Impact of hypromellose acetate succinate and Soluplus^? on the performance of -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 (R) to inhibit the recrystallization of beta-carotene and improve its in vivo bioavailability through the fabrication of ternary beta-carotene solid dispersions (SDs) with the aid of specific surfactant. Due to rapid micellization, the dissolution profiles of beta-carotene SDs based on HPMCASHF/Span 20 (5:5, w/w) or Soluplus((R))/Span 20 (6:4, w/w) combinations exhibited significant improvement, which were almost 7-10 times higher than beta-carotene bulk powder. DSC and PXRD analysis indicated a notable reduction in the crystallinity degree of beta-carotene within the SDs. The stability study demonstrated a half-life of beta-carotene in the SDs exceeding 30 days. Additionally, the in vivo pharmacokinetics analysis confirmed that the cellulose derivatives/surfactant combinations significantly enhanced the bioavailability of beta-carotene by 1.37fold and 2.3-fold, respectively. Notably, the HPMCAS-HF/Span 20 combination exhibited superior performance. Consequently, the HPMCAS-HF/Span 20 combination held potential for the advancement of an effective drug delivery system for beta-carotene.