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

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Harloff-Helleberg , S , Fliervoet , L A L , Fano , M , Schmitt , M , Antopolski , M , Urtti , A & Nielsen , H M 2019 , ' Exploring the mucoadhesive behavior of sucrose acetate isobutyrate : a novel excipient for oral delivery of biopharmaceuticals ' , Drug Delivery , vol. 26 , no. 1 , pp. 532-541 . https://doi.org/10.1080/10717544.2019.1606866

Title: Exploring the mucoadhesive behavior of sucrose acetate isobutyrate : a novel excipient for oral delivery of biopharmaceuticals
Author: Harloff-Helleberg, Stine; Fliervoet, Lies A. L.; Fano, Mathias; Schmitt, Mechthild; Antopolski, Maxim; Urtti, Arto; Nielsen, Hanne Morck
Contributor: University of Helsinki, Division of Pharmaceutical Biosciences
University of Helsinki, Drug Research Program
Date: 2019-01-01
Language: eng
Number of pages: 10
Belongs to series: Drug Delivery
ISSN: 1071-7544
URI: http://hdl.handle.net/10138/302511
Abstract: Oral drug delivery is an attractive noninvasive alternative to injectables. However, oral delivery of biopharmaceuticals is highly challenging due to low stability during transit in the gastrointestinal tract (GIT), resulting in low systemic bioavailability. Thus, novel formulation strategies are essential to overcome this challenge. An interesting approach is increasing retention in the GIT by utilizing mucoadhesive biomaterials as excipients. Here, we explored the potential of the GRAS excipient sucrose acetate isobutyrate (SAIB) to obtain mucoadhesion in vivo. Mucoadhesive properties of a 90% SAIB/10% EtOH (w/w) drug delivery system (DDS) were assessed using a biosimilar mucus model and evaluation of rheological behavior after immersion in biosimilar intestinal fluid. To ease readability of this manuscript, we will refer to this as SAIB DDS. The effect of SAIB DDS on cell viability and epithelial membrane integrity was tested in vitro prior to in vivo studies that were conducted using SPECT/CT imaging in rats. When combining SAIB DDS with biosimilar mucus, increased viscosity was observed due to secondary interactions between biosimilar mucus and sucrose ester predicting considerable mucoadhesion. Mucoadhesion was confirmed in vivo, as radiolabeled insulin entrapped in SAIB DDS, remained in the small intestine for up to 22 h after administration. Moreover, the integrity of the system was investigated using the dynamic gastric model under conditions simulating the chemical composition of stomach fluid and physical shear stress in the antrum under fasted conditions. In conclusion, SAIB is an interesting and safe biomaterial to promote high mucoadhesion in the GIT after oral administration.
Subject: Sucrose acetate isobutyrate
mucoadhesion
rheology
in vivo SPECT
CT
dynamic gastric model
biopharmaceuticals
oral drug delivery
insulin
Caco-2 cells
IN-VITRO MODELS
DRUG-DELIVERY
RHEOLOGICAL EVALUATION
VIVO EVALUATION
SYSTEM
SAIB
NANOPARTICLES
FORMULATION
METABOLISM
MIXTURES
317 Pharmacy
116 Chemical sciences
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