Maleic Acid as a Co-Former for Pharmaceutically Active GABA Derivatives: Mechanochemistry or Solvent Crystallization?

Article Chemistry, Physical

Combined synthetic and solubility aspects of orotate salt of bilastine

Sunil Kumar Nechipadappu et al.

Summary: This study describes the synthesis and properties of a novel salt of Bilastine with orotic acid, which exhibits thermal stability and increased solubility compared to pure BLA drug.

JOURNAL OF MOLECULAR STRUCTURE (2023)

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Article Chemistry, Physical

Physicochemical aspects and comparative analysis of Voxelotor and its salt and cocrystal

Uday Kumar Neelam et al.

Summary: This study investigated the crystal forms of Voxelotor using crystallographic and solid-state characterization techniques, revealing the improved solubility and stability of VOX-HCl salt and VOX-SC cocrystal.

JOURNAL OF MOLECULAR STRUCTURE (2023)

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Article Pharmacology & Pharmacy

Lopinavir-Loaded Self-Nanoemulsifying Drug Delivery System for Enhanced Solubility: Development, Characterisation and Caco-2 Cell Uptake

Arshad Ali Khan et al.

Summary: A self-nanoemulsifying drug delivery system (SNEDDS) for lopinavir (LPV) was developed to improve its limited oral bioavailability. The optimized formulation showed small droplet size and high stability, and released nearly 99% of LPV within 30 minutes, indicating its potential to enhance the solubility and oral bioavailability of LPV.

CURRENT DRUG DELIVERY (2023)

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Article Chemistry, Multidisciplinary

Huge solubility increase of poorly water-soluble pharmaceuticals by sulfobutylether-β-cyclodextrin complexation in a low-melting mixture

Justine Petitprez et al.

Summary: The poor solubility and bioavailability of pharmaceuticals is a major issue in the pharmaceutical industry and can lead to environmental accumulation and the need for higher doses. In this study, cyclodextrin-based low-melting mixtures were used to greatly enhance the solubility of four steroids. This solubility enhancement is attributed to the formation of inclusion complexes with cyclodextrin within the low-melting mixture.

ENVIRONMENTAL CHEMISTRY LETTERS (2022)

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Article Pharmacology & Pharmacy

Improved solubility of lornoxicam by inclusion into SBA-15: Comparison of loading methods

Adrianna Dadej et al.

Summary: This study compares two methods of loading lornoxicam on SBA-15 and APTES-modified SBA-15 and investigates the drug release profiles and cytotoxicity. The results show that the adsorption equilibrium method is more advantageous and APTES-modified SBA-15 is an effective and non-toxic carrier for lornoxicam.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2022)

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Article Chemistry, Medicinal

Co-Crystals of Etravirine by Mechanochemical Activation

Marieta Muresan-Pop et al.

Summary: This study investigated the co-crystals formation of etravirine with three carboxylic acids. New co-crystals of etravirine with adipic acid, benzoic acid, and 4-hydroxybenzoic acid were synthesized by wet milling and their novelty and different morphology were confirmed by various analyses. The wet milling process resulted in a reduction in fusion enthalpy and melting temperature of the co-crystals. These co-crystals showed stability during storage, except for the co-crystal with benzoic acid. UV absorption spectra revealed conformational changes of etravirine due to hydrogen bonds with carboxylic acids.

JOURNAL OF PHARMACEUTICAL SCIENCES (2022)

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Article Chemistry, Medicinal

Pharmaceutical Cocrystals of Famotidine: Structural and Biopharmaceutical Evaluation

Akshita Jindal et al.

Summary: This study synthesized two novel cocrystals of famotidine and evaluated their properties. The cocrystals significantly improved the solubility and bioavailability of famotidine, leading to an increase in its anti-ulcer and antioxidant potential. The findings suggest that cocrystals are an effective approach for delivering neutral compounds with poor solubility.

JOURNAL OF PHARMACEUTICAL SCIENCES (2022)

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Article Instruments & Instrumentation

Soluplus (R) polymeric nanomicelles improve solubility of BCS-class II drugs

Rosario Pignatello et al.

Summary: This study characterized Soluplus(R) nanomicelles to enhance the apparent solubility of drugs in BCS class II. The prepared nanomicelles showed small and stable particle size and could be easily filtered. The freeze-dried powder materials maintained the micelle size upon reconstitution. Additionally, the nanomicelles demonstrated potential applications in topical ocular administration.

DRUG DELIVERY AND TRANSLATIONAL RESEARCH (2022)

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Article Chemistry, Medicinal

Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration

Kevin Antraygues et al.

Summary: In this study, the objective was to design and synthesize rifabutin prodrugs with increased aqueous solubility for intravenous use. Seventeen prodrugs were synthesized using developed synthetic methodologies, and their water solubility, stability in plasma, and antimicrobial activity against A. baumannii were evaluated. A pharmacokinetic release study in CD1 mice demonstrated the successful release of active rifabutin from selected prodrugs.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Article Pharmacology & Pharmacy

Posaconazole-amino acid cocrystals for improving solubility and oral bioavailability while maintaining antifungal activity and low In vivo toxicity

Venkata Deepthi Vemuri et al.

Summary: The present study successfully modulated the biopharmaceutical parameters of posaconazole through co-crystallization with amino acids as co-formers. The resulting cocrystals showed improved solubility and dissolution compared to the parent molecule, as well as good stability and enhanced bioavailability. These findings highlight the potential of co-crystallization technique in improving the physicochemical properties of poorly water-soluble drugs.

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY (2022)

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Article Pharmacology & Pharmacy

Development of biodegradable chitosan/ graphene oxide nanocomposite via spray drying method for drug loading and delivery application

Neema Pandey et al.

Summary: In this study, biocompatible chitosan (CS) - graphene oxide (GO) nanocomposites were synthesized using the spray drying method, and their mechanical, thermal, and drug delivery properties were evaluated. The results showed that the CS/GO nanocomposite with a concentration of 5 wt% exhibited the best combination of thermal and mechanical properties, making it suitable for the delivery of curcumin (CU) drug. The CS/GO nanocarrier system had a high drug entrapment efficiency and demonstrated controlled release of the CU drug. In vitro experiments showed that the CS/GO/CU nanocomposite had a stronger cytotoxic effect on human prostate cancer cells (PC-3) compared to the CU drug alone.

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY (2022)

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Article Materials Science, Multidisciplinary

Preparation of cisplatin delivery calcium phosphate nanoparticles using poly(Pt(IV) prodrug) as the payload

Yue Yu et al.

Summary: Encapsulating cisplatin in calcium phosphate nanoparticles is challenging due to its low solubility and weak binding affinity. This study presents a unique strategy using a polymer bearing numerous carboxyl side groups and incorporating redox-sensitive cisplatin prodrugs for encapsulation in CPNPs. The encapsulated CPNPs showed enhanced stability and efficacy against cancerous cells compared to free cisplatin and the prodrug alone.

MATERIALS TODAY COMMUNICATIONS (2022)

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Article Chemistry, Medicinal

Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies

Jinqian Liu et al.

Summary: New oral antibiotic CZA is effective against Gram-positive infections and suitable for intravenous administration. It rapidly converts into the active drug CZD in vivo and shows similar or better activity than CZD in preclinical infection models. CZA has undergone Phase 1 and Phase 2 clinical trials and is advancing into further clinical studies.

ACS MEDICINAL CHEMISTRY LETTERS (2022)

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Article Pharmacology & Pharmacy

Platensimycin-berberine chloride co-amorphous drug system: Sustained release and prolonged half-life

Zhe Wang et al.

Summary: Co-amorphous PTM-BCL system was developed for oral delivery of PTM, showing sustained release characteristics and excellent physiochemical stability. The molecular interactions between PTM and BCL were mediated by strong charged-mediated hydrogen bonds. Co-amorphous PTM-BCL exhibited 2- or 3-fold longer half-life in rats than crystalline and amorphous PTM. Rational approach to realize the full potential of potent antibiotic PTM was suggested.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS (2022)

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Article Chemistry, Multidisciplinary

Combining lipid based drug delivery and amorphous solid dispersions for improved oral drug absorption of a poorly water-soluble drug

Georgia-Ioanna Nora et al.

Summary: In this study, the combination of two drug delivery approaches, SNEDDS and ASD, was used to enhance the physical stability, solubility, and absorption of ritonavir. The addition of an ASD to SNEDDS increased the supersaturation degree and physical stability of the system, resulting in higher bioavailability in rats.

JOURNAL OF CONTROLLED RELEASE (2022)

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Article Pharmacology & Pharmacy

Improving the solubility, hygroscopicity and permeability of enrofloxacin by forming 1:2 pharmaceutical salt cocrystal with neutral and anionic co-existing p-nitrobenzoic acid

Lixin Liu et al.

Summary: This study designed and synthesized a pharmaceutical salt cocrystal of enrofloxacin with p-nitrobenzoic acid to improve its solubility and reduce its hygroscopicity. The salt cocrystal was characterized by its crystal structure and found to consist of enrofloxacin cations, p-nitrobenzoic acid anions, and p-nitrobenzoic acid neutral molecules in a 1:1:1 ratio. The presence of the salt cocrystal resulted in improved permeability and antibacterial activity of enrofloxacin.

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY (2022)

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Article Chemistry, Physical

Labrasol mediated enhanced solubilization of natural hydrophobic drugs in Pluronic micelles: Physicochemical and in vitro release studies

Jaspreet Kaur et al.

Summary: In this study, the solubilization of two natural hydrophobic drugs, Quercetin and Curcumin, was investigated in Pluronics and Pluronics-Labrasol mixed micelles. The results showed that the solubility of both drugs was significantly higher in Pluronic P84 and P84-Labrasol mixed micelles compared to other systems. The enhanced solubilization was supported by fluorescence titrations and dynamic light scattering.

JOURNAL OF MOLECULAR LIQUIDS (2022)

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Article Crystallography

A Lection in Humbleness: Crystallization of Chiral and Zwitterionic APIs Baclofen and Phenibut

Marco Herbst et al.

Summary: This study discusses the crystallization and multicomponent crystal formation of active pharmaceutical ingredients with dicarboxylic acid co-formers. The research elucidates the crystallization process of several crystalline entities and investigates the factors influencing the outcome.

CRYSTALS (2022)

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Article Chemistry, Multidisciplinary

Co-crystals of zwitterionic GABA API's pregabalin and phenibut: properties and application

Daniel Komisarek et al.

Summary: Several multicomponent crystalline species formed by zwitterionic GABA analogues pregabalin and phenibut are presented in this study. The compounds are evaluated based on their crystal structure and properties such as melting behaviour, solubility, and lattice energies. Furthermore, the major property distinctions between a homo- and heterochiral co-crystalline system and how they enable enantiopurification of pregabalin are discussed.

CRYSTENGCOMM (2022)

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Article Thermodynamics

Ball-milled valsartan and its combination with mannitol: the case of drug polyamorphism

Iara Cristina Schmucker Lenschow et al.

Summary: This study investigates the influence of ball milling conditions and the association of Valsartan (VAL) with mannitol on its dissolution rate and solid-state properties. The results show that ball milling changes the polyamorphic forms of VAL and the association with mannitol improves the dissolution rate of the drug.

JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY (2022)

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Article Chemistry, Multidisciplinary

Sparfloxacin Multicomponent Crystals: Targeting the Solubility of Problematic Antibiotics

Mariama Djalo et al.

Summary: The study reports five novel molecular salts of sparfloxacin with generally regarded as safe coformers, which show higher water solubility and potential for lower dosage intake. These new forms exhibit improved physicochemical properties compared to sparfloxacin itself, with the citrate salt showing a 1 order higher aqueous solubility.

CRYSTAL GROWTH & DESIGN (2021)

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Article Chemistry, Multidisciplinary

A Case Study on the Desired Selectivity in Solid-State Mechano- and Slow-Chemistry, Melt, and Solution Methodologies

Krzysztof Budny-Godlewski et al.

Summary: Solution-based syntheses are commonly used in chemistry but have disadvantages, prompting the search for new mild and green synthetic methods. This study compared four different reaction media and found that solid-state approaches were stoichiometry sensitive, allowing for the selective synthesis of two adducts through simple stoichiometric control. Additionally, density functional theory calculations revealed structural and thermodynamic features of the adducts, showing unique non-redox active metal complexes supported by nitroxide radicals.

CHEMSUSCHEM (2021)

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Review Pharmacology & Pharmacy

Mechanochemistry: A Green Approach in the Preparation of Pharmaceutical Cocrystals

Mizrain Solares-Briones et al.

Summary: Mechanochemistry is considered an alternative and environmentally friendly synthetic tool that has a significant impact on various chemistry fields, especially in the preparation of pharmaceutical cocrystals. Its advantages include the ability to carry out reactions under solvent-free or minimal solvent conditions, reducing environmental impact and improving efficiency in the synthesis of multicomponent solid forms.

PHARMACEUTICS (2021)

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Review Biochemistry & Molecular Biology

Classics in Chemical Neuroscience: Baclofen

Caitlin N. Kent et al.

ACS CHEMICAL NEUROSCIENCE (2020)

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Article Chemistry, Multidisciplinary

Tuning Physicochemical Properties of Antipsychotic Drug Aripiprazole with Multicomponent Crystal Strategy Based on Structure and Property Relationship

Yanxiao Zhao et al.

CRYSTAL GROWTH & DESIGN (2020)

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Article Chemistry, Multidisciplinary

Mercury 4.0: from visualization to analysis, design and prediction

Clare F. Macrae et al.

JOURNAL OF APPLIED CRYSTALLOGRAPHY (2020)

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Article Biochemistry & Molecular Biology

Combined X-ray Crystallographic, IR/Raman Spectroscopic, and Periodic DFT Investigations of New Multicomponent Crystalline Forms of Anthelmintic Drugs: A Case Study of Carbendazim Maleate

Alexander P. Voronin et al.

MOLECULES (2020)

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Article Chemistry, Multidisciplinary

Green Mechanochemical Strategy for the Discovery and Selective Preparation of Polymorphs of Active Pharmaceutical Ingredient γ-Aminobutyric Acid (GABA)

Lingyu Wang et al.

ACS SUSTAINABLE CHEMISTRY & ENGINEERING (2020)

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Review Chemistry, Organic

Solvent-free Methods for Co-crystal Synthesis: A Review

Saroj Kumar et al.

CURRENT ORGANIC SYNTHESIS (2019)

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Article Chemistry, Multidisciplinary

Resolution of Baclofenium Hydrogenomaleate By Using Preferential Crystallization. A First Case of Complete Solid Solution at High Temperature and a Large Miscibility Gap in the Solid State

Francois-Xavier Gendron et al.

CRYSTAL GROWTH & DESIGN (2019)

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Review Pharmacology & Pharmacy

Is prodrug design an approach to increase water solubility?

Bruna M. A. Sanches et al.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2019)

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Review Chemistry, Medicinal

NMR spectroscopy in drug discovery and development: Evaluation of physico-chemical properties

Mire Zloh

ADMET AND DMPK (2019)

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Article Chemistry, Multidisciplinary

In Situ Investigations of Mechanochemical One-Pot Syntheses

Hannes Kulla et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2018)

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Review Pharmacology & Pharmacy

Antiepileptic drugs as analgesics/adjuvants in inflammatory pain: current preclinical evidence

Maja Tomic et al.

PHARMACOLOGY & THERAPEUTICS (2018)

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Article Chemistry, Physical

Determination of the solubility of 2-Methyl-1,3-benzothiazol-5-amine molecule with aqueous ethanol by NMR spectroscopy

Gokhan Dikmen

JOURNAL OF MOLECULAR LIQUIDS (2018)

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Article Pharmacology & Pharmacy

Drug solubilization by complexation

Thorsteinn Loftsson

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2017)

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Review Biochemistry & Molecular Biology

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

Daniela Hartmann Jornada et al.

MOLECULES (2016)

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Review Pharmacology & Pharmacy

Perspectives on the amorphisation/milling relationship in pharmaceutical materials

M. Descamps et al.

ADVANCED DRUG DELIVERY REVIEWS (2016)

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Article Chemistry, Multidisciplinary

Cocrystal and Salt Forms of Furosemide: Solubility and Diffusion Variations

Manas Banik et al.

CRYSTAL GROWTH & DESIGN (2016)

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Article Medicine, Legal

The relevance of international assessments to GRAS determinations

Claire Kruger

REGULATORY TOXICOLOGY AND PHARMACOLOGY (2016)

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Editorial Material Plant Sciences

Plant GABA: Not Just a Metabolite

Alan W. Bown et al.

TRENDS IN PLANT SCIENCE (2016)

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Article Chemistry, Multidisciplinary

Soluble Salts and Cocrystals of Clotrimazole

Sudhir Mittapalli et al.

CRYSTAL GROWTH & DESIGN (2015)

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Article Chemistry, Multidisciplinary

Are gamma amino acids promising tools of crystal engineering? - Multicomponent crystals of baclofen

Nikoletta B. Bathori et al.

CRYSTENGCOMM (2015)

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Article Biochemistry & Molecular Biology

Efficient Synthesis of β-Aryl-γ-lactams and Their Resolution with (S)-Naproxen: Preparation of (R)-and (S)-Baclofen

Iris J. Montoya-Balbas et al.

MOLECULES (2015)

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Article Chemistry, Multidisciplinary

Crystal structure refinement with SHELXL

George M. Sheldrick

ACTA CRYSTALLOGRAPHICA SECTION C-STRUCTURAL CHEMISTRY (2015)

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Article Medicine, Research & Experimental

Unravelling the Relationship between Degree of Disorder and the Dissolution Behavior of Milled Glibenclamide

Pei T. Mah et al.

MOLECULAR PHARMACEUTICS (2014)

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Review Pharmacology & Pharmacy

Use of pharmaceutical salts and cocrystals to address the issue of poor solubility

David P. Elder et al.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2013)

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Article Chemistry, Analytical

Biorelevant pKa (37°C) predicted from the 2D structure of the molecule and its pKa at 25°C

Na Sun et al.

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS (2011)

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Review Pharmacology & Pharmacy

Nanosuspension: An approach to enhance solubility of drugs

Vishal R. Patel et al.

JOURNAL OF ADVANCED PHARMACEUTICAL TECHNOLOGY & RESEARCH (2011)

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Review Pharmacology & Pharmacy

A Comparison of the Pharmacokinetics and Pharmacodynamics of Pregabalin and Gabapentin

Howard N. Bockbrader et al.

CLINICAL PHARMACOKINETICS (2010)

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Article Chemistry, Multidisciplinary

Understanding and Predicting the Effect of Cocrystal Components and pH on Cocrystal Solubility

Sarah J. Bethune et al.

CRYSTAL GROWTH & DESIGN (2009)

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Article Chemistry, Multidisciplinary

Crystal Engineering of an Anti-HIV Drug Based on the Recognition of Assembling Molecular Frameworks

Felipe T. Martins et al.

CRYSTAL GROWTH & DESIGN (2009)

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Article Chemistry, Multidisciplinary

Solubility Advantage of Pharmaceutical Cocrystals

David J. Good et al.

CRYSTAL GROWTH & DESIGN (2009)

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Article Pharmacology & Pharmacy

Use of 1H NMR to facilitate solubility measurement for drug discovery compounds

Melissa Lin et al.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2009)

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Software Review Chemistry, Multidisciplinary

OLEX2: a complete structure solution, refinement and analysis program

Oleg V. Dolomanov et al.

JOURNAL OF APPLIED CRYSTALLOGRAPHY (2009)

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Article Pharmacology & Pharmacy

Comparative pharmacological activity of optical isomers of phenibut

Maija Dambrova et al.

EUROPEAN JOURNAL OF PHARMACOLOGY (2008)

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Article Chemistry, Multidisciplinary

A short history of SHELX

George M. Sheldrick

ACTA CRYSTALLOGRAPHICA A-FOUNDATION AND ADVANCES (2008)

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Review Pharmacology & Pharmacy

Salt formation to improve drug solubility

Abu T. M. Serajuddin

ADVANCED DRUG DELIVERY REVIEWS (2007)

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Article Medicine, Research & Experimental

The salt-cocrystal continuum: The influence of crystal structure on ionization state

Scott L. Childs et al.

MOLECULAR PHARMACEUTICS (2007)

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Review Psychology, Clinical

Role of GABA in anxiety and depression

Allan V. Kalueff et al.

DEPRESSION AND ANXIETY (2007)

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Article Pharmacology & Pharmacy

GABA and glycine as neurotransmitters: a brief history

NG Bowery et al.

BRITISH JOURNAL OF PHARMACOLOGY (2006)

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Article Pharmacology & Pharmacy

The effect of crystal morphology and mill type on milling induced crystal disorder

V Chikhalia et al.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2006)

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Review Chemistry, Multidisciplinary

Mechanochemistry: The mechanical activation of covalent bonds

MK Beyer et al.

CHEMICAL REVIEWS (2005)

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Article Neurosciences

Baclofen decreases methamphetamine self-administration in rats

R Ranaldi et al.

NEUROREPORT (2002)

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Article Chemistry, Multidisciplinary

What is the true solubility advantage for amorphous pharmaceuticals?

BC Hancock et al.

PHARMACEUTICAL RESEARCH (2000)

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Maleic Acid as a Co-Former for Pharmaceutically Active GABA Derivatives: Mechanochemistry or Solvent Crystallization?

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