Submit to Special Issue Submit Abstract to Special Issue Review for Pharmaceutics Edit a Special Issue

Journal Menu

Journal Browser

Special Issue "Dosage Form Formulation Technologies for Improving Bioavailability"

Special Issue Editors
Special Issue Information
Keywords
Published Papers

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmacokinetics and Pharmacodynamics".

Deadline for manuscript submissions: 10 November 2023 | Viewed by 3896

Share This Special Issue

Special Issue Editors

Dr. Gábor Vasvári

E-Mail Website
Guest Editor

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, H-4032 Debrecen, Hungary
Interests: novel drug delivery; nano- and microformulations; stability investigation of drug delivery formulations; investigation of solubility, solubility enhancing technology
Special Issues, Collections and Topics in MDPI journals

Dr. Ádám Haimhoffer

E-Mail Website
Guest Editor

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, H-4032 Debrecen, Hungary
Interests: gastroretention; dosage form design; in vivo bioavability; cyclodextrin; cyclodextrin-polymer

Special Issue Information

Dear Colleagues,

The challenges of drug development could be extremely tough, high risk of failure or non-approval competes with the great benefits following the successful marketing authorization of a new molecular entities. Therefore, the more effective formulation in dosage form design is vital to overcome the possible disadvantageous physicochemical or biopharmaceutical properties of an approved API. Improving the oral, transdermal, or parenteral bioavailability relying on rational dosage form design or redesign, even after years of the market launch would increase therapeutic efficacies or patient compliance and lower the severity and the occurrence of unwanted side-effects. Innovative techniques, technological applications together with recently developed excipients would open the doors to the global markets for more patient-friendly products.

This Special Issue welcomes original research papers especially, but not limited to cooperative works between academia and pharmaceutical companies, where reformulations or original dosage form design were performed. Papers or reviews including the principles of Quality by Design to improve the bioavailability of drug belonging to BCS Classes of II or IV are warmly encouraged for submission. We are looking for manuscripts that optimize the innovative technology by the design of experiments as well. Non-pharma institutes or departments and their innovative research projects are also invited to contribute this Special Issue, if their novel and original results could be adapted to dosage form formulation or production.

Dr. Gábor Vasvári
Dr. Ádám Haimhoffer
Guest Editors

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 2600 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

innovative formulations
drug release optimization
pharmaceutical dosage form
quality by design
design of experiments
novel technologies
solubility enhancement
orphan drug

Published Papers (4 papers)

Download All Papers

Order results

Result details

Show export options Show export options

Select all

Export citation of selected articles as:

Research

Jump to: Review

Open AccessArticle

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

and

Pharmaceutics 2023, 15(3), 802; https://doi.org/10.3390/pharmaceutics15030802 - 01 Mar 2023

Viewed by 800

Abstract

Fibre-based oral drug delivery systems are an attractive approach to addressing low drug solubility, although clear strategies for incorporating such systems into viable dosage forms have not yet been demonstrated. The present study extends our previous work on drug-loaded sucrose microfibres produced by centrifugal melt spinning to examine systems with high drug loading and investigates their incorporation into realistic tablet formulations. Itraconazole, a model BCS Class II hydrophobic drug, was incorporated into sucrose microfibres at 10, 20, 30, and 50% w/w. Microfibres were exposed to high relative humidity conditions (25 °C/75% RH) for 30 days to deliberately induce sucrose recrystallisation and collapse of the fibrous structure into powdery particles. The collapsed particles were successfully processed into pharmaceutically acceptable tablets using a dry mixing and direct compression approach. The dissolution advantage of the fresh microfibres was maintained and even enhanced after humidity treatment for drug loadings up to 30% w/w and, importantly, retained after compression into tablets. Variations in excipient content and compression force allowed manipulation of the disintegration rate and drug content of the tablets. This then permitted control of the rate of supersaturation generation, allowing the optimisation of the formulation in terms of its dissolution profile. In conclusion, the microfibre-tablet approach has been shown to be a viable method for formulating poorly soluble BCS Class II drugs with improved dissolution performance. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

► Show Figures

Figure 1

Open AccessArticle

The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics

Laura Di Renzo

Antonella Smeriglio

Mariarosaria Ingegneri

Paola Gualtieri

and

Domenico Trombetta

Pharmaceutics 2023, 15(3), 743; https://doi.org/10.3390/pharmaceutics15030743 - 23 Feb 2023

Viewed by 518

Abstract

Current evidence supports the use of extra virgin olive oil (EVOO) and its minor components such as hydroxytyrosol or 3,4-dihydroxyphenyl ethanol (DOPET), to improve cardiovascular and metabolic health. Nevertheless, more intervention studies in humans are needed because some gaps remain in its bioavailability and metabolism. The aim of this study was to investigate the DOPET pharmacokinetics on 20 healthy volunteers by administering a hard enteric-coated capsule containing 7.5 mg of bioactive compound conveyed in EVOO. The treatment was preceded by a washout period with a polyphenol and an alcohol-free diet. Blood and urine samples were collected at baseline and different time points, and free DOPET and metabolites, as well as sulfo- and glucuro-conjugates, were quantified by LC-DAD-ESI-MS/MS analysis. The plasma concentration versus time profiles of free DOPET was analyzed by a non-compartmental approach, and several pharmacokinetic parameters (C_max, T_max, T_1/2, AUC_{0–440 min}, AUC_0–∞, AUC_t–∞, AUC_{extrap_pred}, C_last and K_el) were calculated. Results showed that DOPET C_max (5.5 ng/mL) was reached after 123 min (T_max), with a T_1/2 of 150.53 min. Comparing the data obtained with the literature, the bioavailability of this bioactive compound is about 2.5 times higher, confirming the hypothesis that the pharmaceutical formulation plays a pivotal role in the bioavailability and pharmacokinetics of hydroxytyrosol. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

► Show Figures

Graphical abstract

Open AccessArticle

Thermoresponsive Azithromycin-Loaded Niosome Gel Based on Poloxamer 407 and Hyaluronic Interactions for Periodontitis Treatment

Kunchorn Kerdmanee

Thawatchai Phaechamud

and

Sucharat Limsitthichaikoon

Pharmaceutics 2022, 14(10), 2032; https://doi.org/10.3390/pharmaceutics14102032 - 24 Sep 2022

Cited by 2 | Viewed by 1249

Abstract

Azithromycin (AZM) is a potential antimicrobial drug for periodontitis treatment. However, a potential sustained-release system is needed for intra-periodontal pocket delivery. This study focused on the development and evaluation of a thermoresponsive azithromycin-loaded niosome gel (AZG) to search for a desirable formulation for periodontitis treatment. AZG was further developed from an AZM-loaded niosomal formulation by exploiting the advantages of poloxamer 407 (P407) and hyaluronic acid (HA) interactions. The results showed that the addition of HA decreased the gelation temperature and gelation time of AZG. HA was found to increase the viscosity as well as mucoadhesive and tooth-root surface adhesive properties. The AZG solution state was injectable and exhibited pseudoplastic shear-thinning behavior. P407–HA interactions in AZG could contribute to gel strength. AZG showed 72 h of continuous drug release following the Korsmeyer–Peppas model and potentially enhanced drug permeation. The formulations apparently presented more efficient antibacterial activity against major periodontal pathogens than the standard AZM solution. AZM intra-periodontal pocket formulation and the remarkable properties of niosomes exhibited potential characteristics, including ease of administration, bioadhesion to the anatomical structure of the periodontal pocket, and sustained drug release with competent antimicrobial activity, which could be beneficial for periodontitis treatment. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

► Show Figures

Figure 1

Review

Jump to: Research

Open AccessReview

Recent Options and Techniques to Assess Improved Bioavailability: In Vitro and Ex Vivo Methods

and

Pharmaceutics 2023, 15(4), 1146; https://doi.org/10.3390/pharmaceutics15041146 - 04 Apr 2023

Viewed by 816

Abstract

Bioavailability assessment in the development phase of a drug product is vital to reveal the disadvantageous properties of the substance and the possible technological interventions. However, in vivo pharmacokinetic studies provide strong evidence for drug approval applications. Human and animal studies must be designed on the basis of preliminary biorelevant experiments in vitro and ex vivo. In this article, the authors have reviewed the recent methods and techniques from the last decade that are in use for assessing the bioavailability of drug molecules and the effects of technological modifications and drug delivery systems. Four main administration routes were selected: oral, transdermal, ocular, and nasal or inhalation. Three levels of methodologies were screened for each category: in vitro techniques with artificial membranes; cell culture, including monocultures and co-cultures; and finally, experiments where tissue or organ samples were used. Reproducibility, predictability, and level of acceptance by the regulatory organizations are summarized for the readers. Full article

(This article belongs to the Special Issue Dosage Form Formulation Technologies for Improving Bioavailability)

► Show Figures

Journal Menu

Journal Browser

Special Issue "Dosage Form Formulation Technologies for Improving Bioavailability"

Share This Special Issue

Special Issue Editors

Special Issue Information

Keywords

Published Papers (4 papers)

Research

Review

Further Information

Guidelines

MDPI Initiatives

Follow MDPI