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Pharmaceuticals
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Recent Advance in Oral Drug Delivery Development
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Recent Advance in Oral Drug Delivery Development

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

Deadline for manuscript submissions: closed (22 April 2022) | Viewed by 21230

Special Issue Editor

Dr. Joël Schlatter

E-Mail Website
Guest Editor
Assistance Publique-Hôpitaux de Paris, AP-HP, Hôpital Universitaire Necker-Enfants Malades, Service de Pharmacie, Université de Paris, 75015 Paris, France
Interests: stability; oral formulation; pediatric; drugs; elderly

Special Issue Information

Dear Colleagues, 

Oral drug delivery is the most preferred method as it is convenient, non-invasive and easy to incorporate into lifestyle of the patient. Nevertheless, several factors including poor solubility, low dissolution rate, stability and bioavailability of many dugs remain a constant challenge in achieving desired therapeutic targets. The delivery of drugs must overcome various obstacles, including the acidic gastric environment, the presence of intestinal efflux and influx transporters. In recent years, the emergence of new technologies for oral delivery systems offers opportunities for patients to easily receive medications that were previously administered by injection, in particular. Because of the benefits in terms of convenience and cost for patients and the growing demand for home care stimulated by COVID-19, explorations in developing oral delivery systems are expanding. 

Hence, a new age of science and technology has emerged with the marketing of fast-dissolving drugs, self-emulsifying formulations that enhance the oral bioavailability of hydrophobic active compounds, osmotic devices for the controlled drug delivery independent upon gastrointestinal conditions, and vesicular systems that sustained drug delivery to a specific site. 

The journal Pharmaceuticals invites both reviews and original articles highlighting recent progress in the development of oral drug delivery. Topics include: new drug formulations, selective optimization device for oral drug bioavailability, investigation of innovative ways of getting oral formulations, beyond pharmaceuticals applications, oral drug delivery research. The collection of manuscripts will be published as a Special Issue of the journal.

Dr. Joël Schlatter
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

  • drug
  • delivery
  • new technology
  • oral adminstration
  • devices

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Published Papers (6 papers)

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Editorial

Jump to: Research, Review

3 pages, 195 KiB  
Editorial
Special Issue “Recent Advances in Oral Drug Delivery Development”
by Joël Schlatter
Pharmaceuticals 2023, 16(9), 1289; https://doi.org/10.3390/ph16091289 - 13 Sep 2023
Viewed by 1318
Abstract
This Special Issue, entitled “Recent Advances in Oral Drug Delivery Development”, aims to demonstrate new advances and future trends in the field of oral drug delivery [...] Full article
(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)

Research

Jump to: Editorial, Review

21 pages, 5186 KiB  
Article
Exorbitant Drug Loading of Metformin and Sitagliptin in Mucoadhesive Buccal Tablet: In Vitro and In Vivo Characterization in Healthy Volunteers
by Rouheena Shakir, Sana Hanif, Ahmad Salawi, Rabia Arshad, Rai Muhammad Sarfraz, Muhammad Irfan, Syed Atif Raza, Kashif Barkat, Fahad Y. Sabei, Yosif Almoshari, Meshal Alshamrani and Muhammad Ali Syed
Pharmaceuticals 2022, 15(6), 686; https://doi.org/10.3390/ph15060686 - 30 May 2022
Cited by 7 | Viewed by 4246 | Correction
Abstract
The aim of the proposed study is to develop a mucoadhesive buccal delivery system for the sustained delivery of metformin (MET) and sitagliptin (SIT) against diabetes mellitus (DM) with improved bioavailability. Polymeric blend of Carbopol® 940 (CP), agarose (AG) or polyvinylpyrrolidone K30 [...] Read more.
The aim of the proposed study is to develop a mucoadhesive buccal delivery system for the sustained delivery of metformin (MET) and sitagliptin (SIT) against diabetes mellitus (DM) with improved bioavailability. Polymeric blend of Carbopol® 940 (CP), agarose (AG) or polyvinylpyrrolidone K30 (PVP) as mucoadhesive agents in formulations (R1–R15) were compressed via the direct compression technique. Tablets were characterized for solid state studies, physicochemical and in vivo mucoadhesion studies in healthy volunteers. Outcomes did not reveal any unusual peak or interaction between the drugs and polymers in the physical mixture through Fourier Transform Infrared Spectroscopy (FTIR) and DSC analysis. The mucoadhesive blend of CP and PVP was superior compared to other blends. The formulation R4 revealed exorbitant loading of drugs with complete drug release for 6 h with ex vivo mucoadhesive strength and time of 26.99 g and 8.1 h, respectively. It was further scrutinized to evaluate it as an optimized formulation where it was found to be stable for up to 6 months. The formulation R4 depicted Korsmeyer–Peppas model and first-order mode of release correspondingly for SIT and MET. Moreover, it showed hemocompatibility, biocompatibility and stability with non-significant changes in the dissolution profile. Overall, the CP blend with PVP was found appropriate to yield the desired release coupled with the optimized mucoadhesive properties of the buccal tablets, ensuring sufficient pharmaceutical stability. Full article
(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)
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15 pages, 1854 KiB  
Article
Development of a Hospital Compounded, Taste-Masked, Temozolomide Oral Suspension and 5-Year Real-Life Experience in Treating Paediatric Patients
by Maxime Annereau, Mélanie Hinterlang, Hugues Bienayme, Gilles Vassal, Antoine Pinon, Mathieu Schmitt, Lucas Denis, Caroline Lemarchand, Laurent Martin, François Lemare, Samuel Abbou, Jérémy Bastid and Lionel Tortolano
Pharmaceuticals 2022, 15(5), 555; https://doi.org/10.3390/ph15050555 - 29 Apr 2022
Cited by 4 | Viewed by 3635
Abstract
The development of oral pediatric forms by pharmaceutical companies is still insufficient. In fact, many drugs used in paediatric oncology, such as temozolomide, are not labeled and adapted for paediatric use. Temozolomide (TMZ) is an alkylating agent used as the standard of care [...] Read more.
The development of oral pediatric forms by pharmaceutical companies is still insufficient. In fact, many drugs used in paediatric oncology, such as temozolomide, are not labeled and adapted for paediatric use. Temozolomide (TMZ) is an alkylating agent used as the standard of care for many adult and pediatric brain tumours, such as neuroblastoma, glioblastoma and medulloblastoma. The present study was carried out to propose a suitable and palatable formulation of the oral liquid preparation of TMZ. The suspension is composed of TMZ suspended in SyrSpend SF pH 4, as well as TMZ crystallization stabilizing agents and sweetening agents. To reach this formulation, several taste-masking agents were evaluated. Here, we describe the method of preparation of the formation as well as the monocentric population treated with the formulation over a 5–year period. A 20 mg/mL TMZ suspension was developed. TMZ suspension is stable for 6 weeks, stored between 2 and 8 degrees, protected from light, and compatible with nasogastric tubes. Thirty-eight patients participated in the palatability study and choose cola flavour, and 104 patients were treated in Gustave Roussy with the developed suspension; no unexpected event was reported. To conclude, we propose here a new TMZ liquid formulation which is stable for at least 6 weeks and well-tolerated with extensive feedback. Full article
(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)
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15 pages, 1936 KiB  
Article
Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations
by Philippe-Henri Secretan, Olivier Thirion, Hassane Sadou Yayé, Thibaud Damy, Alain Astier, Muriel Paul and Bernard Do
Pharmaceuticals 2021, 14(12), 1242; https://doi.org/10.3390/ph14121242 - 30 Nov 2021
Cited by 10 | Viewed by 2668
Abstract
Because of its antioxidant, antimutagenic, and anti-infectious properties, epigallocatechin gallate (EGCG) is the most interesting compound among the green tea catechins polyphenols. However, its health effects are inconclusive due to its very low bioavailability, largely due to a particular instability that does not [...] Read more.
Because of its antioxidant, antimutagenic, and anti-infectious properties, epigallocatechin gallate (EGCG) is the most interesting compound among the green tea catechins polyphenols. However, its health effects are inconclusive due to its very low bioavailability, largely due to a particular instability that does not allow EGCG to reach the potency required for clinical developments. Over the last decade, many efforts have been made to improve the stability and bioavailability of EGCG using complex delivery systems such as nanotechnology, but these efforts have not been successful and easy to translate to industrial use. To meet the needs of a large-scale clinical trial requiring EGCG in a concentrated solution to anticipate swallowing impairments, we developed an EGCG-based aqueous solution in the simplest way while trying to circumvent EGCG instability. The solution was thoroughly characterized to sort out the unexpected stability outcome by combining experimental (HPLC-UV-mass spectrometry and infrared spectroscopy) and computational (density functional theory) studies. Against all odds, the EGCG–sucrose complex under certain conditions may have prevented EGCG from degradation in aqueous media. Indeed, in agreement with the ICH guidelines, the formulated solution was shown to be stable up to at least 24 months under 2–8 °C and at ambient temperature. Furthermore, considerable improvement in bioavailability in rats, against EGCG powder formulated in hard-gel capsules, was shown after gavage. Thus, the proposed formulation may provide an easily implementable platform to administer EGCG in the context of clinical development. Full article
(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)
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10 pages, 4160 KiB  
Article
Subchronic Toxicity Study of Oral Anthrafuran on Rabbits
by Michael I. Treshchalin, Helen M. Treshalina, Vasilisa A. Golibrodo, Andrey E. Shchekotikhin and Eleonora R. Pereverzeva
Pharmaceuticals 2021, 14(9), 900; https://doi.org/10.3390/ph14090900 - 4 Sep 2021
Cited by 2 | Viewed by 2177
Abstract
A new antitumor multi-target drug anthrafuran, with cellular targets such as topoisomerase I/II and some protein kinases, was obtained in Gause Institute of New Antibiotics and was demonstrated to have a reliable specific effect on different murine and human tumor models by oral [...] Read more.
A new antitumor multi-target drug anthrafuran, with cellular targets such as topoisomerase I/II and some protein kinases, was obtained in Gause Institute of New Antibiotics and was demonstrated to have a reliable specific effect on different murine and human tumor models by oral administration. In this study, we focused on the evaluation of subchronic toxicity of oral anthrafuran drug formulation (AF) on Chinchilla rabbits. The absence of any changes in the condition or behavior of animals was shown for oral anthrafuran. Changes with reversible and dose-dependent hepato- and nephrotoxicity at low doses, as well as hemato- and gastrointestinal toxicity at high doses, were confirmed pathomorphologically. The identified toxic properties are extremely valuable, since oral anthrafuran does not have the limiting cardio- and myelotoxicity. Anthrafuran with 2 mg/kg/day or 6 mg/kg/day doses was administrated orally over 15 days. Investigations include assessment of the body weight, hematological and serum biochemical parameters and urinalysis, electrocardiography and pathomorphological evaluation of the internal organs. Quantitative data were processed statistically with Student’s t-Test, p < 0.05. Revealed during the subchronic study were the favorable toxicological properties of oral anthrafuran as opposed to clinical anthracyclines, oral idarubicin, or parenteral doxorubicin, which allows it to be considered promising for further research. Full article
(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)
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Review

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28 pages, 1698 KiB  
Review
Solidification of Self-Emulsifying Drug Delivery Systems as a Novel Approach to the Management of Uncomplicated Malaria
by Eun Bin Seo, Lissinda H. du Plessis and Joe M. Viljoen
Pharmaceuticals 2022, 15(2), 120; https://doi.org/10.3390/ph15020120 - 20 Jan 2022
Cited by 9 | Viewed by 5689
Abstract
Malaria affects millions of people annually, especially in third-world countries. The mainstay of treatment is oral anti-malarial drugs and vaccination. An increase in resistant strains of malaria parasites to most of the current anti-malarial drugs adds to the global burden. Moreover, existing and [...] Read more.
Malaria affects millions of people annually, especially in third-world countries. The mainstay of treatment is oral anti-malarial drugs and vaccination. An increase in resistant strains of malaria parasites to most of the current anti-malarial drugs adds to the global burden. Moreover, existing and new anti-malarial drugs are hampered by significantly poor aqueous solubility and low permeability, resulting in low oral bioavailability and patient noncompliance. Lipid formulations are commonly used to increase solubility and efficacy and decrease toxicity. The present review discusses the findings from studies focusing on specialised oral lipophilic drug delivery systems, including self-emulsifying drug delivery systems (SEDDSs). SEDDSs facilitate the spontaneous formation of liquid emulsions that effectively solubilise the incorporated drugs into the gastrointestinal tract and thereby improve the absorption of poorly-soluble anti-malaria drugs. However, traditional SEDDSs are normally in liquid dosage forms, which are delivered orally to the site of absorption, and are hampered by poor stability. This paper discusses novel solidification techniques that can easily and economically be up-scaled due to already existing industrial equipment that could be utilised. This method could, furthermore, improve product stability and patient compliance. The possible impact that solid oral SEDDSs can play in the fight against malaria is highlighted. Full article
(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)
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