Liposomal Form of the Echinochrome-Carrageenan Complex

Abstract

Inclusion of drugs in liposomes offers the potential for localized and sustained delivery to mucosal surfaces. The inclusion of the carrageenan matrix with echinochrome A ((Ech)—the active substance of the drug Histochrome) in liposomes was studied. According to the spectral characteristics, Ech was not oxidized and retained stability after encapsulation in the liposomes and the lyophilization process. Loading the liposomes with negatively charged polysaccharide results in the increase in the zeta potential to more negative values (from −14.6 to −24.4 mV), that together with an increasing in the sizes of liposomes (from 125.6 ± 2.5 nm to 159.3 ± 5.8 nm) propose of the formation of the polymer coating on liposomes. The interactions of liposomes with porcine stomach mucin was determined by the DLS and SEM methods. The changes in the zeta-potential and size of the mucin particles were observed as the result of the interaction of liposomes with mucin. To evaluate the mucoadhesive properties of liposomes and the penetration of Ech in the mucosa, a fresh-frozen inner surface of the small intestine of a pig as a model of mucous tissue was used. Polysaccharide-coated liposomes exhibit very good mucoadhesive properties −50% of Ech remains on the mucosa.

Implication of Echinochrome A in the Plasticity and Damage of Intestinal Epithelium

“…Previous studies on gastric ulcers have proven the therapeutic effect in an acidic environment [12], but have not fully elucidated the changes in Ech A after exposure. If acid-induced denaturation is specified, advanced drug delivery methods such as liposome encapsulation, should be considered [67,68].…”

Mucoadhesive Marine Polysaccharides

“…To explore the mucoadhesive properties of CRG, porcine stomach mucin, which is similar to the mucin in the epithelium of the gastrointestinal tracts of humans, was used. The interaction between CRGs of different properties (MW, absent/or present AGC) with crude porcine gastric mucin in dilute aqueous solution (at pH 6.5) was studied by DLS, by measuring their surface potential, by turbidity methods and by electron microscopy (SEM and TEM [ 115 , 116 ].…”

“…The changes in ζ-potential values may be used as an indication of mucoadhesive properties of polysaccharides. The ability of CRG to interact with mucin was determined by measuring their surface potential [ 115 , 116 ]. A monomodal ζ-potential distribution was measured for the CRG–mucin mixtures.…”

“…To evaluate the mucoadhesive properties of liposomes and the penetration of Ech on the mucosa, was used a fresh frozen inner surface of the small intestine of a pig as a model of mucous tissue. Liposomes containing CRG/Ech exhibited very good mucoadhesive properties—50% of Ech remained on the mucosa [ 116 ].…”

Antiherpetic Activity of Carrageenan Complex with Echinochrome A and Its Liposomal Form

“…Prescribing liposomes as drug delivery systems for treating infectious diseases and tumors has been well documented [ 24 ]. The incorporation of a hydrophobic Ech into liposomes has been previously shown by us [ 25 ].…”