Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review
Co-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological activity through non-covalent interactions with one or more co-formers. A “green method” has recently prompted many researchers to develop...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-05-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/11/3279 |
| _version_ | 1797532157644636160 |
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| author | Ilma Nugrahani Maria Anabella Jessica |
| author_facet | Ilma Nugrahani Maria Anabella Jessica |
| author_sort | Ilma Nugrahani |
| collection | DOAJ |
| description | Co-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological activity through non-covalent interactions with one or more co-formers. A “green method” has recently prompted many researchers to develop solvent-free techniques or minimize solvents for arranging the eco-friendlier process of co-crystallization. Researchers have also been looking for less-risk co-formers that produce the desired API’s physicochemical properties. This review purposed to collect the report studies of amino acids as the safe co-former and explored their advantages. Structurally, amino acids are promising co-former candidates as they have functional groups that can form hydrogen bonds and increase stability through zwitterionic moieties, which support strong interactions. The co-crystals and deep eutectic solvent yielded from this natural compound have been proven to improve pharmaceutical performance. For example, <span style="font-variant: small-caps;">l</span>-glutamine could reduce the side effects of mesalamine through an acid-base stabilizing effect in the gastrointestinal fluid. In addition, some amino acids, especially <span style="font-variant: small-caps;">l</span>-proline, enhances API’s solubility and absorption in its natural deep eutectic solvent and co-crystals systems. Moreover, some ionic co-crystals of amino acids have also been designed to increase chiral resolution. Therefore, amino acids are safe potential co-formers, which are suitable for improving the physicochemical properties of API and prospective to be developed further in the dosage formula and solid-state syntheses. |
| first_indexed | 2024-03-10T10:55:08Z |
| format | Article |
| id | doaj.art-f010c546a28844a2bb2c2f9039a5404a |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T10:55:08Z |
| publishDate | 2021-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-f010c546a28844a2bb2c2f9039a5404a2023-11-21T21:56:54ZengMDPI AGMolecules1420-30492021-05-012611327910.3390/molecules26113279Amino Acids as the Potential Co-Former for Co-Crystal Development: A ReviewIlma Nugrahani0Maria Anabella Jessica1Pharmacochemistry Department, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaPharmacochemistry Department, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaCo-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological activity through non-covalent interactions with one or more co-formers. A “green method” has recently prompted many researchers to develop solvent-free techniques or minimize solvents for arranging the eco-friendlier process of co-crystallization. Researchers have also been looking for less-risk co-formers that produce the desired API’s physicochemical properties. This review purposed to collect the report studies of amino acids as the safe co-former and explored their advantages. Structurally, amino acids are promising co-former candidates as they have functional groups that can form hydrogen bonds and increase stability through zwitterionic moieties, which support strong interactions. The co-crystals and deep eutectic solvent yielded from this natural compound have been proven to improve pharmaceutical performance. For example, <span style="font-variant: small-caps;">l</span>-glutamine could reduce the side effects of mesalamine through an acid-base stabilizing effect in the gastrointestinal fluid. In addition, some amino acids, especially <span style="font-variant: small-caps;">l</span>-proline, enhances API’s solubility and absorption in its natural deep eutectic solvent and co-crystals systems. Moreover, some ionic co-crystals of amino acids have also been designed to increase chiral resolution. Therefore, amino acids are safe potential co-formers, which are suitable for improving the physicochemical properties of API and prospective to be developed further in the dosage formula and solid-state syntheses.https://www.mdpi.com/1420-3049/26/11/3279amino acidszwitterionicco-crystalanionic co-crystalionic co-crystalsalt co-crystal |
| spellingShingle | Ilma Nugrahani Maria Anabella Jessica Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review Molecules amino acids zwitterionic co-crystal anionic co-crystal ionic co-crystal salt co-crystal |
| title | Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review |
| title_full | Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review |
| title_fullStr | Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review |
| title_full_unstemmed | Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review |
| title_short | Amino Acids as the Potential Co-Former for Co-Crystal Development: A Review |
| title_sort | amino acids as the potential co former for co crystal development a review |
| topic | amino acids zwitterionic co-crystal anionic co-crystal ionic co-crystal salt co-crystal |
| url | https://www.mdpi.com/1420-3049/26/11/3279 |
| work_keys_str_mv | AT ilmanugrahani aminoacidsasthepotentialcoformerforcocrystaldevelopmentareview AT mariaanabellajessica aminoacidsasthepotentialcoformerforcocrystaldevelopmentareview |