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. 2010 Jul;5(2):107-17.

Niosome as a drug carrier for topical delivery of N-acetyl glucosamine

M A Shatalebi  1 , S A Mostafavi, A Moghaddas
Affiliations

Niosome as a drug carrier for topical delivery of N-acetyl glucosamine

M A Shatalebi et al. Res Pharm Sci. 2010 Jul.

Abstract

Niosomes are non-ionic surfactant vesicles that have potential applications in the delivery of hydrophilic and hydrophobic drugs. The topical form of N-acetyl glucosamine (NAG) recently has been considered in the treatment of hyperpigmentation disorders due to its inhibitory effect on thyrosinase enzymes in melanocytes. To improve NAG penetration into the skin we formulated the drug in niosomes and investigated its flux across excised rat skin using Franz diffusion cells. The drug assay was performed by a novel and specific high performance liquid chromatography method. Niosomal vesicles were further characterized by optical and scanning electron microscopy and particle size analysis. Niosomes prepared with Span 40 produced a drug encapsulation of about 50%. The vesicle size was markedly dependent on the composition of the niosome formulations and was in range of 500-4500 nm (Span 80 < Span 60 < Span 40 niosomes). Span 40-niosomes provided a higher NAG flux across the skin than Span 60- and Span 80-nisomes. All formulations significantly improved the extent of drug assessed to be localized in the skin (P< 0.05), as compared to NAG hydroalcoholic (HA) solution. Our study demonstrated the potential of niosomes for improved NAG localization in the skin, as needed in hyperpigmentation disorders.

Keywords: HPLC; N-Acetyl Glucosamine; Noisome; Topical delivery.

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Figures

Fig. 1
Fig. 1
N-acetyl glucosamine chemical structure.
Fig. 2
Fig. 2
Representative HPLC chromatograms for NAG: (A) blank ethanol 96% solution; (B) NAG spike in ethanol 96% medium (10 µg/ml).
Fig. 3
Fig. 3
Optical micrographs of NAG niosomes prepared by film hydration method. A) Span 40:chol:DCP (2.8:3.35:1 mole ratio), B) Span 60:chol:DCP (2.8:3.35:1 mole ratio), C) Span 80:chol:DCP (2.8:3.35:1 mole ratio)
Fig. 4
Fig. 4
Scanning electron microscopy of NAG prepared by film hydration method. A) Span 40:chol:DCP (2.8:3.35:1 mole ratio), B) Span 60:chol:DCP (2.8:2.35:1 mole ratio), C) Span 80:chol:DCP (2.8.3.35:1 mole ratio).
Fig. 5
Fig. 5
The effects of surfactant type (B1: Span 40, B2: Span 60 and B3: Span 80) and its relative concentration (-1: low or 2.6 mole ratio, 0: medium or 2.9 mole ratio, and 1: high or 3.2 mole ratio) on the particle size (a), zeta potential (b), drug encapsulation efficiency (c), and drug skin permeability (d) of NAG-containing niosomes comprised of Span:chol:DCP (X:3.2:1, mole ratio).
Fig. 6
Fig. 6
Release profiles of NAG from niosomes into ethanol 96% through a cellulose acetate membrane using Franz diffusion cells, compared to the drug HA solution.
Fig. 7
Fig. 7
Comparison of drug permeation from NAGcontaining niosomes and HA solution through the rat skin into ethanol 96% at 37 °C. The points represent mean ± SD (n=3).
Fig. 8
Fig. 8
Comparison of drug permeability from NAGcontaining niosomes and HA solution through the rat skin into ethanol 96% at 37 °C.
Fig. 9
Fig. 9
Flux of drug from NAG-containing niosomes and HA solution through the rat skin into ethanol 96% at 37 °C.
Fig. 10
Fig. 10
Estimation of residual NAG on the rat skin after 24 h of topical administration of NAG-niosomes and HA solution.
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