Artemisinin hydroxypropyl-β-cyclodextrin inclusion complex loaded with porous starch for enhanced bioavailability

Many fat-soluble drugs face challenges in oral bioavailability due to poor water solubility. Existing solutions often fail to balance solubility and stability. Prior research has shown that cyclodextrin inclusion complexes can improve drug solubility. However, no prior work had resolved how to effectively load these complexes into a porous matrix. This gap motivated the exploration of porous starch as a carrier. The need to enhance Artemisinin's solubility remains a key challenge. No prior work had tested this specific combination of cyclodextrin and porous starch. The current study addresses this limitation. It provides new insights into drug delivery for water-insoluble compounds.

The primary aim was to improve Artemisinin's bioavailability by forming an inclusion complex with hydroxypropyl-β-cyclodextrin. The study focused on optimizing drug loading and entrapment efficiency. The researchers sought to evaluate the physicochemical properties of the complex. They also aimed to assess antimalarial activity in vitro and in vivo. The motivation stemmed from Artemisinin's poor solubility and limited bioavailability. The study tested whether porous starch could serve as an effective carrier. The goal was to compare the new formulation with existing drug products. The findings aim to inform future drug delivery strategies.

The study used hydroxypropyl-β-cyclodextrin to form an inclusion complex with Artemisinin. The complex was then loaded into porous starch using hydrogen bonding. Optimization of preparation conditions focused on drug loading and entrapment efficiency. Optical and thermodynamic methods characterized the complex's properties. The researchers measured solubility and bioavailability at 48 hours. In vitro and in vivo antimalarial activity were tested. Comparative analysis included market ART piperaquine tablets. The study evaluated physicochemical properties of the final formulation.

The maximum drug loading of the AHPS formulation reached 16.51%. Entrapment efficiency was measured at 67.26%. The complex showed improved solubility compared to pure Artemisinin. Bioavailability at 48 hours was higher than in the market formulation. In vitro antimalarial activity was enhanced in the AHPS formulation. In vivo results confirmed better activity than the standard drug product. Hydrogen bonding was confirmed as the main interaction mechanism. The porous starch matrix effectively retained the inclusion complex.

The AHPS formulation demonstrated improved solubility and bioavailability compared to Artemisinin alone. The inclusion complex with hydroxypropyl-β-cyclodextrin enhanced drug loading. Porous starch served as an effective carrier for the complex. The study showed better antimalarial activity in both in vitro and in vivo models. The findings suggest a new approach for fat-soluble drug delivery. The researchers propose that this method could be applied to other poorly soluble drugs. The formulation's properties align with the authors' stated goals. The study supports the potential of this delivery system for clinical use.