Alginate Oligosaccharides Affect Mechanical Properties and Antifungal Activity of Alginate Buccal Films with Posaconazole.

Marta Szekalska,Magdalena Wróblewska,Katarzyna Winnicka,Monika Trofimiuk,Anna Basa

doi:10.3390/md17120692

Marta Szekalska, Magdalena Wróblewska + Show 3 more

Open Access

https://doi.org/10.3390/md17120692

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Abstract

Sodium alginate and its oligosaccharides through potential antifungal properties might improve the activity of antifungal drugs enhancing their efficacy and potentially reducing the frequency of application. Mucoadhesive buccal films are oral dosage forms designed for maintaining both local or systemic drug effects and seem to be a very promising alternative to conventional oral formulations. Hence, in this study, mucoadhesive buccal films based on the alginate and its oligosaccharide oligomer composed predominantly of mannuronic acid for the administration of posaconazole-antifungal drug from the azole group were developed. As the polymer gelation method, a relatively new freeze-thaw technique was chosen. All prepared formulations were examined for pharmaceutical tests, swelling, mechanical, and mucoadhesive properties. In addition, the influence of sodium alginate (ALG) and alginate oligosaccharides (OLG) on POS antifungal activity on Candida species was performed. It was observed that film formulation containing 1% ALG and 1% OLG (F2) was characterized by optimal mucoadhesive and swelling properties and prolonged drug release up to 5 h. Additionally, it was shown that OLG affected the growth reduction of all tested Candida spp. The obtained data has opened the way for future research for developing OLG-based dosage forms, which might increase the activity of antifungal drugs.

Highlights

Fungal infections, despite the constant progress of medicine, still constitute a valid therapeutic problem
The obtained data has opened the way for future research for developing OLG-based dosage forms, which might increase the activity of antifungal drugs
The data antibacterial obtained in our study suggested that both enhancing the activity of selected antibiotics

Summary

Introduction

Despite the constant progress of medicine, still constitute a valid therapeutic problem. One of the most common opportunistic fungal infections is candidiasis, which is generally caused by Candida species. Candida is a genus of yeast belonging to the normal, commensal microbiota of the gastrointestinal tract, vagina, skin, oral cavity, or other mucosal surfaces in healthy humans. In the case of patients critically ill, with immunodeficiency or AIDS, patients that use total parenteral nutrition after transplantation and treated by cytotoxic chemotherapies or broad-spectrum antibiotics, Candida spp. might contribute to systemic infection. The genus Candida consists of various species, predominant etiological agents of human infection are Candida albicans, Candida parapsilosis, Candida tropicalis, and Candida krusei. Candida albicans causes oral candidiasis – one of the most common opportunistic fungal infections, where local drug dosage forms are effective, especially buccal films. While a wide range of available antifungal substances can be used for effective treatment

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