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Drug delivery & formulation glossary & taxonomy
Evolving Terminology for Emerging Technologies
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Mary Chitty MSLS
Last revised January 07, 2020

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active transport of drugs: Carriage of a solute across a biological membrane, which requires a suitable carrier and the expenditure of energy. IUPAC Pharmaceutics

adjuvant: 1. Additive with no intended pharmacological action, used in the formulation of dosage forms.  2. In pharmacology, a substance added to a drug to speed or increase the action of the main component. 3. In immunology, a substance (such as aluminum hydroxide) or an organism (such as killed mycobacterium) that increases the response to an antigen.  IUPAC Pharmaceutics

adjuvants vaccines:  An adjuvant is a substance that is formulated as part of a vaccine to enhance its ability to induce protection against infection. The word “adjuvant” comes from the Latin adjuvare and means “to help.” Adjuvants help activate the immune system, allowing the antigens — pathogen components that elicit an immune response — in vaccines to induce long-term protective immunity. NIH, NIAID

antibody drug conjugates: Biologics

bioavailability: 1. Ratio of the systemic exposure from extravascular (ev) exposure to that following intravenous (iv) exposure as described by the equation: where F is the bioavailability, A and B are areas under the (plasma) concentration-time curve following ev and iv administration, respectively, and Dev and Div are the administered ev and iv doses. 2. Relative amount of the administered dose of a drug that reaches systemic circulation from a certain dosage form in comparison to the amount that reaches the systemic circulation by iv administration. See also relative bioavailability. [7,12] IUPAC Pharmaceutics

As indicated in Chapter 21 CFR (Codes of Federal Regulations) Part 320.1, bioavailability of a drug is defined as the extent and rate to which the active drug ingredient or active moiety from the drug product is absorbed and becomes available at the site of drug action. The extent and rate of drug absorption are usually measured by the area under the blood or plasma concentration-time curve (AUC) and the maximum concentration (Cmax), respectively. For drug products that are not intended to be absorbed into bloodstream, bioavailability may be assessed by measurements intended to reflect the rate and extent to which the active ingredient or active moiety is absorbed and becomes available at the site of action. A comparative bioavailability study refers to the comparison of bioavailabilities of different formulations of the same drug or different drug products. As indicated in Chow and Liu (2008), the definition of bioavailability has evolved over time with different meanings by different individuals and organizations [1]. For example, differences are evident in the definitions by Academy of Pharmaceutical Sciences in 1972, the Office of Technology Assessment (OTA) of the Congress of the United States in 1974, and the 1984 Drug Price Competition and Patent Restoration Act which is amendments to the Food, Drug, and Cosmetic Act. For more discussion regarding the definition of bioavailability, see [2-4].  Bioavailability and Bioequivalence in Drug Development. Wiley Interdiscip Rev Comput Stat. 2014;6(4):304-312.

bioequivalence:  a term in pharmacokinetics used to assess the expected in vivo biological equivalence of two proprietary preparations of a drug. If two products are said to be bioequivalent it means that they would be expected to be, for all intents and purposes, the same. ... Birkett (2003) defined bioequivalence by stating that, "two pharmaceutical products are bioequivalent if they are pharmaceutically equivalent and their bioavailabilities (rate and extent of availability) after administration in the same molar dose are similar to such a degree that their effects, with respect to both efficacy and safety, can be expected to be essentially the same. Pharmaceutical equivalence implies the same amount of the same active substance(s), in the same dosage form, for the same route of administration and meeting the same or comparable standards."[1] For The World Health Organization (WHO) "two pharmaceutical products are bioequivalent if they are pharmaceutically equivalent or pharmaceutical alternatives, and their bioavailabilities, in terms of rate (Cmax and tmax) and extent of absorption (area under the curve), after administration of the same molar dose under the same conditions, are similar to such a degree that their effects can be expected to be essentially the same" [2]. The United States Food and Drug Administration (FDA) has defined bioequivalence as, "the absence of a significant difference in the rate and extent to which the active ingredient or active moiety in pharmaceutical equivalents or pharmaceutical alternatives becomes available at the site of drug action when administered at the same molar dose under similar conditions in an appropriately designed study."[3] Wikipedia accessed 2018 Nov 6

When two formulations of the same drug or two drug products are claimed bioequivalent, it is assumed that they will provide the same therapeutic effect or that they are therapeutically equivalent. In this case, most people interpret that they can be used interchangeably. Two drug products are considered pharmaceutical equivalents if they contain identical amounts of the same active ingredient. Two drugs are identified as pharmaceutical alternatives to each other if both contain an identical therapeutic moiety, but not necessarily in the same amount or dosage form or as the same salt or ester. Two drug products are said to be bioequivalent if they are pharmaceutical equivalents (i.e., similar dosage forms made, perhaps, by different manufacturers) or pharmaceutical alternatives (i.e., different dosage forms) and if their rates and extents of absorption do not show a significant difference to which the active ingredient or active moiety in pharmaceutical equivalents or pharmaceutical alternatives become available at the site of action when administered at the same molar dose under similar conditions in an appropriately designed study.  Bioavailability and Bioequivalence in Drug Development. Wiley Interdiscip Rev Comput Stat. 2014;6(4):304-312.

biological availability: The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. MeSH 1979 

Also known as bioavailability.

biopharmaceutics:  The study of the chemical and physical properties of drugs, and the relationship between these, dosage, and activity  Wiktionary

biologics formulation: Optimizing Biologics Formulation Development January 20-21, 2020 • San Diego, CA formulation challenges of emerging modalities, new strategies for predictive analysis at this stage, exciting new analytical methodologies and accelerating and the best practices being employed to overcome formulation challenges.
Optimizing Biologics Formulation Development

Blood-Brain Barrier June 19-20, 2018 • Boston, MA | Antibodies and new drugs that are promising for treating brain diseases and disorders are often limited by poor brain exposure. Research is focused on examining new ways to deliver drugs to the brain, including gene therapy and treatment of the BBB’s microvessels. Cambridge Healthtech Institute’s Fourth Annual Blood-Brain Barrier conference will focus on the key areas of understanding BBB transport and dysfunction in disease through a series of case studies and cutting-edge research presentations. This conference will address questions surrounding BBB permeability, blood flow, translational research, and biomarkers of BBB breakdown. Special attention will be paid to in vivo models and tools that are available to investigate BBB transport and pathology in disease. The conference will also provide updates from the industry on antibody delivery and transport across the BBB.

Advancing CNS Biotherapeutics and Crossing the Blood-Brain Barrier  January 14-15, 2019 • San Diego, CA  the hottest topics and biggest opportunities in discovering and developing highly efficacious therapeutic agents against CNS disorders and innovative strategies for delivering therapies across the blood-brain barrier (BBB), new research on topics such as the biologics for CNS targets and biomarkers, brain cancer, neurodegeneration, neuroinflammation, neuroimmunology, alteration of CNS/BBB barriers due to injury or disease, preclinical models, neuroimaging, tools for prediction of brain penetration, and updates from the industry on topics such as antibody delivery and vector-mediated transport across BBB.

Blood Brain Barrier and CNS Drug Discovery Strategies and Tools to Address Hurdles in CNS Drug Discovery APRIL 12, 2019 San DIEGo CA  The blood-brain barrier (BBB) plays a critical role in brain homeostasis – a function it does so well that scientists and drug developers continue to grapple with the challenges of delivering drugs into the brain to treat devastating and life-threatening diseases such as brain cancer and neurodegenerative disorders. As we understand more about the state of the BBB in a healthy and a disease-challenged brain, novel strategies, methods and tools are developed to design and study brain-penetrant molecules.

carrier-mediated drug transport: Transfer of a drug across a membrane by a transporter (often a protein) constituent of the cytosol membrane. Also known as active transport as opposed to passive diffusion/absorption. IUPAC Pharmaceutics

cosolvent: Vehicle (often ethanol) used in combination to increase the solubility of drugs. Frequently, the solubility of a drug in a mixed solvent system is greater than can be predicted from its solubility in each solvent component separately. IUPAC Pharmaceutics

crystalline: Term that describes a solid of regular shape and the presence of three-dimensional order on the level of atomic dimensions, for a given molecule. Note 1: Crystallinity may be detected by diffraction techniques, heat-of-fusion measurements, etc. Note 2: Crystalline forms are often preferred, over amorphous forms, in pharmaceutical dosage forms, due to uniformity, reproducibility, and sometimes lack of hygroscopicity IUPAC Pharmaceutics

dosage form: Formulated preparation of molecules/drugs that are rarely if ever suitable for administration to patients without additives. See also tablet, syrup, solution, cream, suppositories, etc. IUPAC Pharmaceutics

drug delivery: refers to approaches, formulations, technologies, and systems for transporting a pharmaceuticalcompound in the body as needed to safely achieve its desired therapeutic effect.[1] It may involve scientific site-targeting within the body, or it might involve facilitating systemic pharmacokinetics; in any case, it is typically concerned with both quantity and duration of drug presence. Drug delivery is often approached via a drug's chemical formulation, but it may also involve medical devices or drug-device combination products. Drug delivery is a concept heavily integrated with dosage form and route of administration, the latter sometimes even being considered part of the definition.[2]   Wikipedia accessed 2018 Nov 5

drug delivery system: Sophisticated dosage form, which, by its construction, is able to modify/control the availability of the drug substance to the body by temporal or spatial considerations. controlled release, extended release, delayed release, delayed action, dosage form, depot, embedding, gradual release, fast release or immediate release, i.e., conventional dosage form, implants, liposome, long-acting, modified release, prolonged action, pulsatile release slow release. : IUPAC Pharmaceutics

drug-eluting stent: Refers to a stent with an active drug that is intended to produce a therapeutic effect (e.g., reduction of restenosis) [13]. IUPAC Pharmaceutics

drug targeting:  A strategy aiming at the delivery of a compound to a particular tissue of the body. IUPAC Medicinal Chemistry  

The Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs. Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.   Aims and Scope, Journal of Drug Targeting, Taylor & Francis

formulation: Summary of operations carried out to convert a pharmacologically active compound into a dosage form suitable for administration. See also drug delivery systems, excipient, solubilizing agents. IUPAC  Pharmaceutics

gene therapy: Use of products containing genetic material (e.g., pDNA, antisense DNA, siRNA) to treat a disease or condition, or to modify or manipulate the expression of genetic material or to alter the biological properties of living cells. IUPAC Pharmaceutics  more in Biologics

Insulin Infusion Systems: Portable or implantable devices for infusion of insulin. Includes open-loop systems which may be patient-operated or controlled by a pre-set program and are designed for constant delivery of small quantities of insulin, increased during food ingestion, and closed-loop systems which deliver quantities of insulin automatically based on an electronic glucose sensor. MeSH Year introduced: 1982

liposome: Artificial spherical lipid bilayer droplet formed mainly from phospholipids having a core of waterphase, small enough to form a relatively stable dispersion in aqueous media and with potential use in drug delivery. [3] IUPAC Pharmaceutics

micelle(s): Aggregates of colloidal dimensions (i.e., association of colloids) formed reversibly from amphiphile molecules. [3]  Note 1: A micelle is thus a structural unit of the dispersed phase (surfactant) in an emulsion, suspension, or a gel; a unit whose repetition in three dimensions constitutes the micellar structure of the gel; it does not denote the individual particles in free suspension or solution, or the unit structure of a crystal. Note 2: Arrangements of groups of molecules of hydrophobic liquids in aqueous environment, formed by surface-active agents. [7]  See also critical micelle concentration. IUPAC Pharmaceutics

microfiltration: Pressure-driven, membrane-based separation process in which particles and dissolved macromolecules larger than 0.1 μm are rejected. Note: Can be used for sterilization with 0.22-μm size filters. [18] IUPAC Pharmaceutics

Solid spherical particles of micron-size range, used as matrix dosage forms. IUPAC  Pharmaceutics

molecular pharmaceutics: Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems.,,, Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. American Chemical Society, About Molecular Pharmaceutics   Broader term: pharmaceutics

nanodelivery: Nanomaterials for targeted delivery are uniquely capable of localizing delivery of therapeutics and diagnostics to diseased tissues. The ability to achieve high, local concentrations of drugs or image contrast agents at a target site provides the opportunity for improved system performance and patient outcomes along with reduced systemic dosing. Targeted Nanodelivery of Drugs and Diagnostics, Margaret A. Phillips, Martin L. Gran, and Nicholas A. Peppas, Nano Today 2010 April 1 5(2)”143-150

nanoencapsulation: Formation of nanoparticles encapsulating a drug. IUPAC Pharmaceutics

nanoparticles: Microscopic particle whose size is measured in nanometers, often restricted to so-called nanosized particles  (NSPs; <100 nm in aerodynamic diameter), also called ultrafine particles. Note 1: Drug may be embedded in (as in a matrix) or adsorbed or encapsulated. Note 2: Particles containing drug of sizes less than 0.5 μm are often named as nanoparticles. [3] IUPAC  Pharmaceutics  Wikipedia   See also Miniaturization & Nanoscience

nucleotide delivery: A multitude of factors affect the biological activity of nucleoside analogs (Nu), which must be phosphorylated intracellularly by cellular or viral enzymes before exerting their effects. It follows that the intracellular metabolism of nucleosides is a key event for the appearance of their biological response. Comments on nucleotide delivery forms Author links open overlay panel ChristianPérigaudJean-LucGirardetGillesGosselinJean-LouisImbach  Advances in Antiviral Drug Design Volume 2, 1996, Pages 147-172

Oligonucleotide Discovery and Delivery Optimizing Design, Delivery and Performance MARCH 26-27, 2019 CambridGE MA   Program |  latest strategies at the forefront of discovery, chemistry and delivery with in-depth sessions on new chemistries, novel delivery mechanisms and the most important preclinical and clinical advances. Leading oligonucleotide scientists deliver detailed case studies on antisense, RNA, aptamer and oligonucleotide conjugates 

parenteral: administration of drugs, parenteral route Method of introducing substances into an organism, avoiding the gastrointestinal tract [1]. Note 1: Parenteral routes may be employed whenever enteral routes are contraindicated or inadequate. Note 2: Parenteral administration includes some conventional (intravenous, intramuscular, subcutaneous) and some special (intradermal, intraventricular, etc.) routes. Note 3: Parenteral products can be solutions, suspensions, and emulsions. They are presented as sterile products. It is commonly used to imply administration by injection or infusion. See also administration. IUPAC Pharmaceutics

pharmaceutics: Science of preparation of drugs, dosage forms, and drug delivery systems taking into account the pharmacokinetics and pharmacodynamics of the drug as well as its physical and chemical properties. IUPAC Pharmaceutics Narrower term: molecular pharmaceutics  See also Pharmacogenomics glossary & taxonomy

pharmacodelivery: Site-directed pharmacodelivery is a desirable but elusive goal. Endothelium and epithelium create formidable barriers to endogenous molecules as well as targeted therapies in vivo. Deidre P. MacIntosh et. al, Targeting endothelium and its dynamic caveolae for tissue-specific transcytosis in vivo: A pathway to overcome cell barriers to drug and gene delivery, PNAS 99 (4): 1996-2001, Feb. 19, 2002 

polymorph: Solid material that exists at least in two different molecular arrangements, i.e., distinctly different crystal species. Note 1: The differences between polymorphs disappear in solution or in the vapor phase. Note 2: Solubility, melting point, density, crystal shape, crystal structure, and some other physical properties often differ from one polymorph to the other. IUPAC Pharmaceutics

polymorphic transition: Transition of a solid crystalline phase to another phase having the same chemical composition but a different crystal structure. Note: The transition may occur at a characteristic temperature and pressure, called the inversion point. 
[3,20] IUPAC Pharmaceutics

Existence of two or more different crystal structures for the same compound. IUPAC Pharmaceutics

preformulation: Exploratory activity that begins early in pharmaceutics, involving studies designed to determine the compatibility of excipients with the active substance for a biopharmaceutical; physicochemical and bioanalytical investigation in support of promising experimental formulations. [21] IUPAC Pharmaceutics

prodrug: Chemically modified form of a pharmacologically active compound that has to undergo biochemical or chemical transformation before exhibiting its pharmacological effect.  IUPAC Pharmaceutics

protein delivery: It is a safe bet that if a therapeutic protein is bringing in big money and its patent is nearing expiration, someone somewhere with a clever technology is planning a market invasion based on improving how the protein is delivered.

targeted drug delivery: sometimes called smart drug delivery,[1] is a method of delivering medication to a patient in a manner that increases the concentration of the medication in some parts of the body relative to others. This means of delivery is largely founded on nanomedicine, which plans to employ nanoparticle-mediated drug delivery in order to combat the downfalls of conventional drug delivery. These nanoparticles would be loaded with drugs and targeted to specific parts of the body where there is solely diseased tissue, thereby avoiding interaction with healthy tissue. The goal of a targeted drug delivery system is to prolong, localize, target and have a protected drug interaction with the diseased tissue. The conventional drug delivery system is the absorption of the drug across a biological membrane, whereas the targeted release system releases the drug in a dosage form. The advantages to the targeted release system is the reduction in the frequency of the dosages taken by the patient, having a more uniform effect of the drug, reduction of drug side-effects, and reduced fluctuation in circulating drug levels. The disadvantage of the system is high cost, which makes productivity more difficult and the reduced ability to adjust the dosages. Wikipedia accessed 2018 Nov 5

therapeutic equivalence: Approved Drug Products with Therapeutic equivalence evaluations "Orange Book"
Search the Orange Book Database

Drug delivery resources
Contract Pharma Glossary of Pharmaceutical and Biopharmaceutical Terms, revised annually 
IUPAC, Glossary of terms related to pharmaceutics, Pure and Applied Chemistry 81, 971–999, 2009, 

How to look for other unfamiliar  terms

IUPAC definitions are reprinted with the permission of the International Union of Pure and Applied Chemistry.

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