Advances in Gastro-Retentive Drug Delivery Systems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (10 November 2023) | Viewed by 10894

Special Issue Editor


E-Mail Website
Guest Editor
Dpto. Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, 41012 Seville, Spain
Interests: drug delivery; responsive hydrogels; nanoparticles; functional materials; triggered release; living polymerization

Special Issue Information

Dear Colleagues,

A major focus of drug-related research has, for many years, been on the synthesis and discovery of potent, pharmacologically active agents to manage, treat, or cure diseases. Surprisingly, the main difficulties encountered in achieving effective treatment are not always linked to the availability of potent drugs, but to the finding of appropriate vehicles or carriers to get the drug to the required location. The oral route is favoured for drug administration, as it is non-invasive and easy to administer, so it has a low impact on patients. It represents approximately 90% of all therapeutics used. Most drugs are absorbed in the stomach or in the upper part of the small intestine; however, the absorption, and hence its bioavailability, is definitively influenced by environmental factors such as variations of pH, fluctuation in gastric emptying time, or enzymatic activity, which leads to a significant variability in the effectiveness of the treatment. Gastro-retentive systems have emerged as a new approach to overcome the inconveniences associated with oral drug administration, with the aim of improving the oral bioavailability of drugs that display either a narrow absorption window, reduced solubility in water at neutral or alkaline pHs, and/or that are sensitive to the harsh environments found in the GIT.

Prof. Dr. M. Violante De Paz
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. Pharmaceutics 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

  • oral bioavailability
  • extended release
  • gastric residence
  • gastric floating DDS
  • delayed gastric emptying devices
  • gastro-mucoadhesive dosage forms
  • low-density formulations
  • expanding formulations
  • porous matrices
  • microspheres

Published Papers (3 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

11 pages, 3565 KiB  
Article
Influence of In Situ Calcium Pectinate Coating on Metoprolol Tartrate Pellets for Controlled Release and Colon-Specific Drug Delivery
by Pimphaka Wanasawas, Ampol Mitrevej and Nuttanan Sinchaipanid
Pharmaceutics 2022, 14(5), 1061; https://doi.org/10.3390/pharmaceutics14051061 - 15 May 2022
Cited by 6 | Viewed by 2232
Abstract
In situ calcium pectinate-coated pellets were proposed by applying an alternate coating method to drug-layered pellets to achieve colon-specific drug delivery. Solution layering of metroprolol tartrate, a water-soluble model drug, on inert core pellets was achieved using a centrifugal granulator followed by successive [...] Read more.
In situ calcium pectinate-coated pellets were proposed by applying an alternate coating method to drug-layered pellets to achieve colon-specific drug delivery. Solution layering of metroprolol tartrate, a water-soluble model drug, on inert core pellets was achieved using a centrifugal granulator followed by successive alternate coating with pectin and calcium chloride layers using a fluidized bed bottom spray coater. The effect of the coating sequence on the drug release was studied in phosphate buffer pH 7.4 and 6.0. These test conditions were used to mimic the physiological environments in the distal small intestine and proximal colon, respectively. The results showed that the in situ calcium pectinate layer was successfully generated from the alternate coating of pectin and calcium layers after hydration to form gelation, which was able to control the drug release. The coating sequence played an important role in the drug release. The outermost pectin layer tended to retard the drug release whilst the outermost calcium layer accelerated the release regardless of the number of coating layers. These findings indicate that the release behavior followed the Higuchi model, with the drug release from the coated pellets described by a diffusion control mechanism. It is concluded that the success of the in situ calcium pectinate-coated pellets in controlling the drug release is due to the coating of the outermost layer with pectin and the maintenance of the optimum ratio of calcium to pectin upon hydration. Full article
(This article belongs to the Special Issue Advances in Gastro-Retentive Drug Delivery Systems)
Show Figures

Figure 1

15 pages, 34437 KiB  
Article
Preparation of Acyclovir-Containing Solid Foam by Ultrasonic Batch Technology
by Ádám Haimhoffer, Ferenc Fenyvesi, István Lekli, Mónika Béresová, István Bak, Máté Czagány, Gábor Vasvári, Ildikó Bácskay, Judit Tóth and István Budai
Pharmaceutics 2021, 13(10), 1571; https://doi.org/10.3390/pharmaceutics13101571 - 27 Sep 2021
Cited by 8 | Viewed by 2133
Abstract
In recent years, the application of solid foams has become widespread. Solid foams are not only used in the aerospace field but also in everyday life. Although foams are promising dosage forms in the pharmaceutical industry, their usage is not prevalent due to [...] Read more.
In recent years, the application of solid foams has become widespread. Solid foams are not only used in the aerospace field but also in everyday life. Although foams are promising dosage forms in the pharmaceutical industry, their usage is not prevalent due to decreased stability of the solid foam structure. These special dosage forms can result in increased bioavailability of drugs. Low-density floating formulations can also increase the gastric residence time of drugs; therefore, drug release will be sustained. Our aim was to produce a stable floating formula by foaming. Matrix components, PEG 4000 and stearic acid type 50, were selected with the criteria of low gastric irritation, a melting range below 70 °C, and well-known use in oral drug formulations. This matrix was melted at 54 °C in order to produce a dispersion of active substance and was foamed by different gases at atmospheric pressure using an ultrasonic homogenizer. The density of the molded solid foam was studied by the pycnometer method, and its structure was investigated by SEM and micro-CT. The prolonged drug release and mucoadhesive properties were proved in a pH 1.2 buffer. According to our experiments, a stable foam could be produced by rapid homogenization (less than 1 min) without any surfactant material. Full article
(This article belongs to the Special Issue Advances in Gastro-Retentive Drug Delivery Systems)
Show Figures

Figure 1

Review

Jump to: Research

44 pages, 521 KiB  
Review
In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations
by Nieves Iglesias, Elsa Galbis, Lucía Romero-Azogil, Elena Benito, Ricardo Lucas, M. Gracia García-Martín and M.-Violante de-Paz
Pharmaceutics 2020, 12(7), 636; https://doi.org/10.3390/pharmaceutics12070636 - 07 Jul 2020
Cited by 26 | Viewed by 4566
Abstract
The extensive use of oral dosage forms for the treatment of diseases may be linked to deficient pharmacokinetic properties. In some cases the drug is barely soluble; in others, the rapid transit of the formulation through the gastrointestinal tract (GIT) makes it difficult [...] Read more.
The extensive use of oral dosage forms for the treatment of diseases may be linked to deficient pharmacokinetic properties. In some cases the drug is barely soluble; in others, the rapid transit of the formulation through the gastrointestinal tract (GIT) makes it difficult to achieve therapeutic levels in the organism; moreover, some drugs must act locally due to a gastric pathology, but the time they remain in the stomach is short. The use of formulations capable of improving all these parameters, as well as increasing the resident time in the stomach, has been the target of numerous research works, with low-density systems being the most promising and widely explored, however, there is further scope to improve these systems. There are a vast variety of polymeric materials used in low-density gastroretentive systems and a number of methods to improve the bioavailability of the drugs. This works aims to expedite the development of breakthrough approaches by providing an in-depth understanding of the polymeric materials currently used, both natural and synthetic, their properties, advantages, and drawbacks. Full article
(This article belongs to the Special Issue Advances in Gastro-Retentive Drug Delivery Systems)
Back to TopTop