Impact of Hypromellose acetate succinate and Soluplus® on the performance of β-carotene solid dispersions with the aid of sorbitan monolaurate: In vitro-in vivo comparative assessment

Solid dispersions (SDs) possess the potential to enhance the bioavailability of insoluble active pharmaceutical ingredients (APIs) by effectively converting them into amorphous state. However, SDs have a tendency to recrystallize unless appropriate excipients are employed. The objective of this study was to evaluate the ability of hypromellose acetate succinate HF (HPMCAS-HF) and Soluplus® to inhibit the recrystallization of β-carotene and improve its in vivo bioavailability through the fabrication of ternary β-carotene solid dispersions (SDs) with the aid of specific surfactants. Due to rapid micellization, the dissolution profiles of β-carotene SDs based on HPMCAS-HF/Span 20 (5:5, w/w) or Soluplus®/Span 20 (6:4, w/w) combinations exhibited significant improvement, which were almost 7–10 times higher than β-carotene bulk powder.

Highlights

• HPMCAS-HF and Soluplus® were assessed for fabricating ternary β-carotene SDs.
• Introducing Span 20 improved dissolution and bioavailability of the ternary SDs.
• The recrystallization of β-carotene was significantly impeded in the ternary SDs.
• The rapid micellization of the excipients did favor to the dissolution of the SDs.
• HPMCAS-HF/Span 20 combination performed relatively superior.

DSC and PXRD analysis indicated a notable reduction in the crystallinity degree of β-carotene within the SDs. The stability study demonstrated a half-life of β-carotene in the SDs exceeding 30 days. Additionally, the in vivo pharmacokinetics analysis confirmed that the combinations of cellulose derivatives/surfactants significantly enhanced the bioavailability of β-carotene by 1.37-fold and 2.3-fold, respectively. Notably, the HPMCAS-HF/Span 20 combination exhibited superior performance. Consequently, the HPMCAS-HF/Span 20 combination holds potential for the advancement of an effective drug delivery system for β-carotene.

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Yinglan Li, Jie Xu, Qingran Guan, Huaizhen Zhang, Zhuang Ding, Qingpeng Wang, Zhengping Wang, Jun Han, Min Liu, Yanna Zhao, Impact of Hypromellose acetate succinate and Soluplus® on the performance of β-carotene solid dispersions with the aid of sorbitan monolaurate: In vitro-in vivo comparative assessment, International Journal of Biological Macromolecules, 2023, 126639, ISSN 0141-8130, https://doi.org/10.1016/j.ijbiomac.2023.126639.

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