1. Formulation And Characterization Posaconazole Nanoemulgel by Using Natural Oils For Fungal Infections.
- Author
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Sarvan, Padmaja, Kota, Ranjan, Rajeev, Bharti, Mukund Lata, Bora, Aditya, Meena, Mukesh Kumar, Sharma, Komal, Kar, Nihar Ranjan, and Arora, Ritika
- Subjects
PEANUT oil ,MYCOSES ,DRUG solubility ,SKIN permeability ,ESSENTIAL oils - Abstract
Nanoemulgel (NEG) pharmaceutical formulations are gaining popularity because of their ability to serve both as a nanoemulsion and as a gel. These products are well-known for their ease of use, spreadability, controlled release, and ability to hydrate dry skin. Natural essential oils have been shown to promote the cutaneous permeability of topical formulations, enhancing medication safety and efficacy. Herein, we developed NEG for the enhanced permeation of posaconazole against candidiasis using Mustard oil (Mustard oil-NEG), using the gelling agents carbopol 943 and hydroxypropyl methylcellulose (HPMC). We tested various excipients to increase the solubility of posaconazole and formulate a nanoemulsion (NE). We measured the NE droplet particle size, shape, entrapment efficiency, and drug release. Furthermore, the physicochemical properties of the optimized nanoemulsion formulation were characterized by techniques such as Fourier transform infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) analysis. The NEs were loaded into gels to form NEGs. NEGs were characterized for drug content, homogeneity, rheology, spreadability, and antifungal activity against Candida albicans, both in vitro and in vivo. Optimized posaconazole NEG preparations consisted of either 15% Mustard oil or 20% Arachis oil. Droplet sizes in the optimized NEs were <100 nm, and the polydispersity indexes were 0.24 and 0.26. The percentages of posaconazole released after 24 h from the clove-oil-NEG and eucalyptus-oil-NEGs were 91 ± 4.5 and 89 ± 7%, respectively. Scanning electron microscopy (SEM) showed that the NEGs had a smooth, uniform, and consistent shape and internal structural organization. The drug contents in the clove-oil-NEG and eucalyptus-oil-NEG were 98.5 ± 2.2 and 98.8 ± 3.4%, respectively. Permeation values of posaconazole from clove-oil-NEG and eucalyptus-oil-NEG were 117 ± 7 and 108.34 ± 6 µg cm
-2 , respectively. The posaconazole NEG formulations also had higher levels of fungal growth inhibition than a marketed formulation. Finally, in vivo studies showed that the NEGs do not irritate the skin. Posaconazole NEG with either 15% Mustard oil or 20% Arachis oil is stable with better efficacy than posaconazole alone due to excellent dispersion, drug dissolution, and permeability and thus might be recommended for the effective and safe treatment of candidiasis. [ABSTRACT FROM AUTHOR]- Published
- 2023