Sodium glycocholate (SGC) is a bile salt, which is a biochemical formed by the conjugation of cholic acid with glycine. It contains glycocholate and is white to white creamed powder odorless or practically odorless.
Fig.1 Chemical Structure of SGC.
The researchers have developed a liposomal delivery system containing glycocholate as an enzyme inhibitor and permeation enhancer for oral insulin delivery. rhINS-loaded liposomes containing SGC were prepared by a reversed-phase evaporation method. Transmission electron micrographs revealed a nearly spherical and deformed structure with discernable lamella for sodium glycocholate liposomes. SGC liposomes showed better protection of insulin against enzymatic degradation by pepsin, trypsin, and α-chymotrypsin than liposomes containing the bile salt counterparts of sodium taurocholate (STC) and sodium deoxycholate (SDC). It is concluded that SGC liposomes have the potential for use in the oral delivery of protein and peptide drugs.
Fig.2 Protection of recombinant human insulin from pepsin degradation (A) and trypsin degradation (B) by liposomes with different types of bile salts, ie, SGC, STC, SDC for 4 hours at 37oC. (Niu, 2011)
Recent reports have shown that liposomes containing bile salts can improve the oral and transdermal absorption of drug molecules compared with traditional liposomes. Bile salts used in drug delivery systems mainly include SGC, SDC, and STC, because they are less irritating. Liposomes containing cholesterol or bile salts, including SGC, SDC, and STC, were prepared by the thin-membrane dispersion method. Their particle size and entrapment efficiency were similar. In vitro corneal transport and in vivo corneal uptake experiments suggested that liposomes containing bile salts have better transmembrane permeation ability than those containing cholesterol and can improve the transport of tacrolimus across the cornea by 3-4-fold. Cytotoxicity and in vivo corneal tolerance studies indicated that liposomes containing STC or SGC were well tolerated, whereas those containing SDC were toxic to both SDHCECs and rabbit cornea. Therefore, liposomes containing STC and SGC have low toxicity and great permeability and they are potential carriers for ocular drug delivery systems.
Fig.3 Morphology of tacrolimus-loaded liposomes containing STC (A), SDC (B), or SGC (C), and conventional liposomes (D) by transmission electron microscopy. (Dai, 2013)
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