α-Mangostin/γ-Cyclodextrin Inclusion Complex: Formation and Thermodynamic Study

Abstract

α-Mangostin (α-M) has various biological activities, such as anti-cancer, antibacterial, anti-fungal, anti-tyrosin, anti-tuberculosis, anti-inflammatory, and antioxidant. However, it has very low solubility in water. The formulation of this compound requires high amounts of solubilizers, which limits its clinical application. In addition, its low solubility in water is a barrier to the distribution of this drug, thus affecting its potency. Cyclodextrin (CD) is widely used as a solubility enhancer of poorly soluble drugs. This study aimed to increase the solubility of α-M in water through complex formation with CD. The complex of α-Mangostin and γ-Cyclodextrin (α-M/γ-CD CX) was prepared by the solubilization method, resulting in a solubility improvement of α-M in water. Characterization of α-M/γ-CD CX by using FTIR-Spectrometry, XRD, H-, C-, and HMBC-NMR showed that α-M was able to form an inclusion complex with γ-CD. The complex yielded an entrapment efficiency of 84.25 and the thermodynamic study showed that the α-M/γ-CD CX was formed spontaneously, based on the negative values of Gibbs energy and ΔH. Interestingly, the solubility of α-M/γ-CD CX significantly increased by 31.74-fold compared with α-M. These results suggest that α-M/γ-CD CX has the potential in the formulation of water-based preparation for clinical applications.

Potency of Xanthone Derivatives from Garcinia mangostana L. for COVID-19 Treatment through Angiotensin-Converting Enzyme 2 and Main Protease Blockade: A Computational Study

“…However, the potential of α-mangostin tends to be hindered due to its unfavorable physicochemical properties. Its low solubility in water makes it difficult to formulate into drug preparations, especially for oral administration, which is commonly preferred by patients [ 28 , 29 ]. Interestingly, the potential of other isolated xanthone derivative compounds from the pericarp of Garcinia mangostana L. has not been further explored for their potency in combating SARS-CoV-2 and their compatibility to be formulated as oral drug preparations.…”

Studies of the Formation and Stability of Ezetimibe-Cyclodextrin Inclusion Complexes

“…The molecule, included in the complex, is protected by the macromolecule against a harmful influence of varied external factors such as high temperature or UV radiation [ 20 , 21 ]. Cyclodextrins can be successfully used in complexing medicines [ 22 , 23 ] and other biologically active compounds [ 24 ]. Song et al showed that cyclodextrins can also be used to remove organic micropollutants from water [ 25 ].…”