Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity

Abstract

The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box–Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly (p < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant (p < 0.05) enhanced antifungal activity against C. albicans and A. niger. The findings of the study revealed that BS is an important drug delivery system for transdermal delivery.

Preparation, Characterization, and Evaluation of Curcumin–Graphene Oxide Complex-Loaded Liposomes against Staphylococcus aureus in Topical Disease

“…Moreover, the sustained drug release was observed after 10 h up to 24 h. In the first 6 h of the in vitro drug release, as shown in Figure , slower drug release from complex-loaded liposomes over the CUR-loaded liposomes was observed, and it may be attributed to the complex formation that may cause slower drug release. Furthermore, it is supported with the published literature. , The in vitro drug release kinetics on multiple models were investigated, and it was observed that the first-order model ( R 2 = 0.9991) was the best fit for CUR-GO-loaded liposomes (shown in Table ). The drug release model revealed that the drug release exponent occurred because of the non-Fickian diffusion process, which is often observed to be n > 0.5 and is fitted into the first order .…”

“…Furthermore, it is supported with the published literature. 27 , 31 The in vitro drug release kinetics on multiple models were investigated, and it was observed that the first-order model ( R 2 = 0.9991) was the best fit for CUR-GO-loaded liposomes (shown in Table 2 ). The drug release model revealed that the drug release exponent occurred because of the non-Fickian diffusion process, which is often observed to be n > 0.5 and is fitted into the first order.…”

“…Kinetic models for in vitro drug release data were fit using zero-order, first-order Higuchi, Hixon–Crowell, and Korsemeyer models. These data were put through regression analysis . According to these equations, the graphs of the relevant models were drawn.…”

“…According to these equations, the graphs of the relevant models were drawn. There is a formula for each drug release model listed below . Using fundamental diffusion law correlations, Higuchi sought to establish a link between the drug release rate and the underlying physical constants.…”

“…These data were put through regression analysis. 27 According to these equations, the graphs of the relevant models were drawn. There is a formula for each drug release model listed below.…”