ulceration. Therefore, TSDs are dubbed as efficacious carriers to enhance the bioavailability of flurbiprofen while simultaneously reducing its side effects. Full article
(This article belongs to the Special Issue Recent Advances in Stomach and Intesinal Drug Delivery Systems)
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