Vitamin E TPGS based nanogel for the skin targeting of high molecular weight anti-fungal drug: development and in vitro and in vivo assessment

Abstract

The molecules having molecular weight greater than 500 Da are considered to be ineffective in the treatment of skin diseases due to their low skin permeation. The present study entails the development of Vitamin E TPGS nanoemulsion based nanogel formulation of high molecular weight drug, Amphotericin B (AmB 923 Da), intended for effective treatment of cutaneous fungal infections. The nanoemulsion formulations were prepared in strength similar to the marketed topical formulation and optimized with respect to S mix ratio (surfactant: co-surfactant), type of surfactant, co-surfactant, globule size, size distribution, percent transmittance, dispersibility, viscosity and rheology. The optimized nanoemulsion formulation was further incorporated in gel base to form AmB nanogel formulation. As compared to marketed topical formulation, the optimized nanogel exhibited 3.9 fold higher skin deposition through porcine ear skin. Confocal laser scanning microscopy study (CLSM) showed the specific distribution of AmB in different parts of the skin and confirmed the permeation of nanogel to the deeper layers of the skin. The antifungal activity of optimized nanogel formulation tested using microdilution method was found to be 2.0 fold higher against Aspergillus niger and Candida albicans in contrast to marketed formulation. The results depicted that the prepared nanogel formulation is a better alternative for effective topical delivery of AmB.

Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell

“…Carbopol 934 was selected as a carrier base for NDLs due to its excellent bio-adhesive properties, nonirritant nature, ability to form pharmaceutically elegant gels, and better storage stability (Kaur et al., 2015 ). The gel formulation exhibited neutral pH, considered ideal for topical application without having possibility of skin irritation, and had high drug content (92.13 ± 4.12%).…”

“…The flow curve was achieved by plotting shear speed against respective viscosity ( Supplemental Figure S3(d) ). The analysis of rheogram revealed a non-Newtonian pseudo-plastic flow pattern which is desirable for topical applications as it covers a maximum skin area (Kaur et al., 2015 ).…”

Recent Advances in the Application of Vitamin E TPGS for Drug Delivery

“…The nanogels exhibited 3.9-fold higher skin deposition through porcine ear skin and 2.0-fold higher antifungal activity against Aspergillus niger and Candida albicans compared with the marketed topical formulation. The nanogels can penetrate into the deeper layers of skin 157 . A topical formulation of griseofulvin, an antifungal agent, was prepared in the Carbopol (980 NF) base with the combination of TPGS as the penetration enhancer.…”

Role of Nanoemulsion for Safe and Cost-Effective Delivery of Amphotericin B

“…The drug is amphiphilic in nature, which is the foremost hurdle to be overcome in designing of an effective delivery system. Consequently, the need for modifying the existing dosage form is necessary to formulate a novel delivery system [4].…”

“…This formulation exhibited increased deposition on the skin. Confocal laser scanning microscopy (CLSM) determined the distribution of the formulation deeper into the skin [4].…”