化学
硫醇
兰瑞肽
SN2反应
谷胱甘肽
立体化学
生物化学
激素
酶
肢端肥大症
生长激素
作者
Munazza Ijaz,Sonja Bonengel,Ožbej Zupančič,Muhammad Yaqoob,Markus Hartl,Shah Hussain,Christian W. Huck,Andreas Bernkop‐Schnürch
标识
DOI:10.1517/17425247.2016.1167034
摘要
To develop a self nano-emulsifying delivery system (SNEDS) for model peptide lanreotide providing a protective effect towards thiol-disulfide exchange reactions.Ion-paired complexes of lanreotide with surfactants were prepared. In the following, Log P (octanol/water) of these complexes was determined. Lanreotide-loaded SNEDS (Lan/Deo-SN2 and Lan/Deo-SN3) were characterized for payload, droplet size and zeta potential. Lan/Deo-SN2 and Lan/Deo-SN3 were incubated with reduced glutathione (GSH) and thiol-enriched casein peptones for the assessment of thiol-disulfide exchange reactions. Ultra-centrifugation was used for separation of lanreotide released from SNEDS.A maximum payload of 6.4% was achieved for Lan/Deo-SN2. Mean droplet size of Lan/Deo-SN2 and Lan/Deo-SN3 was 45 ± 0.20 nm and 37 ± 0.02 nm, respectively. Both formulations showed significant protection towards thiol-disulfide exchange reactions. After 3 h of incubation with GSH, 48% and 80% of lanreotide remained intact when incorporated in Lan/Deo-SN2 and Lan/Deo-SN3, respectively. Furthermore, Lan/Deo-SN2 and Lan/Deo-SN3 showed 47% and 51% protection against thiol enriched casein peptones, respectively. Both formulations showed sustained lanreotide release over a period of 3 h.Owing to the results, the above-mentioned approach might be a useful tool to overcome the sulfhydryl barrier of the GI-tract.
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