The Realm of Pharmaceutical Multicomponent Forms

A special issue of Crystals (ISSN 2073-4352). This special issue belongs to the section "Biomolecular Crystals".

Deadline for manuscript submissions: closed (30 November 2020) | Viewed by 3435

Special Issue Editors


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Guest Editor
LAQV-REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
Interests: mechanochemistry; deep eutectic solvents; green chemistry; pharmaceutical formulations; crystal engineering; multivariate data analysis
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
1. Centro de Química Estrutural, Institute of Molecular Sciences, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisbon, Portugal
2. Associação do Instituto Superior Técnico para a Investigação e Desenvolvimento (IST-ID), Av. Rovisco Pais 1, 1049-003 Lisbon, Portugal
Interests: mechanochemistry; crystal engineering; supramolecular chemistry; BioMOFs; polymorphs; co-crystals; metallodrugs and metallopharmaceuticals; Antibiotic Coordination Frameworks (ACFs)
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue of Crystals highlights the use of co-crystallization and the development of other multicomponent forms in the pharmaceutical context, as a tool to improve drug properties and consequently tackle specific drug problems.

Co-crystallization is a crystal engineering approach in which a drug is combined to one or more coformers by non-covalent interactions with the intention of tuning drugs’ properties, such as solubility, bioavailability, stability, and mechanical properties, among others. The coformers should be molecules considered safe for pharmaceutical applications or even other drugs. Nevertheless, in addition to co-crystals, also other multicomponent forms, such as solvates, ionic co-crystals, molecular salts, eutectic mixtures, and even co-amorphous materials, can be synthesized, leading to significant improvements in drug properties.

During the development process, it is important to bear in mind that industry in general, and the pharmaceutical industry in particular, is changing the way of producing new materials, using more sustainable methods with less toxic materials. Solvent-free synthetic methods are being investigated, and the paradigm of batch manufacturing is changing to continuous manufacturing, decreasing the amount of residues and increasing energetic efficiency.

The aim of this Special Issue is to show how different multicomponent forms can improve drug properties and how they can be transposed to industrial settings. Therefore, works related to the development of all the abovementioned multicomponent forms are welcome in this Special Issue. Additionally, industrial applications of sustainable and greener co-crystallization methods are encouraged.

Dr. Mafalda Cruz Sarraguça
Dr. Vânia André
Guest Editors

Manuscript Submission Information

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Keywords

  • Co-crystallization
  • Co-crystals
  • Ionic co-crystals
  • Molecular salts
  • Eutectic mixtures
  • Co-amorphous
  • Industrial applications
  • Sustainability

Published Papers (1 paper)

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Research

18 pages, 3348 KiB  
Article
Top-Down Synthesis of a Lamivudine-Zidovudine Nano Co-Crystal
by Bwalya A. Witika, Vincent J. Smith and Roderick B. Walker
Crystals 2021, 11(1), 33; https://doi.org/10.3390/cryst11010033 - 30 Dec 2020
Cited by 13 | Viewed by 2920
Abstract
Lamivudine (3TC) and zidovudine (AZT) are antiretroviral agents used to manage HIV/AIDS infection. A wet media milling top-down approach was used to develop and produce nano co-crystals of 3TC and AZT. Micro co-crystals were prepared by solvent evaporation and subsequently milled in the [...] Read more.
Lamivudine (3TC) and zidovudine (AZT) are antiretroviral agents used to manage HIV/AIDS infection. A wet media milling top-down approach was used to develop and produce nano co-crystals of 3TC and AZT. Micro co-crystals were prepared by solvent evaporation and subsequently milled in the presence of two surfactants, viz., sodium lauryl sulfate (SLS) and α-tocopheryl polyethylene glycol succinate 1000 (TPGS 1000). Optimisation was undertaken using design of experiments (DoE) and response surface methodology (RSM) to establish and identify parameters that may affect the manufacturing of nano co-crystals. The impact of SLS and TPGS 1000 concentration, milling time, and number of units of milling medium on the manufacturing of nano co-crystals, was investigated. The critical quality attributes (CQA) monitored were particle size (PS), Zeta potential (ZP), and polydispersity index (PDI). Powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, transmission electron microscopy, energy dispersive X-ray spectroscopy scanning electron microscopy, and cytotoxicity assays were used for additional characterization of the optimised nano co-crystal. The mean PS, PDI, and ZP of the optimised top-down nanocrystal were 271.0 ± 92.0 nm, 0.467 ± 0.073, and −41.9 ± 3.94 mV, respectively. In conclusion, a simple, inexpensive, rapid, and precise method of nano co-crystal manufacturing was developed, validated, and optimised using DoE and RSM, and the final product exhibited the target CQA. Full article
(This article belongs to the Special Issue The Realm of Pharmaceutical Multicomponent Forms)
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