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. 2018 Sep 10;16(9):324.
doi: 10.3390/md16090324.

Liposomal Form of the Echinochrome-Carrageenan Complex

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Free PMC article

Liposomal Form of the Echinochrome-Carrageenan Complex

Irina M Yermak et al. Mar Drugs. .
Free PMC article

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.

Keywords: carrageenan; echinochrome A; liposomes; mucine; mucoadhesive properties.

Conflict of interest statement

The authors declare no conflict of interest. The funders had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, or in the decision to publish the results.

Figures

Figure 1
Figure 1
Structure of Ech.
Figure 2
Figure 2
Hydrodynamic diameter distribution of (a) liposomes-100 and (b) liposomes-400 stored in apyrogenic water 2 h (black dash line), 24 h (grey line), 80 h (black dot line) and saline solution (black solid line).
Figure 3
Figure 3
Absorption spectra of the Ech extracted with butanol from freshly prepared liposomes (black lines); from freshly prepared lyophilized dried liposomes (red line); from lyophilized dried liposomes after 30 days of storage at 4 °C (blue line).
Figure 4
Figure 4
Scanning electron microscopy images of (a) CRG/ECH liposomes-100, (b) CRG/ECH liposomes-400, (c) mucin, (d) mucin-CRG/ECH liposomes-100 and (e) mucin-CRG/ECH liposomes-400. Mag. = 50.87 KX, EHT = 10.00 kV.
Figure 4
Figure 4
Scanning electron microscopy images of (a) CRG/ECH liposomes-100, (b) CRG/ECH liposomes-400, (c) mucin, (d) mucin-CRG/ECH liposomes-100 and (e) mucin-CRG/ECH liposomes-400. Mag. = 50.87 KX, EHT = 10.00 kV.
Figure 5
Figure 5
Hydrodynamic diameter distribution of (a) CRG/Ech liposomes-100 and (b) CRG/Ech liposomes-400 incubated in a mucin solution (0.15 mg/mL) for 2 h. CRG/Ech liposomes—black dash line, mucin—grey line, CRG/Ech liposomes with mucin—black solid line.
Figure 6
Figure 6
Absorption spectra of the Ech from freshly prepared liposomes (black line) and the liposome solution removed from the inner surface of the small intestine after an hour (red line).

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