Akademik Veri Yönetim Sistemi
IV. INTERNATIONAL AGRICULTURAL, BIOLOGICAL &LIFE SCIENCECONFERENCE, Edirne, Türkiye, 22 - 31 Ağustos 2022, ss.197
INTRODUCTION
The respiratory system is in dynamic
contact with the atmosphere until the person's last breath (1). Viral agents
commonly enter the body through the respiratory tract and cause infections. In
studies on respiratory tract infections; influenza A, influenza B, rhinovirus
(RV), respiratory syncytial virus (RSV), coronaviruses are among the viruses
that are frequently encountered as viral agents (2). In this study, it was
aimed to develop antiviral in situ mucoadhesive spray formulations with
protective activity to prevent viruses from causing disease in the body by
settling in the respiratory system through the nasal route. For this purpose,
the broad spectrum potent antiviral “18β-Glycyrrhetinic acid (GA)”, which is
the main active ingredient of licorice root extract, was used in formulations.
METHODS
Various formulations have been prepared using gellan
gum (DGG) which provides in situ gelling, and different mucoadhesive polymers such
as hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (Na-CMC), xanthan gum, Carbopol® 974P NF with biodegradability,
good solubility in water and good release properties.
In
order to determine the proper in situ gel formulation; rheological properties,
mechanical properties, and mucoadhesive strength of the formulations were
investigated. In addition; in vitro
gelling capacity, ex vivo
mucoadhesion strength, water holding capacity, sprayability, and in vitro cytotoxicity were also studied.
RESULTS
As a result, it was concluded that the formulation
containing 0.5% DGG and 0.5% CMC polymers showed optimum properties. This in
situ gel formulation has a clear appearance with uniform sprayability. When it
was mixed with simulated nasal fluid at 34°C, its viscosity increased
significantly to form a clear gel. According to the data of texture profile
analysis, it was determined that it had higher adhesiveness (0.560 mJ) compared
to other formulations. Similarly, in the rheological synergism study performed
with mucin solution, the mucoadhesive strength (9.53 Pa) was found to be higher.
In the ex vivo mucoadhesion test, it
has the highest mucoadhesion strength (19.67 g) after the formulation
containing 0.7% CMC. The formulation containing 0.7% CMC was eliminated due to
improper sprayability pattern. Considering all the criteria, it was decided to
continue further studies with the formulation containing 0.5% DGG + 0.5% CMC
which has the desired properties.
According to the results of in vitro cytotoxicity study with the active substance, it didn't
cause any significant decrease in cell viability at concentrations between 4
and 80 µg/ml. No reduction in cell viability was observed at all tested
concentrations between 4 and 60 µg/ml. A concentration of 80 µg/ml (p < 0.05) slightly reduced cell
viability to 87.90% which is evaluated
as non-toxic according to ISO 10993-5:2009 standard.
CONCLUSION
It is considered that the developed
mucoadhesive in situ gel can provide a great benefit in protecting individuals
from viral infections and can also be a potential product to meet the need for
protection against viral agents. Thus, it will be easier to control the spread
rate of viral infections and contribute to reducing the negative impact.