Tetracycline-niosomes versus Tetracycline Hydrochloride-niosomes: How to Modulate Encapsulation and Percutaneous Permeation Properties

Abstract

Nowdays, the design of the optimalniosomal formulation may ensure the best performance in terms of physico-chemical properties and drug skin permeation. Our study want to propose the loading of Tetracycline or Tetracycline hydrocholoride drugs as strategy to modulate niosomes properties, with particular emphasis on encapsulation and percutaneous permeation behavior. Niosomes were prepared from mixtures of nonionic commercial surfactants with different final value of hydrophilelipophile balance (HLB). Significant increase in size respect to the corresponding empty vesicles occurred when drugs were encapsulated, while the presence of glyceryl monostearate resulted in a reduction of the diameter. Drugs entrapment efficiencies were found to be directly related to the chemical properties of the system: tetracycline showed better affinity for lipophilic matrices, while tetracycline hydrochloride was better encapsulated in hydrophilic ones. Finally we found drugs permeation across the skin was affected by many variables, such as bilayer composition, niosomes size, nature of the drugs and their entrapment efficiency, where by depending on the intended effect (topical or systemic) the opportune formulation may be selected.

<p>Potential of Nanoparticles as Permeation Enhancers and Targeted Delivery Options for Skin: Advantages and Disadvantages</p>

“…Surfactants with high HLB values are not capable of forming vesicle because of the high hydrophilicity of their molecules, but Spans and Tweens are suitable non-ionic surfactants for noisomes preparation. 66 One of the mechanisms responsible for skin penetration enhancement of niosomes is a reduction in trans-epidermal water loss (TEWL) and the other is fusion or adsorption of the vesicular drug delivery systems to the skin surface resulting in a higher concentration gradient and so higher skin penetration. Niosomes could also modify the stratum corneum structure and make it looser and more permeable.…”

Synthesis and Characterization of Thymol-Loaded Niosomal Film for the Prevention of Implant-Related Infection

“…Thymol was successfully incorporated into the niosome with 81% EE, which was a suitable encapsulation rate compared to that reported in the other studies [ 34 - 35 ] . Sohrabi et al [ 35 ] reported 73% efficiency for drug entrapment in niosomal carrier for moxifloxacin as a antimicrobial agent.…”

Enhancing Permeation of Drug Molecules Across the Skin via Delivery in Nanocarriers: Novel Strategies for Effective Transdermal Applications

“…Nonionic surfactants are safer, fairly non-toxic and biocompatible with the host, and can act as a thickening agent in TDD. Surfactants that exhibit increased HLB values are not capable to form a vesicle due to the advanced hydrophilicity of their particles, however, Tweens and Spans are ideal non-ionic surfactants for the preparation of noisome ( Tavano et al, 2017 ). One of the processes for enhanced permeation of niosomes through the skin is the elimination of trans-epidermal water loss (TEWL) while the alternate mechanism is the adsorption or fusion of the vesicles with skin lipids.…”