The Spray-Dried Alginate/Gelatin Microparticles with Luliconazole as Mucoadhesive Drug Delivery System

Candida species are opportunistic fungi, which are primary causative agents of vulvovaginal candidiasis. The cure of candidiasis is difficult, lengthy, and associated with the fungi resistivity. Therefore, the research for novel active substances and unconventional drug delivery systems providing effective and safe treatment is still an active subject. Microparticles, as multicompartment dosage forms due to larger areas, provide short passage of drug diffusion, which might improve drug therapeutic efficiency. Sodium alginate is a natural polymer from a polysaccharide group, possessing swelling, mucoadhesive, and gelling properties. Gelatin A is a natural high-molecular-weight polypeptide obtained from porcine collagen. The purpose of this study was to prepare microparticles by the spray-drying of alginate/gelatin polyelectrolyte complex mixture, with a novel antifungal drug-luliconazole. In the next stage of research, the effect of gelatin presence on pharmaceutical properties of designed formulations was assessed. Interrelations among polymers were evaluated with thermal analysis and Fourier transform infrared spectroscopy. A valid aspect of this research was the in vitro antifungal activity estimation of designed microparticles using Candida species: C. albicans, C. krusei, and C. parapsilosis. It was shown that the gelatin addition affected the particles size, improved encapsulation efficiency and mucoadhesiveness, and prolonged the drug release. Moreover, gelatin addition to the formulations improved the antifungal effect against Candida species.

Automated summary

Candida species are the main causative agents of vulvovaginal candidiasis, which is difficult to cure and associated with fungal resistivity. Microparticles with larger surface area can provide short drug diffusion passage, potentially improving therapeutic efficiency. Sodium alginate, a natural polymer, possesses swelling, mucoadhesive, and gelling properties, while gelatin A, a natural polypeptide, has a high molecular weight. This study prepared microparticles using a mixture of alginate/gelatin polyelectrolyte complex and a novel antifungal drug-luliconazole. The addition of gelatin improved the particle size, encapsulation efficiency, mucoadhesiveness, drug release, and antifungal effect against Candida species.