Encapsulation of astaxanthin in OSA-starch based amorphous solid dispersions with HPMCAS-HF/Soluplus® as effective recrystallization inhibitor

In this study, the interaction among multifunctional excipients, including polysaccharides, cellulose derivatives, and surfactants, was particularly investigated, together with its impact on the physicochemical properties of astaxanthin amorphous solid dispersions (ASTX ASDs). It was indicated that Span 20 could rapidly form hemimicelles or aggregates in the presence of hypromellose acetate succinate HF (HPMCAS-HF, HF) or Soluplus®, while octenyl succinic anhydride modified starch (OSA-starch) efficiently assisted in the coalescence inhibition of drug-excipients aggregates, which was jointly beneficial to the recrystallization inhibition of amorphous ASTX.

Highlights

• Span 20 could form hemimicelles or aggregates in the presence of HF or SOL.
• OSA-starch assisted coalescence inhibition of ASTX-HF/SOL-Span 20 hemimicelles.
• The dissolution of ASTX ASDs in different media revealed significant promotion.
• The oral bioavailability of ASTX ASDs enhanced significantly as well.
• HF coordinated relatively superior with OSA-starch.

ASTX ASDs were further prepared with OSA-starch, HPMCAS-HF/Soluplus®, and Span 20 as the wall materials. DSC, SEM, and XRD confirmed that crystalline ASTX had transformed to amorphous state in the ASDs, while FT-IR spectra provided evidence suggesting the existence of hydrogen bonds and hydrophobic interaction between ASTX and the excipients. The dissolution of ASTX ASDs in different media revealed significant promotion, while the pharmacokinetic results further demonstrated the oral bioavailability of ASTX ASDs enhanced remarkably, exhibiting 2.75-fold (SD₁) and 1.87-fold (SD₂) increase, respectively, compared to ASTX bulk powder.

In summary, the cellulose derivatives-surfactant interaction had great impact on the physicochemical properties of ASTX ASDs, and their combinations exhibited great potential for delivering the hydrophobic bioactive compounds efficiently.

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Materials

Astaxanthin (ASTX) (>96 % purity), chitosan quaternary ammonium salt (abbreviated as chitosan), and β-cyclodextrin were purchased from Macklin Biochemical Technology Co., LTD (Shanghai, China). Octenyl succinic acid modified starch (OSA-starch) (Hi-Cap® 100) was provided by Ingredion Incorporated (Bridgewater, NJ, USA). Inulin was purchased from Yuanye Biotechnology Co., Ltd. (Shanghai, China). Hypromellose acetate succinate (HPMCAS) HF was provided by Ashland (Kentucky, USA). Soluplus was provided by BASF.

Yinglan Li, Qipeng Wei, Jianshuo Su, Huaizhen Zhang, Zhiping Fan, Zhuang Ding, Min Wen, Min Liu, Yanna Zhao,
Encapsulation of astaxanthin in OSA-starch based amorphous solid dispersions with HPMCAS-HF/Soluplus® as effective recrystallization inhibitor, International Journal of Biological Macromolecules, Volume 279, Part 1, 2024, 135421, ISSN 0141-8130, https://doi.org/10.1016/j.ijbiomac.2024.135421.

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