Abstract
Reformulation of anti-tuberculosis drugs into dry powder particles for inhalation is a novel strategy that aims to increase therapeutically relevant drug concentration at the primary site of infection and to limit associated toxicity by avoiding or minimizing first-pass metabolism. Development of such formulations ultimately requires quantified evidence of the deposition, absorption and clearance of inhaled active ingredient. In this context, we investigated the potential of radiolabelling particles with 153Sm for subsequent gamma imaging, and to demonstrate that the technique is not detrimental to particle integrity. The study showed that the known properties of spray dried leucine (a major constituent of an inhalable capreomycin formulation) for deep lung inhalation are not altered by incorporation of samarium-chloride (SmCl3) at 10% (w/w), or by neutron activation of particles that include stable 152SmCl3. SEM imaging indicated that the particle morphology was homogeneous and spherical after neutron activation. No discoloration of the samples or a change in dry powder particle size at 5 minutes occurred, provided the optimized formulations were activated for only 1 minute. Activation for 1 minute still provides enough 153Sm for imaging purposes.
Keywords: Gamma imaging, 153Sm radiolabel, spray dried powder particles, pulmonary drug delivery, tuberculosis, leucine, capreomycin, human immunodeficiency virus (HIV), multi-drug resistance, Neutron Activation, Chemical, Reagents, chromatography (HPLC), Samarium Formulation, homogeneous.
Drug Delivery Letters
Title:Characterization of Radiolabeled Dry Powder Leucine, a Constituent of Inhalable Capreomycin
Volume: 2 Issue: 3
Author(s): Lindie Venter, Judith Wagener, P. Bernard Fourie and Jan Rijn Zeevaart
Affiliation:
Keywords: Gamma imaging, 153Sm radiolabel, spray dried powder particles, pulmonary drug delivery, tuberculosis, leucine, capreomycin, human immunodeficiency virus (HIV), multi-drug resistance, Neutron Activation, Chemical, Reagents, chromatography (HPLC), Samarium Formulation, homogeneous.
Abstract: Reformulation of anti-tuberculosis drugs into dry powder particles for inhalation is a novel strategy that aims to increase therapeutically relevant drug concentration at the primary site of infection and to limit associated toxicity by avoiding or minimizing first-pass metabolism. Development of such formulations ultimately requires quantified evidence of the deposition, absorption and clearance of inhaled active ingredient. In this context, we investigated the potential of radiolabelling particles with 153Sm for subsequent gamma imaging, and to demonstrate that the technique is not detrimental to particle integrity. The study showed that the known properties of spray dried leucine (a major constituent of an inhalable capreomycin formulation) for deep lung inhalation are not altered by incorporation of samarium-chloride (SmCl3) at 10% (w/w), or by neutron activation of particles that include stable 152SmCl3. SEM imaging indicated that the particle morphology was homogeneous and spherical after neutron activation. No discoloration of the samples or a change in dry powder particle size at 5 minutes occurred, provided the optimized formulations were activated for only 1 minute. Activation for 1 minute still provides enough 153Sm for imaging purposes.
Export Options
About this article
Cite this article as:
Venter Lindie, Wagener Judith, Bernard Fourie P. and Rijn Zeevaart Jan, Characterization of Radiolabeled Dry Powder Leucine, a Constituent of Inhalable Capreomycin, Drug Delivery Letters 2012; 2 (3) . https://dx.doi.org/10.2174/2210304x11202030155
DOI https://dx.doi.org/10.2174/2210304x11202030155 |
Print ISSN 2210-3031 |
Publisher Name Bentham Science Publisher |
Online ISSN 2210-304X |
Call for Papers in Thematic Issues
Nanomaterial Assisted Targeted Therapies for Chronic Disorders- Preclinical to Clinical Outcomes
In recent years, the integration of nanomaterials into therapeutic strategies has emerged as a promising avenue in the pursuit of more effective treatments for chronic disorders. This dynamic field, explored in the context of "Nanomaterial Assisted Targeted Therapies for Chronic Disorders - Preclinical to Clinical Outcomes," seeks to bridge the ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Investigation of Potential Inhibitors of Chorismate-Utilizing Enzymes
Current Medicinal Chemistry Predictors of Response to TNF Antagonists
Current Pharmaceutical Design Initiation of the Immune Response by Extracellular Hsp72: Chaperokine Activity of Hsp72
Current Immunology Reviews (Discontinued) Despite an Extensive Sequence Analysis Identification of Functional Candidates Amongst Hypothetical Proteins of Neisseria gonorrhoeae
Letters in Drug Design & Discovery Anti-Inflammatory Activity of Polysaccharide Fraction of Curcuma longa Extract (NR-INF-02)
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Contribution of Host Genetics to TB Disease
Current Respiratory Medicine Reviews Regulation of Inflammation and Myocardial Fibrosis in Experimental Autoimmune Myocarditis
Inflammation & Allergy - Drug Targets (Discontinued) Inhibition of Efflux of Quinolines as New Therapeutic Strategy in Malaria
Current Topics in Medicinal Chemistry Medicinal and Beneficial Health Applications of Tinospora cordifolia (Guduchi): A Miraculous Herb Countering Various Diseases/Disorders and its Immunomodulatory Effects
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Meet Our Editorial Board Member
Current Medicinal Chemistry Tuberculosis and Diabetes Mellitus Co-morbidity
Current Respiratory Medicine Reviews Structure-Based Drug Discovery Accelerated by Many-Core Devices
Current Drug Targets Neurological Effects of SARS-CoV-2 and Neurotoxicity of Antiviral Drugs Against COVID-19
Mini-Reviews in Medicinal Chemistry From the Obscure and Mysterious Acute Phase Response to Toll-Like Receptors and the Cytokine Network
Current Immunology Reviews (Discontinued) Zebrafish Model in Drug Safety Assessment
Current Pharmaceutical Design Anti-Infective Peptides to Enhance the Host Innate Response: Design, Development and Delivery
Protein & Peptide Letters Fatty Acid Intakes and Coronary Heart Disease Mortality in Japan: NIPPON DATA90, 1990-2005
Current Nutrition & Food Science Docking-Related Survey on Natural-Product-Based New Monoamine Oxidase Inhibitors and Their Therapeutic Potential
Combinatorial Chemistry & High Throughput Screening Dietary Antioxidants: Immunity and Host Defense
Current Topics in Medicinal Chemistry Meet Our Editorial Board Member:
Current Medicinal Chemistry