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. 2020 Dec;27(1):1514-1523.
doi: 10.1080/10717544.2020.1837295.

Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies

Rofida Albash  1 , Yasmina Elmahboub  2 , Kholoud Baraka  3 , Menna M Abdellatif  4 , Ahmed Adel Alaa-Eldin  5
Affiliations

Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies

Rofida Albash et al. Drug Deliv. 2020 Dec.

Abstract

Fenticonazole nitrate (FTN) is a potent antifungal drug adopted in the treatment of vaginal candidiasis. It has inadequate aqueous solubility hence, novel ultra-deformable liposomes 'Terpesomes' (TPs) were developed that might prevail over FTN poor solubility besides TPs might abstain the obstacles of mucus invasion. TPs were assembled by thin-film hydration then optimized by Box Behnken design utilizing terpenes ratio (X1), sodium deoxycholate amount (X2), and ethanol concentration (X3) as independent variable, whereas their impact was inspected for entrapment efficiency (Y1), particle size (Y2), and polydispersity index (Y3). Design Expert® was bestowed to select the optimal TP for more studies. The optimal TP had entrapment efficiency of 62.18 ± 1.39%, particle size of 310.00 ± 8.16 nm, polydispersity index of 0.20 ± 0.10, and zeta potential of -10.19 ± 0.2.00 mV. Elasticity results were greater in the optimal TP related to classical bilosomes. Further, ex vivo permeation illustrated tremendous permeability from the optimal TP correlated to classical bilosomes, and FTN suspension. Besides, in vivo assessment displayed significant inhibition effect in rats from FTN-TPs gel compared to FTN gel. The antifungal potency with undermost histopathological variation was detected in rats treated with FTN-TPs gel. Overall, the acquired findings verified the potency of utilizing FTN-TPs gel for treatment of vaginal candidiasis.

Keywords: Box Behnken design; fenticonazole nitrate; microbiological study; terpesomes; ultra-deformable liposomes; vaginal drug delivery.

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Conflict of interest statement

The authors report no conflict of interest.

Figures

Figure 1.
Figure 1.
Response 3D plots for the effect of terpenes ratio (X1), SDC amount (X2) and ethanol concentration (X3) on (a) EE% and (b) PS. SDC: sodium deoxy cholate; EE%: entrapment efficiency percent and PS: particle size.
Figure 2.
Figure 2.
Contour plots for the effect of terpenes ratio (X1), SDC amount (X2) and ethanol concentration (X3) on (a) EE% and (b) PS. SDC: sodium deoxy cholate; EE%: entrapment efficiency percent and PS: particle size.
Figure 3.
Figure 3.
Morphology of the optimal TP. TP: terpesomes.
Figure 4.
Figure 4.
DSC thermograms of FTN and the optimal TP. FTN: fenticonazole nitrate and TP: terpesomes.
Figure 5.
Figure 5.
Cumulative amount of FTN permeated per unit area from classical bilosomes and the optimal TP relative to FTN suspension. FTN: fenticonazole nitrate; TP: terpesomes.
Figure 6.
Figure 6.
In-vivo study graphical chart of positive control, FTN gel and FTN-TPs gel treated groups. FTN: fenticonazole nitrate and TP: terpesomes.
Figure 7.
Figure 7.
Photomicrographs showing histopathological sections (hematoxylin and eosin stained) of normal control (group I), positive control (group II), rat’s treated with FTN gel (group III) and rat’s treated with FTN-loaded UTPs gel (A) magnification power of 16x and (B) magnification power of 40x. FTN: fenticonazole nitrate; TP: terpesomes.
See this image and copyright information in PMC

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