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

Area of Science:

• Pharmacology
• Materials Science
• Drug Delivery

Background:

• α-Mangostin (α-M) exhibits diverse biological activities but suffers from poor water solubility.
• Low solubility limits α-M formulation and clinical application due to poor drug distribution and reduced potency.
• Cyclodextrins (CDs) are established excipients for enhancing the solubility of poorly soluble compounds.

Purpose of the Study:

• To enhance the aqueous solubility of α-Mangostin (α-M) through complexation with γ-Cyclodextrin (γ-CD).
• To characterize the inclusion complex formed between α-M and γ-CD.
• To evaluate the potential of the α-M/γ-CD complex for water-based pharmaceutical formulations.

Main Methods:

• Preparation of the α-Mangostin/γ-Cyclodextrin (α-M/γ-CD) inclusion complex using the solubilization method.
• Characterization of the complex using FTIR-Spectrometry, X-ray Diffraction (XRD), and NMR (¹H, ¹³C, HMBC).
• Determination of entrapment efficiency and thermodynamic parameters (Gibbs energy, ΔH) to assess complex formation spontaneity.

Main Results:

• The formation of an inclusion complex between α-M and γ-CD was confirmed through spectroscopic and crystallographic analyses.
• The α-M/γ-CD complex achieved an entrapment efficiency of 84.25%.
• Solubility of α-M was significantly increased by 31.74-fold in the α-M/γ-CD complex compared to free α-M.
• Thermodynamic data indicated spontaneous formation of the inclusion complex.

Conclusions:

• The α-Mangostin/γ-Cyclodextrin (α-M/γ-CD) inclusion complex effectively enhances the water solubility of α-Mangostin.
• The characterized α-M/γ-CD complex demonstrates high entrapment efficiency and spontaneous formation.
• This complex holds significant potential for developing water-based pharmaceutical formulations of α-Mangostin for improved clinical efficacy.