Delivery of radix ophiopogonis polysaccharide via sucrose acetate isobutyrate-based in situ forming systems alone or combined with its mono-PEGylation

Abstract

This work aimed to achieve long-lasting delivery of radix ophiopogonis polysaccharide (ROP) by sucrose acetate isobutyrate (SAIB)-based in situ forming systems (ISFSs) alone or combined with mono-PEGylation of ROP. When the ‘90%SAIB/10% solvent’ system was used, the mean residence time (MRT) of ROP was prolonged by 4.3 5 ∼ 7.00 times and the initial release rate was reduced significantly. However, this system was only suitable for days-long sustained release of ROP in short-term therapy. As to the ‘SAIB/additives/solvent’ system containing mono-PEGylated ROP, the results indicated that SAIB/poly(d,l-lactide-co-glycolide) (PLGA)/N-methyl-2-pyrrolidone (NMP) was superior to SAIB/polylactic acid (PLA)/NMP and SAIB/PLA/ethanol in controlled release. Moreover, weeks- to months-long (16–60 d) smooth release of ROP could be achieved by varying the concentration (10–30%) and molecular weight (MW) of PLGA (10–50 kDa) or by employing a moderate MW of PEGylated ROP (∼20 or ∼30 kDa). With further increasing the conjugate MW to ∼40 kDa, the contribution of drug elimination to its plasma retention seemed to surpass that of the SAIB-based system, resulting in that the system no longer had an obvious influence on the in vivo behavior of the conjugate. Besides, the results of host response confirmed that with less solvent being used, the SAIB-based systems showed a higher biocompatibility than the PLGA-based systems, suggesting that they could be freely chosen in the prevention and/or cure of chronic diseases.

Electrosprayed minocycline hydrochloride-loaded microsphere/SAIB hybrid depot for periodontitis treatment

“…Among the available sustained-release delivery systems, sucrose acetate isobutyrate (SAIB) is one of the most prospective systems with biodegradability and injectability, and it is usually considered safe by the U.S. Food and Drug Administration (FDA) (Wang et al., 2018 ; Harloff-Helleberg et al., 2019 ). Furthermore, the viscosity of the SAIB can be dramatically reduced when mixing with a little amount of solvent, for example, ethanol, allowing the SAIB to be easily inject using small needles.…”

“…Furthermore, the viscosity of the SAIB can be dramatically reduced when mixing with a little amount of solvent, for example, ethanol, allowing the SAIB to be easily inject using small needles. Upon injection, the solvent diffuses from the depot into body fluid, resulting in a highly viscous SAIB depot from where the drug can be released in a sustained manner (Wang et al., 2018 ; Harloff-Helleberg et al., 2019 ; Yang et al., 2019 ). However, burst release still existed in the application of SAIB (Park & Lee, 2009 ).…”

Effect of microsphere size on the drug release and experimental characterization of an electrospun naringin‐loaded microsphere/sucrose acetate isobutyrate (SAIB) depot

“…Sucrose acetate isobutyrate (SAIB), a highly hydrophobic, water‐insoluble and fully esterified sucrose derivative, has been used to form SAIB‐based depots for long‐term drug release over periods ranging from a few days to 3 months . With the assistance of a small amount of organic solvent (eg, approximately 10%‐15% ethanol), SAIB‐based depots become viscous and injectable depots that can be used to deliver various drugs, including small molecules and biomacromolecules. SAIB is generally regarded as safe (GRAS) by the Food and Drug Administration (FDA) .…”

Exploring the mucoadhesive behavior of sucrose acetate isobutyrate: a novel excipient for oral delivery of biopharmaceuticals

“…SAIB is a sucrose derivative, obtained by full esterification of sucrose with acetate and isobutyrate groups, and it is generally regarded as safe (GRAS) by the U.S. Food and Drug Administration (FDA) (U.S. Food and Drug Administration, 2018). Interestingly, the potential of using SAIB has been studied in injectable drug delivery systems (DDSs) for small molecules (Lee et al., 2006; Lu et al., 2008; Wang et al., 2018). In those studies, SAIB was used to form a water insoluble, yet biodegradable, matrix when mixed with 10% ethanol resulting in a matrix from where the investigated drugs were released in a sustained manner.…”