Special Issue "Methodology, Design and Regulatory Considerations for the Bioequivalence of Oral Inhaled Products"

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (20 May 2021).

Special Issue Editors

Prof. Dr. Stefano Giovagnoli
E-Mail Website
Guest Editor
Department of Pharmaceutical Sciences, University of Perugia, 6100 Perugia, Italy
Interests: controlled release; solid state properties; organic and inorganic nano- microparticles; inhaled dry powders; drug physical modification; cell microencapsulation and engineering
Special Issues and Collections in MDPI journals
Dr. Bo Olsson
E-Mail Website
Guest Editor
Emmace Consulting AB, 223 81 Lund, Sweden
Interests: aerosol technology; drug delivery to the lung; lung deposition and disposition models; inhalation pharmacokinetics; inhalation biopharmaceutics
Dr. Zachary Warnken
E-Mail
Guest Editor
Division of Molecular Pharmaceutics and Drug Delivery, University of Texas at Austin, Austin, TX 78712, USA
Interests: repurposing drugs; poorly water soluble drugs; personalized medicine; pulmonary medicine; nasal drug delivery
Dr. Daniel Moraga-Espinoza
E-Mail
Guest Editor
1. Laboratorio de Tecnología Farmacéutica, Universidad de Valparaíso, 2340000 Valparaíso, Chile
2. Centro de Investigacion Farmacopea Chilena, Universidad de Valparaíso, 2340000 Valparaíso, Chile
Interests: inhalation; bioequivalence of OIDPs; powder flow characterization

Special Issue Information

Dear Colleagues,

While there are long standing methods for determining the bioequivalence of systemically delivered drugs such as injectables and oral solid dosage forms, assessing the bioequivalence of orally inhaled products requires special attention to various unique aspects, such as formulation properties and device design, to ensure equivalent therapeutic efficacy between products in patients. As many inhaled products are intended for a local therapeutic effect, pharmacokinetic studies, if even possible, fail to support equivalent performance between products. In order to provide generic products at reduced cost to patients, methods for determining bioequivalence without clinical testing are needed. Methods and updates to current regulatory guidelines for bioequivalence, for accurately assessing and predicting drug deposition placement in the lungs, and for delivery devices and drug solubility at the site of action, among others, that can be standardized and reproducible are needed in order to meet this need.

This Special Issue highlights the research that has taken place regarding the methodology, regulatory and device design space for inhaled products.

Prof. Dr. Stefano Giovagnoli
Dr. Bo Olsson
Dr. Zachary Warnken
Dr. Daniel Moraga-Espinoza
Guest Editors

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2200 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

  • inhaled drug delivery
  • bioequivalence
  • dry powder inhalers
  • regulatory agencies
  • analytical methodology
  • IVIVC

Published Papers (2 papers)

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Research

Article
A Safety and Tolerability Study of Thin Film Freeze-Dried Tacrolimus for Local Pulmonary Drug Delivery in Human Subjects
Pharmaceutics 2021, 13(5), 717; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13050717 - 13 May 2021
Viewed by 641
Abstract
Due to the low and erratic bioavailability of oral tacrolimus (TAC), the long-term survival rate following lung transplantation remained low compared to other solid organs. TAC was reformulated and developed as inhaled formulations by thin film freezing (TFF). Previous studies reported that inhaled [...] Read more.
Due to the low and erratic bioavailability of oral tacrolimus (TAC), the long-term survival rate following lung transplantation remained low compared to other solid organs. TAC was reformulated and developed as inhaled formulations by thin film freezing (TFF). Previous studies reported that inhaled TAC combined with 50% w/w lactose (LAC) was safe and effective for the treatment of lung transplant rejection in rodent models. In this study, we aimed to investigate the safety and tolerability of TFF TAC-LAC in human subjects. The formulation can be delivered to the lung as colloidal dispersions after reconstitution and as a dry powder. Healthy subjects inhaled TAC-LAC colloidal dispersions at 3 mg TAC/dose via a vibrating mesh nebulizer in the first stage of this study and TAC-LAC dry powder at 3 mg TAC/dose via a single dose dry powder inhaler in the second stage. Our results demonstrated that oral inhalation of TAC-LAC colloidal dispersions and dry powder exhibited low systemic absorption. Additionally, they were well-tolerated with no changes in CBC, liver, kidney, and lung functions. Only mild adverse side effects (e.g., cough, throat irritation, distaste) were observed. In summary, pulmonary delivery of TFF TAC-LAC would be a safe and promising therapy for lung transplant recipients. Full article
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Article
Assessment and Development of the Antifungal Agent Caspofungin for Aerosolized Pulmonary Delivery
Pharmaceutics 2021, 13(4), 504; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13040504 - 07 Apr 2021
Viewed by 369
Abstract
Invasive Pulmonary Aspergillosis (IPA) and Pneumocystis jiroveci Pneumonia (PCP) are serious fungal pulmonary diseases for immunocompromised patients. The brand name drug CANCIDAS® (Caspofungin acetate for injection) is FDA approved to treat IPA, but is only 40% effective. Efficacious drug levels at the [...] Read more.
Invasive Pulmonary Aspergillosis (IPA) and Pneumocystis jiroveci Pneumonia (PCP) are serious fungal pulmonary diseases for immunocompromised patients. The brand name drug CANCIDAS® (Caspofungin acetate for injection) is FDA approved to treat IPA, but is only 40% effective. Efficacious drug levels at the lung infection site are not achieved by systemic administration. Increasing the dose leads to toxicity. The objective, here, is to reformulate caspofungin for aerosolization to high drug concentration by lung targeted delivery and avoid systemic distribution. Described in this paper is a new, room temperature-stable formulation that meets these goals. The in vitro antifungal activity, solid state and reconstituted stability, and aerosol properties of the new formulation are presented. In addition, pharmacokinetic parameters and tissue distribution data are determined from nose-only inhalation studies in rats. Plasma and tissue samples were analyzed by High Performance Liquid Chromatography-tandem Mass Spectrometry (HPLC-MS-MS). Inhaled drug concentrations for caspofungin Active Pharmaceutical Ingredient (API), and the new formulation, were compared at the same dose. In the lungs, the parameters Cmax and Area Under Curve (AUC) showed a 70%, and 60%, respective increase in drug deposition for the new formulation without significant systemic distribution. Moreover, the calculated pharmacodynamic indices suggest an improvement in efficacy. These findings warrant further animal toxicology studies and human clinical trials, with inhaled caspofungin, for treating IPA. Full article
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