A Review on Co-crystals of Herbal Bioactives for Solubility Enhancement: Preparation Methods and Characterization Techniques

Abstract

Co-crystallization is a promising approach for improving physical and pharmacological properties of API, viz., solubility, dissolution rate, stability, hygroscopicity, tablet ability, mechanical properties, bioavailability, and therapeutic efficacy. Different methods for the preparation of pharmaceutical co-crystals have been discussed. Instrumental and physicochemical characterization methods have also been included. Herbal bioactives are potential candidates for co-crystallization to improve solubility, mask taste, and improve bioavailability. Literature on the development of co-crystals of herbal bioactives like curcumin, quercetin, berberine, resveratrol, naringenin, and miscellaneous herbal compounds has been reported systematically in the present review. In conclusion, co-crystallization of herbal bioactives is a promising method for enhancing their physical properties. However, toxicological, stability, regulatory, and scaleup issues must be adequately addressed before commercial viability can be expected.

Spiers Memorial Lecture: Mechanochemistry, tribochemistry, mechanical alloying – retrospect, achievements and challenges

“…Formation of co-crystals is considered also as synthesis, namely a supramolecular synthesis based on the rearrangement of intermolecular, not covalent bonds. 194–206 Mechanochemical synthesis of co-crystals of organic compounds (in particular, of pharmaceutical compounds with coformers) is quite often the method of choice as compared to a thermal route (co-melting), or a co-crystallization from solution (when solubilities of components are very different, what is usually the case). Very often mechanical treatment gives solid dispersions and mechanocomposites.…”

New cocrystals of heterocyclic drugs: structural, antileishmanial, larvicidal and urease inhibition studies

“…To alter the physiochemical properties of drugs, as well as to create supramolecular structures, cocrystallization is a benchmark strategy (Essa et al, 2019;Bhowal et al, 2019). The key features of cocrystallization are the small organic molecule (coformer), combined with bioactive compounds, usually active pharmaceutical ingredients (APIs) (Rathi et al, 2022;Wisudyaningsih et al, 2019;Ancheria et al, 2019;Tanabe et al, 2019). The resulting product (cocrystal) may differ in physical and chemical properties compared to the API.…”

Enhancing the dissolution and bacteriostatic activity of trimethoprim through salt formation

“…Various techniques have been used to increase drug solubility, such as adding solubilizers, 13,14 nanocrystal technology, 15,16 solid dispersion, [17][18][19] inclusion technology, 20 microemulsion technology, etc. 21,22 Co-crystallization is a promising approach to improve the physical and pharmacological properties of the API, 23 such as solubility, 24,25 stability, 26 hygroscopicity, 27 tablet ability, 28 bioavailability, 29 and therapeutic efficacy. 30 Some co-crystals/ salts of TMP have been reported.…”