Pharmaceutical Sciences Research Solutions

Drug discovery

Drug discovery lies at the interface of disciplines such as biological sciences and medicine. It often involves expertise in chemistry, biochemistry, and subjects such as protein science, biotherapeutics, and nanobiotechnology. Different drugs can involve specializations, such as:

Genetics
Hematology
Vaccines
Virology

Modern drug discovery in the lab can involve automation, allowing researchers to investigate wide-ranging possibilities.

Our application notes show how our instruments are used in a range of drug discovery solutions. You can find a selection below – take a look to discover more!

Drug Discovery	Method	Sample	Application Note Title (Web link)
Antibody characterization in human blood plasma	GCI	Three SARS-CoV-2 antigens and patient plasma samples (diluted to 5%)	Antibody characterization from COVID-19 patient plasma binding to SARS-COV-2 antigens
APIs - crystalline and amorphous content	XRD	Amorphous/crystalline mixture	Quantitative XRD - Detection of low amounts of crystalline impurities for pharmaceutical process control
APIs and Excipients - crystallization monitoring	XRD	Slurry of Lactose (as a model) in ethanol	On-line crystallization monitoring: Slurry Flow Cell for in situ investigation of crystallization processes
APIs and Excipients - particle size screening	LD	Lactose	Detecting the presence of anomalous large particles within powders using laser diffraction particle size analysis
APIs and Excipients - automated identification of polymorphs using Raman	IMG	Acetaminophen	Discriminating between polymorphs of acetaminophen using Morphologically Directed Raman Spectroscopy
APIs and Excipients - Composition and polymorph identification	XRD	Ventolin™ (salbutamol)	Diffraction on aerosol drugs. Measurements on small quantities of pharmaceutical samples
APIs and Excipients - crystallite size	XRD	Azithromycin antibiotic	Crystallite size determination of a pharmaceutical compound by Rietveld analysis
APIs and Excipients - crystallite size with temperature and humidity	XRD	Salbutamol	Automatic condensation-free combined temperature-humidity control for XRD studies
APIs and excipients - high throughput identification of polymorphs by XRD	XRD	Cimetidine	High-resolution, high-throughput XRPD
Binding Kinetics of a G-Protein-Coupled receptor	GCI	GPCR and a 725 Da mutated neurotensin	Binding kinetics of a GPCR
Cosmetic ingredients - preparation for ICP	SPE	Cosmetics – harmful trace elements – sample preparation	Metal Determination in Cosmetics by ICP
DNA Vaccines - molecular weight	SEC	Plasmid DNAs, a mixture of three topo isomers: supercoiled (SC), open circle (OC), and linear (lin)	Analysis of plasmid DNA using SEC
Drug development - assay development	ITC	Various proteins, peptides, small molecule compounds, and in buffers	From assay development to lead optimization using Isothermal Titration Calorimetry
Drug discovery - Enzymes	ITC	Phosphatidylinositol 3-kinase (Vps34)	Multiple applications for the Malvern MicroCal Auto-iTC200 in a fragment-based drug discovery campaign
Drug discovery - microcalorimetry of APIs	ITC	APIs, small molecules, and proteins	Application of microcalorimetry in drug discovery at Exelixis
Drug discovery - protein interactions	DSC	Protein/protein interactions, therapeutics	Targeting protein/protein interactions in drug design
Excipients - molecular weight	SEC	Cellulose derivatives (HEC), (HPC), (HPMP), and (HBMC)	Understanding the effect of molecular weight and structure on the performance characteristics of cellulose derivatives using OMNISEC
Excipients - particle shape variations	IMG	Two excipients from different suppliers	Morphological Comparison of Pharmaceutical Excipients
Excipients - particle size and shape	IMG	Lactose as a model for excipients	Pharmaceutical Excipient Characterization
Excipients - particle size distribution	LD	Lactose	Measuring the particle size of small quantities of dry powders using the Aero S and Mastersizer 3000
GCI and kinetic screening with the Creoptix^® WAVEdelta	GCI	Collection of small molecules	Molecular interaction analysis by Grating-Coupled interferometry (GCI)
Off-rate screening: optimising hit-to-lead	GCI	Eighty-three (83) crude reaction mixtures (CRM)	Rapid optimization of hit and lead compounds
Oxygen carriers - particle size, stability	DLS	Hemoglobin-based oxygen carriers (HBOC)	Size, Oligomeric State and Thermal Stability of Chemically Modified Hemoglobins
Small molecules: kinetic screening with waveRAPID	GCI	Target protein against library of small molecules	Pushing the boundaries in pharmaceutical hit discovery with the novel waveRAPID^® kinetic assay
Small molecules: large target-to-analyte molecular weight	GCI	Various small molecule inhibitors of Carbonic Anhydrase II (CAII)	Sensitive kinetic analysis of small molecules binding to large drug targets
Therapeutic Proteins - particle size	DLS	Antibodies	Therapeutic protein characterization
Therapeutic Proteins - stability	DSC	Immunoglobulins, IgG, and IgE	Accelerating biotherapeutic process development using Differential Scanning Calorimetry

Drug delivery

Drug delivery helps ensure that the process of drug release into the human body is safe, effective, and targeted. It can range from relatively simple oral dose tablets to highly sophisticated, targeted drugs such as those used in gene therapy or chemotherapy.

Below, you’ll find a selection of application notes and articles showing how our analytical instruments can provide drug delivery solutions. Feel free to explore them and learn more!

Drug Delivery	Method	Sample	Application Note Title (Web link)
Controlled drug release - size and zeta potential with temperature	DLS	Poly(N-isopropylacrylamide) (PNIPAM) coated Silica particles	Thermo- and pH-Sensitive PNIPAM-Coated Silica Particles Studied Using Light Scattering
Encapsulation - degradation, molecular weight	SEC	PLA-PEO-PLA polymers	Evaluating degradation of drug delivery polymers using Advanced Polymer Chromatography (APC) and advanced multi-detection
Encapsulation - size and concentration	NTA	Polylactic Acid (PLA) particles	Assessing Drug Encapsulation Efficiency using Nanoparticle Tracking Analysis
Encapsulation - size and zeta potential	DLS	Pharmaceutical manufacturing/ agriculture	Characterization of a Protein - Chitosan Complex
Inhalers - foreign particulate matter	IMG	General inhaler formulation	Foreign Particulate Matter testing using the Morphologi^® G3
Inhalers - particle size, shape	IMG	Metered-dose inhaler (MDI) for lung disorders	In vitro bioequivalence studies for a metered dose inhaler formulation using the Morphologi automated particle imaging system
Lipid Emulsions - Induced Flocculation	DLS/ELS	Calcium + Intralipid (soybean oil, egg phospholipids, and glycerin)	Calcium Induced Flocculation of Intralipid
Lipid Emulsions - size, polydispersity in concentrated solutions	DLS	Oil-in-water, parenteral nutrition emulsions	Measuring Globule Size in Lipid Injectable Emulsions Using Non-Invasive Back Scatter Dynamic Light Scattering (NIBS-DLS)
Lipid Emulsions – zeta potential in concentrated solutions	ELS	Intralipid (soy bean oil, egg phospholipids, and glycerin)	Zeta Potential Characterization of Concentrated Lipid Emulsions
Liposomes - size and concentration	NTA	Poly(β-amino ester)s (PBAEs), Poly(lactic-co-glycolic acid) (PLGA)	Direct visualization, sizing, and concentration measurements of drug delivery nanoparticles using Nanoparticle Tracking Analysis (NTA)
Liposomes - size and concentration	IMG	Hydrogenated soy phosphatidylcholine (HSPC)/(5-cholesten-3ß-ol)CHOL	Characterizing the size and concentration of liposomes using multi-angle dynamic light scattering
Liposomes - size and zeta potential	DLS	Anionic and cationic liposomes	Size and zeta potential characterization of liposomes using the Zetasizer Nano
Liposomes – zeta potential	ELS	Complexes with DNA	The use of zeta potential and DLS measurements in gene therapy research
Liposomes- characterization methods	XRD	White paper	Characterization of liposomes by several complementary techniques
Nasal Spray - particle size versus time	LD	Nasal spray	Monitoring Nasal Spray Tail-Off using the Malvern Spraytec
Nasal spray - particle size vs actuation method	LD	Nasal spray	Understanding the performance of nasal spray drug delivery systems using the Malvern Spraytec
Nasal Spray - sorting particle size and shape	IMG	Nasal spray	Automation of manual QC analysis of suspension nasal spray products using the Morphologi automated imaging system
Nebulizers - particle size	LD	Spray solution	Particle characterization of inhalation drug suspensions on the FPIA-3000
Polymer carriers - conjugate levels	SEC	Doxorubicin (Dox) and Polyglutamic acid (PG)	Optimizing drug delivery polymer conjugate levels using Advanced Multi-Detector GPC
Suspensions - particle size distribution	LD	Sodium alginate, sodium bicarbonate, and calcium carbonate	Understanding the functionality of suspension-based pharmaceutical products
Suspensions - particle stability, Zeta potential	DLS	Various particles in apolar solvent systems	The influence of electrostatic stabilization in apolar suspension formulations
Tablets - chemical phase quantification	XRD	Pharmaceutical Science and Technology, and Manufacturing	Quantitative evaluation on pharmaceutical solids
Tablets - particle size and shape	IMG	Generic drugs as powdered tablets	In vitro bioequivalence studies for oral solid dose products using the Morphologi ID

Formulation

No matter how they are administered, all medicines need to be delivered in manageable formulations that have a known shelf life and don’t deteriorate into ineffective or toxic forms. In personal healthcare and cosmetics, the stability, look, and feel of a formulation is also an important part of making a product attractive. Formulation requires expertise in chemistry, process engineering, and specific pharmaceutical sciences.

Below you’ll find a selection of application notes and articles on drug formulation research. Enjoy exploring them and finding out more!

Formulation	Method	Sample	Application Note Title (Web Link)
Creams - particle size and shape	IMG	General topical skin cream	Automated analysis of drug crystals in topicals and creams using the Morphologi G3 automated image analysis system
Creams - particle size, Zeta potential	DLS / ELS	Encapsulated retinol system, retinol (vitamin A), waxes, anionic and ionic surfactants	Optimizing topical skin care formulations and production
Creams - particles Chemical Identification	MDRS	General topical skin cream	Component-specific particle characterization of the active components in a pharmaceutical-topical formulations
Excipients - crystalline/amorphous ratio	XRD	Filler and dilutant: alpha-lactose monohydrate	Crystallinity determination - Quantification of low amounts of amorphous material in a crystalline matrix and vice versa
Excipients - particle size	IMG	Milled lactose fines (LH210), coarse lactose carrier (LH100), and blended with budesonide	Understanding the properties of dry powder inhaler formulations through combined cascade impaction and automated image analysis measurements
Excipients and additives - Protein stabilization	ITC / DSC	ProX, Polysorbate-80, and phenol	Applications of Isothermal Titration Calorimetry and Differential Scanning Calorimetry in biopharmaceutical formulation development
Gels - crystalline particle size and shape	MDRS	Benzoyl peroxide and adapalene in Epiduo gel	Microstructure of crystals in a topical drug product
Liquids - size distributions in microemulsions	DLS	API, oil surfactant, and alcohol in water	Microemulsion characterization using dynamic light scattering
Liquids - nanomaterial dose	NTA	Cerium (IV) Oxide, Titanium dioxide nanoparticles	Time-resolved description of nanomaterial dose under relevant biological and environmental conditions
Manufacturing - materials identification in Quality Control	XRF	General pharmaceuticals	Material identification by FingerPrint
Manufacturing - trace elements	XRF	Cd, Pb, As, Hg, Co, V, Ni, Tl, Pd, Ir, Rh, Ru, Se, Pt, Mo, Cu, and Cr	Non-destructive elemental analysis of impurities in pharmaceuticals according to ICH Q3D and USP <232>
Manufacturing - virus stability	DLS	Three adeno-associated virus (AAV) samples	Measuring the concentration of Adeno-Associated Virus (AAV) with multi-angle dynamic light scattering (MADLS)
Nasal spray - APIs in mixtures	MDRS	Inhalers	Supporting dry powder inhaler formulation development using component-specific particle characterization
Ointment - particle size and shape	IMG	General ointment	Automation of QC microscope measurements of a pharmaceutical ointment using the Morphologi particle characterization system
Oral solid dosage - analytical methods review	Various	White paper - review article	Analytical techniques with a place in the oral solid dosage formulation toolkit
Oral solid dosage - Bioequivalence	MDRS	Painkillers	Confirming the pharmaceutical equivalence of Oral Solid Dose (OSD) products using MDRS and the Morphologi 4-ID
Oral solid dosage - API particle size	LD	Tablet prepared as a suspension	Determining the particle size of active pharmaceutical ingredient within oral solid dose products using the FPIA-3000 dynamic imaging system
Pastes - elemental identification	XRF	Toothpaste	Fast toothpaste identification by FingerPrint
Powders - particle agglomeration	IMG & MDRS	General examples including APIs	Identification of Agglomerates Using Automated Image Analysis
Powders - particle size	MDRS	Cold remedy formulations compared	Deformulation of a pharmaceutical formulation using the Morphologi ID
Protein formulations - aggregation	NTA	Protein aggregates	High-resolution sizing and concentration measurements of sub-visible protein aggregates using NTA
Protein formulations - aggregation	MDRS	Lysozyme (spiked with latex spheres)	Characterization of protein aggregates by Morphologically Directed Raman Spectroscopy
Protein formulations - antibody interactions	DLS	Monoclonal antibodies (mAb), human serum albumin (HSA), and Immunoglobulin G (IgG)	Using A2 and kD to assess protein interactions in formulations
Protein formulations - lipid encapsulation, particle size changes	DLS	Lipid polymer	pH and Temperature Responsive Novel Nanoparticles Characterized by Dynamic Light Scattering
Protein formulations - liquid formulation stability	DSC	Monoclonal antibody, lyophilized	Using Differential Scanning Calorimetry to accelerate liquid formulation development for protein biopharmaceuticals
Protein formulations - long term stability	DSC	Antibodies and Fc-conjugated proteins	Correlating long term biotherapeutic stability with a fast analytical technique
Protein formulations - size, aggregation, stability	SEC	Human Ig in phosphate-buffered saline	Protein stability measurements amplified: Combining SEC-MALS and DLS to maximize data output
Protein formulations - role of stabilizers vs pH	DLS	Recombumin	Formulation stability evaluation using light scattering techniques
Stabilizers - crystal structure with temperature and humidity	XRD	Trehalose	2D XRD at non-ambient conditions
Stabilizers - crystal structure with temperature and humidity	XRD	Trehalose	Temperature- and humidity-controlled XRD
Protein formulations - stability	DLS	Insulin in phosphate-buffered saline (PBS) buffer	Assessing the self-association and stability of Insulin under varying formulation conditions using Taylor Dispersion Analysis
Protein formulations - stability in solution	DSC	Proteins	Use of microcalorimetry and its correlation with Size Exclusion Chromatography for rapid screening of the physical stability of large pharmaceutical proteins in solution
Protein Formulations - stabilizing excipients	DLS	Arginine	Investigating the effects of excipients on the earliest stages of aggregation - Aggregation inhibition by arginine
Protein formulations - Stabilizers vs temperature	DLS	Recombumin	Using Light Scattering to Study the Thermal Stability of Recombumin
Protein formulations - viscosity	SEC	Bovine serum albumin in histidine and arginine buffers.	Effect of excipients on protein formulation viscosity
Sprays - particle size	LD	Hairspray	Characterizing personal and domestic aerosol products using the Malvern Spraytec
Tablet Coating – particle size	LD	Tablet coating containing Titanium Oxide	Optimizing the processing of pigments using particle size analysis
Therapeutic Antibodies - characteristics for stability	DSC	Parent and engineered monoclonal antibodies	Engineering monoclonal antibodies to enhance drugability: A case study
Therapeutic Antibodies - molecular weight	SEC	Antibodies, in phosphate-buffered saline (PBS)	The power of multi-detector SEC in the analysis of antibodies
Therapeutic Antibodies - molecular weight	SEC	Immunoglobulin G (IgG)	Molecular weight measurements of an antibody using Viscotek SEC-MALS 20
Therapeutic Antibodies - purification, elution buffers	DSC	Antibody purification - various elution buffers	Manufacturing biotherapeutic faster using Differential Scanning Calorimetry (DSC)
Therapeutic Antibodies - stability	DSC	Genetically tailored antibody fragments	Selecting the most stable biotherapeutic antibody using Differential Scanning Calorimetry
Therapeutic Antibodies - stability in buffer solutions	DSC	Antibodies in a range of buffers	Preformulation and stability studies of biotherapeutics using DSC

略語解説

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略語	メソッド名	装置	測定された特性
DLS	動的光散乱法（DLS）	ゼータサイザー	分子サイズ、流体力学的半径R_H、粒子サイズ、粒度分布、安定性、濃度、凝集
ELS	電気泳動光散乱	ゼータサイザー	ゼータ電位、粒子電荷、懸濁液の安定性、タンパク質電気泳動移動度
ITC	等温滴定型カロリメトリー	MicroCal ITC	結合親和性、溶液中の分子反応の熱力学
.dsc	示差走査熱型カロリメトリー	Microcal DSC	大きな分子の変性(アンフォールド)、高分子の安定性
GCI	グレーティング結合干渉法	Creoptix WAVEsystem	リアルタイムの結合反応速度と親和性、流体工学によるラベルフリー
IMG	全自動画像解析	モフォロギ 4	粒子の画像処理、形状、サイズの自動測定
MDRS	Morphologically-Directed Raman Spectroscopy	モフォロギ4-ID	粒子の画像処理、形状、サイズの自動測定、化学的同定、汚染物質の検出
LD	レーザ回折	マスターサイザースプレーテックインシテック Parsum	粒子サイズ、粒度分布
NTA	ナノ粒子トラッキング(軌跡)解析	ナノサイト	粒子サイズ、粒度分布、濃度
SEC または GPC	サイズ排除クロマトグラフィー/ ゲル浸透クロマトグラフィー（GPC）	OmniSEC	分子サイズ、分子量、オリゴマー状態、ポリマーまたはタンパク質のサイズ、分子構造
SPE	融合によるサンプル調製	Le Neo LeDoser Eagon 2 The OxAdvanced M4 rFusion	XRF用溶融ビーズ試料の調製、ICP用過酸化物溶液の調製、ビーズ作製用のフラックス計量
UV/Vis/NIR/ SWIR	紫外線/可視/近赤外線/短波赤外線分光分析	LabSpec FieldSpec TerraSpec QualitySpec	材料識別と分析、水分、鉱物、炭素の含有量。航空および衛星分光分析技術の地上検証。
PFTNA	パルス高速熱中性子活性化	CNA	インライン元素分析
XRD-C	X線回折 (結晶構造解析)	Aeris Empyrean	分子結晶構造の精製、結晶相の同定と定量化、結晶対非結晶比、結晶子径分析
XRD-M	X線回折 (ミクロ構造)	Empyrean X’Pert³ MRD(XL)	残留応力、テクスチャ
XRD-CT	コンピュータ断層撮影法による X線吸収画像処理	Empyrean	固体、気孔率、密度の3D画像処理
SAXS	小角X線散乱法	Empyrean	ナノ粒子、サイズ、形状、構造
GISAXS	斜入射小角X線散乱法	Empyrean	ナノ構造の薄膜と表面
HR-XRD	高解像度X線回折	Empyrean X’Pert³ MRD(XL)	薄膜およびエピタキシャル多層、組成、ひずみ、厚さ、品質
XRR	X線反射率法	Empyrean X’Pert³ MRD(XL)	薄膜と表面、膜厚、表面、界面粗さ
XRF	蛍光X線	Epsilon Zetium Axios FAST 2830 ZT	元素組成、元素濃度、微量元素、汚染物質の検出