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      Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications

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          Abstract

          Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation methods, physicochemical properties, and applications. Furthermore, some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients, such as physical stability, chemical stability, mechanical properties, optical properties, bioavailability, sustained release and therapeutic effect. This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications.

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          Pharmaceutical cocrystals is a promising and emerging approach to modulate the performance of pharmaceuticals, including physical stability, chemical stability, mechanical properties, optical properties, release profiles, bioavailability and therapeutic effect.

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          Insoluble drug delivery strategies: review of recent advances and business prospects

          Sandeep Kalepu, Vijaykumar Nekkanti (2015)
          The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been attributed to poor water solubility of the drug. Issues associated with poor solubility can lead to low bioavailability resulting in suboptimal drug delivery. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly water-soluble. With the advent of various insoluble drug delivery technologies, the challenge to formulate poorly water soluble drugs could be achieved. Numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful drug products. Several marketed drugs were reformulated to improve efficacy, safety and patient compliance. In order to gain marketing exclusivity and patent protection for such products, revitalization of poorly soluble drugs using insoluble drug delivery technologies have been successfully adopted by many pharmaceutical companies. This review covers the recent advances in the field of insoluble drug delivery and business prospects.
          Article 0 comments Cited 273 times – based on 0 reviews     Review now
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            A Cocrystal Strategy to Tune the Luminescent Properties of Stilbene-Type Organic Solid-State Materials

            Dongpeng Yan, Amit Delori, Gareth O. Lloyd … (2011)
            Article 0 comments Cited 120 times – based on 0 reviews     Review now
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              Designed biomaterials to mimic the mechanical properties of muscles.

              Sara J. C. Gosline, S. Lv, M. N. Balamurali … (2010)
              The passive elasticity of muscle is largely governed by the I-band part of the giant muscle protein titin, a complex molecular spring composed of a series of individually folded immunoglobulin-like domains as well as largely unstructured unique sequences. These mechanical elements have distinct mechanical properties, and when combined, they provide the desired passive elastic properties of muscle, which are a unique combination of strength, extensibility and resilience. Single-molecule atomic force microscopy (AFM) studies demonstrated that the macroscopic behaviour of titin in intact myofibrils can be reconstituted by combining the mechanical properties of these mechanical elements measured at the single-molecule level. Here we report artificial elastomeric proteins that mimic the molecular architecture of titin through the combination of well-characterized protein domains GB1 and resilin. We show that these artificial elastomeric proteins can be photochemically crosslinked and cast into solid biomaterials. These biomaterials behave as rubber-like materials showing high resilience at low strain and as shock-absorber-like materials at high strain by effectively dissipating energy. These properties are comparable to the passive elastic properties of muscles within the physiological range of sarcomere length and so these materials represent a new muscle-mimetic biomaterial. The mechanical properties of these biomaterials can be fine-tuned by adjusting the composition of the elastomeric proteins, providing the opportunity to develop biomaterials that are mimetic of different types of muscles. We anticipate that these biomaterials will find applications in tissue engineering as scaffold and matrix for artificial muscles.
              Article 0 comments Cited 110 times – based on 0 reviews     Review now
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                Author and article information

                Contributors
                Ting Cai
                Journal
                Journal ID (nlm-ta): Acta Pharm Sin B
                Journal ID (iso-abbrev): Acta Pharm Sin B
                Title: Acta Pharmaceutica Sinica. B
                Publisher: Elsevier
                ISSN (Print): 2211-3835
                ISSN (Electronic): 2211-3843
                Publication date PMC-release: 23 March 2021
                Publication date (Print): August 2021
                Publication date (Electronic): 23 March 2021
                Volume: 11
                Issue: 8
                Pages: 2537-2564
                Affiliations
                [1]State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
                Author notes
                [∗ ]Corresponding author. tcai@ 123456cpu.edu.cn
                Article
                Publisher Item ID: S2211-3835(21)00102-7
                DOI: 10.1016/j.apsb.2021.03.030
                PMC ID: 8424375
                PubMed ID: 34522597
                SO-VID: df471285-ac39-44b4-9e16-c8be11a05081
                Copyright © © 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
                License:

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

                History
                Date received : 10 January 2021
                Date revision received : 22 February 2021
                Date accepted : 10 March 2021
                Categories
                Subject: Review

                Keywords: pharmaceutical cocrystals,cocrystal engineering,physicochemical properties,solid dosage forms,crystallization
                Data availability:
                Keywords: pharmaceutical cocrystals, cocrystal engineering, physicochemical properties, solid dosage forms, crystallization

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