<abstract xmlns="http://www.w3.org/1999/xhtml">

<p>Nystatin is an antifungal agent used for prophylaxis and treatment of candidiasis, especially oral mycosis. Efficacy of nystatin conventional dosage forms is limited by the short residence time and bitter taste of the drug. This research aims at designing an optimized formulation of oral mucoadhesive gel of nystatin-loaded alginate microparticles, which can be retained in the mouth. Sodium alginate solution containing nystatin was added to the solution of calcium chloride under stirring. Microparticles containing nystatin were incorporated into the Carbopol gel. Size, loading, and release profile and mucoadhesion were investigated. The most suitable microparticles with particle size of &lt; 250 μm were prepared with alginate concentration of 1%(w/v), calcium chloride of 1%(w/v), drug:polymer concentration 1%, and ratio of alginate solution:calcium chloride of 1:10. This formulation showed 49.1% drug loading and 98.2% encapsulation efficiency. Carbopol 934 gel provided optimal mucoadhesive properties. Release profile proved a burst release, which can be attributed to the surface associated drug, followed by a slower sustained release phase for all microparticles. The developed system with ability to adhere to the oral mucosa has great appeal for treatment of localized infections and can mask bitter taste of the drug and be retained in the mouth for long periods.</p>
</abstract>

Nystatin is an antifungal agent used for prophylaxis and treatment of candidiasis, especially oral mycosis. Efficacy of nystatin conventional dosage forms is limited by the short residence time and bitter taste of the drug. This research aims at designing an optimized formulation of oral mucoadhesive gel of nystatin-loaded alginate microparticles, which can be retained in the mouth. Sodium alginate solution containing nystatin was added to the solution of calcium chloride under stirring. Microparticles containing nystatin were incorporated into the Carbopol gel. Size, loading, and release profile and mucoadhesion were investigated. The most suitable microparticles with particle size of < 250 μm were prepared with alginate concentration of 1%(w/v), calcium chloride of 1%(w/v), drug:polymer concentration 1%, and ratio of alginate solution:calcium chloride of 1:10. This formulation showed 49.1% drug loading and 98.2% encapsulation efficiency. Carbopol 934 gel provided optimal mucoadhesive properties. Release profile proved a burst release, which can be attributed to the surface associated drug, followed by a slower sustained release phase for all microparticles. The developed system with ability to adhere to the oral mucosa has great appeal for treatment of localized infections and can mask bitter taste of the drug and be retained in the mouth for long periods.

Preparation and evaluation of an oral mucoadhesive gel containing nystatin-loaded alginate microparticles

Research Center for Nanotechnology in Drug Delivery and Department of Pharmaceutics

Department of Quality Control, School of Pharmacy

European Pharmaceutical Journal

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Nystatin is an antifungal agent used for prophylaxis and treatment of candidiasis, especially oral mycosis. Efficacy of nystatin conventional dosage forms is...

Formulation	Adhesion strength (mean ± SD) g/cm²
cp934 gel without alginate particles	1.88 ± 0.04
cp934 gel containing alginate particles	1.94 ± 0.15

Experiment	Alginate (w/v%)	Cacl₂ (w/v%)	Alginate to cacl₂ ratio	drug to polymer ratio	Particle size (μm)
1	1	1	1:10	1:1	<250
2	0.5	1	1:10	1:1	710
3	1	2	1:10	1:1	296
4	1	1	1:5	1:1	450
5	1	1	1:10	1:5	710

Experiments	Alginate solution conc.(w/v%)	CaCl₂ solution conc. (w/v%)	Alginate:CaCl₂ ratio	Drug:polymer ratio

1	1	1	1:5	1:1
2	1	1	1:10	1:1
3	1	2	1:5	1:1
4	1	2	1:10	1:1
5	0.5	1	1:10	1:1
6	0.5	1	1:5	1:1
7	1	1	1:5	1:5
8	1	1	1:5	1:5
9	1	2	1:10	1:5
10	1	2	1:5	1:5
11	0.5	2	1:5	1:5
12	0.5	1	1:5	1:5
13	0.5	1	1:10	1:5
14	0.5	2	1:10	1:1
15	0.5	2	1:5	1:1
16	0.5	2	1:10	1:5

Preparation and evaluation of an oral mucoadhesive gel containing nystatin-loaded alginate microparticles

Article Category: Original Paper

Data publikacji: 11 mar 2021

Zakres stron: 15 - 21

Otrzymano: 27 maj 2019

Przyjęty: 14 sty 2020

DOI: https://doi.org/10.2478/afpuc-2020-0009

Słowa kluczowe
Alginate, Carbopol, Microparticle, Mucoadhesion, Nystatin

© 2020 Mohammadi Samani S. et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Figure 1

Figure 2

Figure 3

Adhesion strength of cp934 gel with and without alginate microparticles (n=6)

Effect of different parameters on size of microparticles

Run parameters for two – level four factorial experimental design

Preparation and evaluation of an oral mucoadhesive gel containing nystatin-loaded alginate microparticles

Article Category: Original Paper

Data publikacji: 11 mar 2021

Zakres stron: 15 - 21

Otrzymano: 27 maj 2019

Przyjęty: 14 sty 2020

DOI: https://doi.org/10.2478/afpuc-2020-0009

Słowa kluczoweAlginate, Carbopol, Microparticle, Mucoadhesion, Nystatin

© 2020 Mohammadi Samani S. et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Figure 1

Figure 2

Figure 3

Adhesion strength of cp934 gel with and without alginate microparticles (n=6)

Effect of different parameters on size of microparticles

Run parameters for two – level four factorial experimental design

Słowa kluczowe
Alginate, Carbopol, Microparticle, Mucoadhesion, Nystatin