Abstract

Aim. The purpose of the work is to determine the bioadhesion indices of vaginal gel with resveratrol and hyaluronic acid, as well as the choice of the type and content of mucoadhesives in the composition. Materials and methods. As research objects samples of gels with different mucoadhesives in the composition were used. Among used mucoadhesives were: sodium alginate (FMC BioPolimer AS, Norway), methyl cellulose (Shin Etsu, Germany), Methocel – methyl cellulose with hydroxypropylmethyl cellulose (Dow Pharmaceutical Sciences, USA), OraRez® W-100L16 – vinyl methyl ether and maleic anhydride copolymer (BOAI, China). As a comparison drug, vaginal gel "Gynodec" (Yuriya-Pharm) was used. During the study, the rate of gel distribution, the degree of deformation under the influence of mechanical forces, the degree of the gel fixation on the surface of the mucosa and the adhesion ability of the samples have been determined. Results. The study has determined that sample No. 2 with sodium alginate has the highest distribution rate, which was 1.56 cm/min. The study of the fixation of samples on the surface of the model of the mucous was performed by the method of flow. The results have showed that the sample with sodium alginate has the closest value to the reference drug. The adhesive ability of samples with different sodium alginate contents was determined. The tensimetric study has found that at a concentration of 0.5 %, the force required to separate the surface is 6158 Pa. Conclusions. On the basis of the complex of physico-chemical studies, bioadhesion indicators of vaginal gel with resveratrol, depending on the type and concentration of mucoadhesives have been determined. According to the distribution parameters on the surface of the genital mucosa model, it has been found that the best properties compared with other types of mucoadhesives has a sample containing sodium alginate. The study by means of a strain gauge has found that the addition of sodium alginate at a concentration of 0.5 % would provide a satisfactory adhesive ability of the vaginal gel.

Highlights

  • Among vaginal dosage forms, gels are widespread, due to the ability to provide prolonged moisturizing action, ease of use and dosage [1]

  • When developing the composition and technology of vaginal gels in addition to rheological characteristics it is important to evaluate the degree of bioadhesion, which determines the possibility of keeping an active pharmaceutical ingredient (API) on the surface of the affected organ by means of interphase forces for a long time [2]

  • If adhesive fixation occurs to the mucous membrane, this process is called mucoadhesion, which determines the time of drug retention on the surface, (2019), «EUREKA: Health Sciences» Number 2 its uniform distribution, the absence of premature evacuation of the administered dose and the completeness of the API release [3, 4]

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Summary

Introduction

Among vaginal dosage forms, gels are widespread, due to the ability to provide prolonged moisturizing action, ease of use and dosage [1]. When developing the composition and technology of vaginal gels in addition to rheological characteristics it is important to evaluate the degree of bioadhesion, which determines the possibility of keeping an active pharmaceutical ingredient (API) on the surface of the affected organ by means of interphase forces for a long time [2]. Interaction with mucins and the possibility of long-term fixation with controlled release of active substances are provided by mucoadhesive substances, as which most often use hydrophilic polymers. They have numerous hydrophilic groups that promote adhesion and cause the swelling of polymers in the fluid and increase the amount of adhesive sites [5, 6]

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