Pharmaceutical Cocrystals for Drug Delivery DOI
Ashwini Nangia

Burger's Medicinal Chemistry and Drug Discovery, Год журнала: 2025, Номер unknown, С. 1 - 62

Опубликована: Май 26, 2025

Abstract Pharmaceutical cocrystals offer the ability to tune solubility, permeability, tableting, and bioavailability of a solid, oral drug formulation without changing chemical structure molecule. Crystal engineering pharmaceutical salts via supramolecular heterosynthons with acceptable generally recognized as safe (GRAS) coformers provides platform technology for improving efficacy optimal delivery. With almost 90% drugs in Biopharmaceutics Classification System (BCS) class II IV suffering from low‐solubility and/or low‐permeability challenges, have provided an opportune intervention populating pipeline over past decade. From prototype cocrystal itraconazole‐succinic acid first salt‐cocrystal complex Entresto containing valsartan‐sacubitril, this review covers origins subject early 2000s peak growth curve model systems between 2005 2015, successful lab‐to‐market translation witnessed The combined application machine learning neural network tools is bringing speed accuracy research exercise designing drug–coformer therapeutic properties. This article snapshot summary latest trends leading discovery, development, continuous manufacturing.

Язык: Английский

Balancing the Heterocycles···Pyromellitic Dianhydride Interactions to Achieve Tunable Emission in Charge-Transfer Cocrystals DOI
Wanglong Hong, Yuxing Deng, Shengli Zhu

и другие.

Crystal Growth & Design, Год журнала: 2025, Номер 25(5), С. 1653 - 1666

Опубликована: Фев. 24, 2025

Cocrystal engineering focuses on adjustable noncovalent interactions (NCIs) and packing motifs through different functional molecular blocks to modulate physicochemical properties. NCIs are vital driving forces in the construction of organic cocrystal materials, such as π–π interactions, arene–perfluoroarene hydrogen bonds, halogen bonds. Herein, pyromellitic dianhydride (PMDA) serves electron acceptor, three heterocycle–acene-fused electron-rich donors, including 5H-benzo[4,5]thieno[3,2-c]carbazole (BTCZ), 5H-benzofuro[3,2-c]carbazole (BFCZ), 5,12-dihydroindolo[3,2-a]carbazole (ICZ), selected react with PMDA fabricate cocrystals. Single crystals BTCZ-PMDA, BFCZ-PMDA, ICZ-PMDA were grown via slow cooling solvent evaporation, their crystal structures, quantified NCIs, photoluminescent properties investigated. The results indicate that two types along stacking direction show imbalanced interaction energies for BTCZ-PMDA while well balanced within ICZ-PMDA. Moreover, red shift peak from 1.83 eV (BTCZ-PMDA) 1.53 (ICZ-PMDA) can be ascribed heterocycles···PMDA overall enhancement bond (N–H···O C–H···O). Therefore, balancing solid-state offer a promising strategy fluorescence charge-transfer

Язык: Английский

Процитировано

0

High-Throughput Encapsulated Nanodroplet Screening for Accelerated Co-Crystal Discovery DOI Creative Commons
Jessica P. Metherall, Philip Corner, James F. McCabe

и другие.

Chemical Science, Год журнала: 2025, Номер unknown

Опубликована: Янв. 1, 2025

A high-throughput nanoscale co-crystallisation approach is presented, that combines automation and small scale to enable the exploration of conditions, resulting in 30 new binary, ternary quaternary co-crystals.

Язык: Английский

Процитировано

0

Novel Drug–Drug Cocrystalline Forms of Carbamazepine with Sulfacetamide: Preparation, Characterization, and In Vitro/In Vivo Performance Evaluation DOI Creative Commons
Denis E. Boycov, Ksenia V. Drozd, Alex N. Manin

и другие.

Pharmaceutics, Год журнала: 2025, Номер 17(5), С. 678 - 678

Опубликована: Май 21, 2025

Objectives: Drug–drug cocrystallization represents a promising approach for the development of novel combination drugs with improved physicochemical and biopharmaceutical properties. The aim present research is to prepare drug-drug cocrystalline forms antiepileptic drug carbamazepine (CBZ) sulfacetamide (SCTM). Methods: CBZ cocrystal methanol solvate hydrate were prepared via solvent evaporation technique characterized by single crystal X-ray diffraction, differential scanning calorimetry thermogravimetric analysis. Results: Single-crystal diffraction thermal analysis revealed that multicomponent solids are isostructural, wherein molecule does not play structure-forming role. To optimize synthesis [CBZ+SCTM+H2O] (1:1:0.7), binary ternary phase diagrams constructed in acetonitrile at 25 °C. A thorough investigation behavior aqueous solution showed pH dissolution medium exerted significant effect on stability solubility (1:1:0.7). According diffusion experiments buffer 6.5, an enhanced rate flux CBZ. Pharmacokinetic studies rabbits exhibited comparable bioavailability parent Conclusions: Overall, this work reports preparation hydrate, which can be considered as alternative solid form oral usage, possessing additive pharmacological effect.

Язык: Английский

Процитировано

0

Pharmaceutical Cocrystals for Drug Delivery DOI
Ashwini Nangia

Burger's Medicinal Chemistry and Drug Discovery, Год журнала: 2025, Номер unknown, С. 1 - 62

Опубликована: Май 26, 2025

Abstract Pharmaceutical cocrystals offer the ability to tune solubility, permeability, tableting, and bioavailability of a solid, oral drug formulation without changing chemical structure molecule. Crystal engineering pharmaceutical salts via supramolecular heterosynthons with acceptable generally recognized as safe (GRAS) coformers provides platform technology for improving efficacy optimal delivery. With almost 90% drugs in Biopharmaceutics Classification System (BCS) class II IV suffering from low‐solubility and/or low‐permeability challenges, have provided an opportune intervention populating pipeline over past decade. From prototype cocrystal itraconazole‐succinic acid first salt‐cocrystal complex Entresto containing valsartan‐sacubitril, this review covers origins subject early 2000s peak growth curve model systems between 2005 2015, successful lab‐to‐market translation witnessed The combined application machine learning neural network tools is bringing speed accuracy research exercise designing drug–coformer therapeutic properties. This article snapshot summary latest trends leading discovery, development, continuous manufacturing.

Язык: Английский

Процитировано

0